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DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with GLENMARK PHARMACEUTICALS LTD, Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 29 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 29 year tenure till date Aug 2016, Around 30 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 9 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 25 Lakh plus views on dozen plus blogs, He makes himself available to all, contact him on +91 9323115463, email, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 13 lakh plus views on New Drug Approvals Blog in 212 countries...... , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc

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(±)-Integrifolin, Compound from plants keeps human cancer cells from multipying


CAS 89647-87-0

MFC15 H18 O4, MW 262.30
Azuleno[4,5-b]furan-2(3H)-one, decahydro-4,8-dihydroxy-3,6,9-tris(methylene)-, (3aR,4R,6aR,8S,9aR,9bR)-
  • Azuleno[4,5-b]furan-2(3H)-one, decahydro-4,8-dihydroxy-3,6,9-tris(methylene)-, [3aR-(3aα,4β,6aα,8β,9aα,9bβ)]-
  • (3aR,4R,6aR,8S,9aR,9bR)-Decahydro-4,8-dihydroxy-3,6,9-tris(methylene)azuleno[4,5-b]furan-2(3H)-one
  • 8-epi-Deacylcynaropicrin
  • 8β-Hydroxyzaluzanin C
  • Integrifolin (guaianolide)









WO 2011085979


Two New Amino Acid-Sesquiterpene Lactone Conjugates from Ixeris dentata


thumbnail image: Total Synthesis of (±)-IntegrifolinSTR1STR1STR1


Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim

Total Synthesis of (±)-Integrifolin

Compound from plants keeps human cancer cells from multipying

Read more at Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim

Weight control is an important concern of human beings, both for medical (pharmaceutical and/or nutraceutical) as well as non-therapeutic, e.g. cosmetic, reasons. More importantly, excessive accumulation of body fat (i.e. obesity (= adiposity), especially with excessive fat in the ventral region and surrounding the viscera) can be dangerous and has been linked to health problems such as type II diabetes, hypertension, heart disease, atherosclerosis (where more than two of the preceding disorders are present, the condition is often called “Metabolic Syndrome” or “syndrome X”), hyperlipidemia, coronary heart disease, stroke, breast and colon cancer, sleep apnoea, gallbladder disease, reproductive disorders such as polycystic ovarian syndrome, gastroesophageal reflux disease, increased incidence of complications of general anesthesia, fatty liver, gout or thromboembolism (see, e.g., Kopelman, Nature 404: 635-43 (2000)). Obesity reduces life-span and carries a serious risk of the co-morbidities listed above, as well disorders such as infections, varicose veins,

acanthosis nigricans, eczema, exercise intolerance, insulin resistance, hypertension hypercholesterolemia, cholelithiasis, orthopedic injury, and thromboembolic disease (Rissanen et al, Br. Med. J. 301 : 835-7 (1990)). Obesity is one of the main factors in the development of cardiovascular diseases. As a side effect the levels of cholesterol, blood pressure, blood sugar and uric acid in obese people are usually higher than those of persons of normal weight. The morbidity from coronary heart disease among the overweight people is increased as well. Among the people aged 40-50, mortality will rise about 1% when body weight increases by 0.5 kg and the death rate will increase 74% when body weight exceeds 25% of the standard. The prevalence of obesity in the United States has more than doubled since the turn of the last century (whole population) and more than tripled within the last 30 years among children aged from 6 to 11. This problem more and more becomes a disease risk also in Europe. In Germany, particularly many people have been found to suffer from overweight recently, already 25% of the young people, children and adolescents there are affected by obesity and related disorders. Furthermore, being overweight is considered by the majority of the Western population as unattractive.

Overweight and obesity result from an imbalance between the calories consumed and the calories used by the body. When the calories consumed exceed the calories burned, the body is in positive energy balance and over time weight gain will occur. The excess calories are stored in the fat cells. When the calories burned exceed the calories consumed, the body is in negative energy balance and over time weight loss will occur.

Determinants of obesity include social factors, psychological factors, genetic factors, developmental factors and decreased physical activity. Some components of a comprehensive weight loss programs include medical assessment, behavioural and dietary modification, nutrition education, mental and cognitive restructuring, increased physical activity, and long term follow-up.

An increasing interest by consumers in the maintenance or reduction of their body weight can be found. This leads to a demand for products useful for these purposes. Preferred are such food products which can conveniently be consumed as part of the daily diet, for example meal replacer products, such as meal replacer bars and beverages. These are usually designed for use as a single-serving food product to replace one or two meals a day.

An issue is that often a saturating effect is missed when such products are consumed, resulting in hunger feelings only a relatively short time after consummation or even in the lack of a saturation feeling already directly after consummation.

Summing up, there remains a need for new safe and effective compositions for promoting weight loss and/or loss of body fat in subjects such as humans. The problem to be solved by the present invention is therefore to find compositions or compounds useful in the treatment of obesity; and/or for improving the total cholesterol HDIJLDL ratio.

Phytochemistry provides a large pool of compounds and compositions to be looked at whether they are able to solve this problem.

The present invention provides methods and compositions useful in the control, treatment and prevention of obesity and obesity-related conditions, disorders, and diseases; and/or and/or for improving the total cholesterol HDL/LDL ratio.

Rosinski, G., et al., Endocrinological Frontiers in Phyiological Insect Ecology, Wroclow Technical University Press, Wroclow 1989, describe that certain tricyclic sequiterpene lactones, such as grossheimin and repin, showed inhibition of larval growth and antifeeding activity in Mealworm (Tenebrio σιοΐϊίοή. Grossheimin shows no anti-feeding but little decrease of absorption of digested food constituents and a little decrease in efficiency in digesting. Repin exhibit low effects at all. Both compounds show no effect on lipid levels in blood.

Shimoda, H., et al, Bioinorganic & Medicinal Chemistry Letters 13 (2003), 223-228, describe that methanolic extracts from Artichoke (Cynara sclolymus L.) with cynaropicrin, aguerin B and grossheimin as components and certain sesquiterpene glycosides suppress serum triglyceride elevation in olive oil-loaded mice. Some of these compounds exhibit a moderate short term (2 hours after olive oil administration) anti-hyperlipidemic activity presented as a lowering of the serum triglyceride (serum TG) concentrations, the long term (6 hours) show in the case of cynaropicrin and aguerine B an increase of the serum TG. Furthermore the authors present data of the gastric emptying (GE) of a methanolic ectract of artichoke. They determine a significantly inhibited GE. However, as shown below, this mechanism is not an explanation for the anti obesity effect shown in the present invention (see Example 1 ).

Fritzsche, J., et al., Eur. Food Res. Technol. 215, 149-157 (2002) describe the effect of certain isolated artichoke leaflet extract components with cholesterol lowering potential. Ahn, E.M-., et al, Arch Pharm. res. 29(1 1 ), 937-941 , 2006, shows ACAT inhibitory activity for two sesquiterpene lactones. KR 20040070985 also shows an effect of certain sesquiterpene lactone derivatives on cholesterol biosynthesis involved enzymes. Gebhard, R., Phytother. Res. 16, 368-372 (2002) and J. Pharmacol. Exp. Ther. 286(3), 1 122-1 128 (1998), shows

enforcement of cholesterol biosynthesis inhibition in HepG2 cells by artichoke extracts. WO 2007/006391 also claims reduction in cholesterol by certain Cynara scolymus variety extracts.

Other reported activities of tricyclic sesquiterpene lactones are antioxidant activity (European Food Research & Technology (2002), 215(2): 149-157), inhibitors of NF kb (Food Style 21 (2007), 1 1 (6): 54-56; JP 2006-206532), serum triglyceride increase-inhibitory effect (Kagaku Kogyo (2006), 57(10): 740-745), hypoglycaemic effect (J. Trad. Med. (2003), 20(2): 57-61), bitter taste (DE 2654184). Any beneficial effects are included in this invention by reference.

None of the documents suggest that a control and treatment of obesity and body fat in warmblooded animals might be possible.

Cynaropicrin, a tricyclic sesquiterpene lactone causes in vivo a strong weight loss. More surprisingly it was found that this effect is not correlated to a decrease in food intake. The weight balance is not affected by reduction of assimilation efficiency; the decrease of body fat and body weight is presumably caused by effects on energy metabolism. Surprisingly, it was found in addition that cynaropicrin also allows for improving the total cholesterol HDL7LDL ratio

Tricyclic sequiterpene lactones or known ingredients of plants of the subclass Asterides, especially from the family of Asteraceae, more specifically from species of the genera of the list consisting of Achilea, Acroptilon, Agranthus, Ainsliaea, Ajania, Amberboa, Andryala, Artemisia, Aster, Bisphopanthus, Brachylaena, Calea, Calycocorsus, Cartolepsis, Centaurea, Cheirolophus, Chrysanthemum, Cousinia, Crepis, Cynara, Eupatorium, Greenmaniella, Grossheimia, Hemistaptia, Ixeris, Jurinea, Lapsana, Lasiolaena, Liatris, Lychnophora, Macroclinidium, Mikania, Otanthus, Pleiotaxis, Prenanthes, Pseudostifftia, Ptilostemon,

Rhaponticum, Santolina, Saussurea, Serratula, Sonchus, Stevia, Taeckholmia, Tanacetum, Tricholepis, Vernonia, Volutarella, Zaluzania; even more specifically from species of the list consisting of Achillea clypeolata, Achillea collina, Acroptilon repens, Agrianthus pungens, Ainsliaea fragrans, Ajania fastigiata, Ajania fruticulosa, Amberboa lippi, Amberboa muricata, Amberboa ramose**, Amberboa tubuliflora and other Amberboa spp.*, Andryala integrifolia, Andryala pinnatifida, Artemisia absinthium, Artemisia cana, Artemisia douglasiana, Artemisia fastigiata, Artemisia franserioides, Artemisia montana, Artemisia sylvatica, Artemisia

tripartita, Aster auriculatus, Bishopanthus soliceps, Brachylaena nereifolia, Brachylaena perrieri, Calea jamaicensis, Calea solidaginea, Calycocorsus stipitatus, Cartolepsis intermedia, Centaurea babylonica, Centaurea bella, Centaurea canariensis*, Centaurea clementei, Centaurea conicum, Centaurea dealbata, Centaurea declinata, Centaurea glastifolia, Centaurea hermanii, Centaurea hyrcanica, Centaurea intermedia, Centaurea janeri, Centaurea kalscyi, Centaurea kandavanensis, Centaurea kotschyi, Centaurea linifolia, Centaurea macrocephala, Centaurea musimomum, Centaurea nicolai, Centaurea pabotii, Centaurea pseudosinaica, Centaurea repens, Centaurea salonitana, Centaurea scoparia, Centaurea sinaica, Centaurea solstitialis, Centaurea tweediei and other Centaurea spp. *, Cheirolophus uliginosus, Chrysanthemum boreale, Cousin ia canescens, Cousinia conifera, Cousinia picheriana, Cousinia piptocephala, Crepis capillaris, Crepis conyzifolia, Crepis crocea, Crepis japonica, Crepis pyrenaica, Crepis tectorum, Crepis virens, Crepis zacintha, Cynara alba, Cynara algarbiensis, Cynara auranitica, Cynara baetica, Cynara cardunculus, Cynara cornigera, Cynara cyrenaica, Cynara humilis, Cynara hystrix, Cynara syriaca, Cynara scolymus**, Cynara sibthorpiana and other Cynara spp.*, Eupatorium anomalum,

Eupatorium chinense, Eupatorium lindleyanum, Eupatorium mohrii, Eupatorium

rotundifolium, Eupatorium semialatum, Greenmaniella resinosa, Grossheimia

macrocephala** and other Grossheimia spp. *, Hemisteptia lyrata, Ixeris chinensis, Ixeris debilis, Ixeris dentata, Ixeris repens, Ixeris stolonifera, Jurinea carduiformis, Jurinea derderioides, Jurinea maxima, Lapsana capillaris, Lapsana communis, Lasiolaena morii, Lasiolaena santosii, Liatris chapmanii, Liatris gracilis, Liatris pycnostachya, Lychnophora blanchetii, Macroclinidium trilobum, Mikania hoehnei, Otanthus maritimus, Pleiotaxis rugosa, Prenanthes acerifolia, Pseudostifftia kingii, Ptilostemon diacanthus, Ptilostemon

gnaphaloides, Rhaponticum serratuloides, Santolina jamaicensis, Saussurea affinis,

Saussurea elegans, Saussurea involucrata, Saussurea laniceps, Saussurea neopulchella** and other Sauusurea spp. *, Serratula strangulata, Sonchus arborea, Stevia sanguinea, Taeckholmia arborea, Taeckholmia pinnata, Tanacetum fruticulosum, Tanacetum

parthenium, Tricholepis glaberrima** and other Tricholepsis spp. *, Vernonia arkansana, Vernonia nitidula, Vernonia noveboracensis, Vernonia profuga, Vernonia sublutea,

Volutarella divaricata, Zaiuzania resinosa; and can potentially be isolated from any part of the plants. Those genera and/or species marked with an asterisk (*) and especially those species marked with two asterisks (**) are especially preferred.

Appropriate plant material can be obtained from various sources, e.g. from:

Alfred Galke GmbH, Gittelde/Harz, Germany; Miiggenburg Pflanzliche Rohstoffe, Bad Bramstedt, Germany; Friedrich Nature Discovery, Euskirchen, Germany; VitaPlant AG, Uttwil, Switzerland; Amoros Nature SL, Hostalric, Spain.


Banksia integrifolia

Coast Banksia

Family: Proteaceae

Banksia integrifolia is a tall shrub or small tree 6 – 16m tall. It is common in sandy coastal areas, but also grows in the forests of tablelands. The light grey bark is hard and rough.

Mature leaves 5 -10 cm long, are stiff, entire (untoothed), dull dark green above and hairy-white underneath. They are generally lanceolate. Younger leaves are irregularly toothed and shorter than the mature leaves. The species name ‘integrifolia’ means whole-leaved.

The pale yellow flower spikes of Banksia integrifolia range from 7-14cm long and 7cm wide. The bent styles emerge from individual flowers on the spike, straightening and spreading.

A short time after flowering, the seed pods protrude cleanly from the woody cone and open to shed black, papery, winged seeds.

Banksia integrifolia flowers from January to June.




Total Synthesis of (±)-Integrifolin

  • DOI: 10.1002/chem.201601275

///////(±)-Integrifolin,  human cancer cells,  multipying


Gnidia glauca

Gnidia glauca


Search of complementary and alternative medicine has gained a thrust in the recent decade due to the pronounced side effects and health hazards of the chemically synthesized drugs. Hereby, a comprehensive knowledge about the traditionally used medicinal plants is indispensable for exploration of its novel bioactive components. One of such comparatively less explored medicinal plant is Gnidia glauca. Although, it has folkloric, traditional phytomedicinal and agrochemical applications in various parts of the world, still there are no available scientific validations or evidences to support the fact. In African medicine it is used for treatment of abdominal pain, cancers, wounds, snake bites, sore throat and burns. It is also well known for its piscicidal, insecticidal, molluscicidal and even homicidal activity for its use as arrow poisons. Similarly, its antineoplastic activity is reported to be remarkably superior [1]. However, till date there is no comprehensive information on the plant.

In view of the background, herein we present the first commentary on complete research carried out till date on G. glauca and its promises as complementary and alternative medicine (Figure 1).

Antimicrobial Activity
Plant pathogenic fungi are major cause of heavy losses in the crop yield as well as the economic turnover of the farmers. Hereby, development of eco-friendly herbal and cheap antifungal agents is of utmost importance. Aqueous extracts of various parts of G. glaucaexhibited variable mycelia inhibition against Phytophthora parasitica, a plant pathogenic fungi causing heart rot in pineapple. At a concentration of 5% the G. glauca seeds, leaves and barks showed an inhibition upto 19.16, 15.90 and 23.46%, respectively. Similarly, an enhanced activity was observed with a higher concentration at 10%, equivalent to 28.47, 34.59, 33.60% for seed, leaves and bark respectively [2]. A significant anticariogenic activity against Streptococcus mutans by the methanolic extract of G. glauca leaves was reported recently. The active extracts showed a high total phenolic (126.25 ± 0.20 μg GAE/ mg) and flavonoid (25.75 ± 0.10 μg CE/mg) content [3]. G. glauca bark extract is reported to have superior antibacterial activity against urinary tract infection causing pathogens likeEscherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Staphylococcus aureus and Enterococcus faecalisas compared to leaf and flower [4].
Back Ache and Joint Ache
According to ethnobotanical information, roots of G. glauca are widely used as a traditional medicine in Embu and Mbeere districts, Eastern Province of Kenya for treatment of back ache and joint ache [5].
Insecticidal and Larvicidal Activity
Leaves of G. glauca are used in Kenya as insecticidal agent [5]. Sequentially extracted hexane and chloroform extracts of dried bark ofG. glauca exhibited moderate mosquito larvicidal activity, whereas hexane, choloroform and MeOH extracts of fresh bark of the plant showed superior larvicidal activity against second instar larvae of Aedes aegypti. Maximum activity upto 100 % mortality was exhibited by the chloroform extract of fresh bark within a few minutes. Bioassay guided fractionation confirmed that compounds like bicoumarin and Pimelea factor P2 are mostly responsible for larvicidal activity [6]. Aqueous extract of G. glauca leaf and bark showed a notable ovicidal activity against the eggs of teak defoliator, Hyblaea puera Cramer upto 44.4 and 45.7 %, respectively [7]. In order to check the antileukemic and piscicidal activity of G. glauca, dried ground roots were extracted at room temperature with 95% ethanol under stirring condition for 24 h. The extract was further partitioned in various proportion of chloroform – water mixture to yield the gold fish piscitoxic fraction identified as gnidiglaucin (C32H46O10 ). However, the isolated compound failed to show inhibitory activity in in-vivo assay for antileukemic activity (P- 388) [8].
A recent ethnobotanical study on medicinal plants used by people in Zegie, Peninsula, Northwestern Ethiopia revealed that the root powder of G. glauca mixed with skimmed milk is taken orally for seven days for treatment of rabies [9].
Antioxidant Activity
The methanolic extract of G. glauca leaf with high antioxidant activity showed major phenolic content of 203.3 GAE/g. It could scavenge both ABTS (IC50 = 16.3 μg/mL) and nitric oxide (IC50 = 360.8 μg/mL) radicals. Further, FRAP value of 993.7 μm TE/mg was recorded at 30 min and 142.5 mg AAE/g of total antioxidant activity was evaluated [1]. In our previous report as well, we observed similar trend where the alcoholic extracts of G. glauca leaf showed high phenolic and flavonoid content. In case of pulse radiolysis generated hydroxyl radical scavenging second order rate constants of ethanolic extracts of G. glauca flower (4×106) was found to be very high indicating superior activity, followed by its leaf (3.73×106) and stem (3.66×106). Methanol extract of leaf showed efficient scavenging activity against DPPH radical, super oxide and nitric oxide radicals [10].
Antidiabetic Activity

Metabolic enzymes, like α-amylase and α-glucosidase are considered as key targets for discovery of antidiabetic drugs. Ethanolic, methanolic and ethyl acetate extracts of G. glauca flowers showed an excellent inhibitory potential (~70 % and above) against α-amylase while only methanol extract of leaf showed high inhibition against α-glucosidase [11].


The higher content of phenolics and flavonoids is responsible for the synthesis of gold nanoparticles by G. glauca flower extract. It showed one of the most rapid routes for synthesis to be completed entirely within just 20 min. The resulting AuNPs were small spheres with a diameter of 10 nm in majority. Exotic shapes like nanotriangles were also observed employing high resolution transmission electron microscopy along with other characterization tools. These AuNPs exhibited excellent catalytic properties in a reaction where 4-nitrophenol is reduced to 4-aminophenol by NaBH4 [12].
Toxicology Study
Toxicology studies to establish the safety of methanolic extract of G. glauca barks and roots involved the evaluation of acute oral toxicity in female rats. Neither mortality, nor morbidity was observed at administered dosages of 175, 550 and 2000 mg/kg body wt., which reveal the safety of these extracts in the doses up to 2000 mg/kg body weight. This study establishing that an LD50 value of G. glauca bark and root extracts, higher than 2000 mg/kg body weight is definitely advantageous for its clinical studies [13]. Thus it provided the scientific rationale supporting the wide usage of G. glauca for diverse therapeutic purposes [14].
G. glauca being one of the very important ethnomedicinal plant, will continue to be explored by researchers from various disciplines. In near future scientific discoveries, adding newer attributes to its therapeutic spectrum will surely enable it to emerge as one of the very vital model system, pivotal to many field of research like, pharmacognosy, pharmacy, phytochemistry, drug discovery and nanobiotechnology.

Professor B.A. Chopade

  M.Sc., Ph.D. Nottingham University, England
Fogarty Fellow Illinois University, Chicago, USAVice- Chancellor
Dr. Babasaheb Ambedkar Marathwada University
Maharashtra State, India

Ph.No. :  (office)  (0240)-2403111   Fax No.   (0240)-2403113/335
E-mail :

Balu A Chopade

Professor B.A. Chopade has been working as a Vice-Chancellor of Dr. Babasaheb Ambedkar Marathwada University, Aurangabad, Maharashtra from 04/06/2014. He has been working as Professor of Microbiology and Coordinator of University of Potential Excellence Programme (UPE Phase I & II) of UGC in Biotechnology at University of Pune. He was Director of Institute of Bioinformatics and Biotechnology (IBB), University of Pune from 2006 to 2012. He has established and developed IBB as a unique national institute and as a centre of excellence in research, innovation and teaching in biotechnology in India. He has successfully established an innovative benchmarking of publications in peer reviewed international journals of repute by undergraduate students at IBB. He was Head of the Department of Microbiology, University of Pune from 1994, 1996-2000 and 2003-2006. He has 35 years of experience in research, innovation, teaching and administration at the University of Pune.

Professor Chopade has several national and international academic honors and professional distinctions to his credits. He was the Government of India Scholar at the University of Nottingham, England and obtained a Ph.D. degree in microbiology and molecular genetics (1983-1986). He was also the recipient of the most prestigious Fogarty International NIH Research Fellowship Award from Govt. of USA for Post-Doctoral Research at the University of Illinois at Chicago (1994-1996) in genetic engineering. He is also recipient of International Award in Microbiology from International Union of Microbiological Societies (IUMS) in 1986. He has had very distinguished academic career and has carved his career entirely on the basis of merit and academic excellence.He was also coordinator of ALIS link programme between British Council London and Department of Microbiology, University of Pune (1994-1997).

He has published more than 100 research papers in peer reviewed international and national journals with high impact factor. The total impact factor of his research is more than 260, with h-index 26 and i10-index 52. His work is cited more than 2002 times ( He has obtained 2 USA and 8 Indian patents. His research work has been cited by Nobel Laureate Professor Arthur Kornberg from University of Stanford, California, USA. His pioneering work on e-DNA and Acinetobacter vesicles is also cited by “Nature” journal from England. His work also has been cited in 3 textbooks of microbiology published from USA and Europe. He has presented more than 150 papers in International and National Conferences and has given large number of plenary lectures. He has successfully supervised 27 Ph.D., 4 M.Phil. and 10 Post Doctoral scholars for their research. Currently 2 Post-Doctoral Fellows and 4 Ph.D. students are working with him. His 3 students had obtained Young Scientist Awards in 1993 at Stockholm, from International Congress of Chemotherapy (ICC), Europe. His research area includes microbial and molecular genetics, biotechnology and nanomedicine. He is on editorial board of Wealth of India Publication series, from CSIR New Delhi, as well as number of research journals. He has obtained research grants and funding of more than rupees 10 crores from national and international funding agencies. He has successfully completed 32 major research projects from various National and International funding agencies. He has developed a new herbal medicine “Infex” which is manufactured by Shrushti Herbal Pharma Ltd., Bangalore. He is a pioneer in the area of Industry-Academia interactions and entrepreneurship in biotechnology and microbiology at IBB, University of Pune.

He was a visiting scientist at the Pasteur Institute, Paris, France and King’s College, University of London in 1990. He has received number of awards and most notable are: Pradnya Bhushan Dr. Babasaheb Ambedkar Award(2014) Aurangabad. Bronze Medal, International Genetically Engineered Machines (iGEM), Massachusetts Institute of Technology (MIT), USA (2009), Pradnyavant Award (2011) by Undalkar Foundation, Karad. Maharashtra, Best teacher award by Pune Municipal Corporation (1993); Best research paper awards in microbial and molecular genetics (1988 & 2002) by Association of Microbiologist of India; He was recipient of Wadia Oration award (2008) by Institution of Engineers, India. Best research paper award in Bioinformatics (2009) by SBC, India. Summer Fellowship of Indian Academy of Sciences, Bangalore (2001). His biography is published by American Biographical Institute, USA (2000) and International Biographical Centre Cambridge (1991). He is member of American Society for Microbiology, USA and Society for General Microbiology, England since 1984. He is also a life member of number of national organizations like Association of Microbiologist of India (AMI) and Biotechnology Society of India (BSI), Society of Biological Chemists of India (SBC) Indian Science Congress (ISC). He is recipient of Marcus’s Who’s Who in Science and Engineering U.S.A. (2001), Marcus’s Who’s Who of the World, U.S.A. (2000), Marcus’s Who’s Who in Medicine, U.S.A. (2002), Marcus’s Who’s Who in Education, U.S.A. (2002).

He has been working on various authorities of University of Pune, as well as many State and Central Universities in India. Such as, Chairman, Board of Studies in Microbiology from 1997-2000 & 2005-2007. Member, BOS in Biotechnology (2005-2006, 2012-2017), Member of Academic Council (1997-2000 & 2000-2005) and Board of College and University Development (BCUD) of University of Pune from 1997-2000 & 2000-2005. Member, Faculty of Science, University of Pune (1997-2000, 2003-2005) and Member, Board of Teaching and Research (BUTR), (1997-2002). Member, Board of studies in Biochemistry and Molecular Biology, Central University Pondichery (2001-2003). Member, Board of Studies in Biochemistry and Molecular Biology, Shivaji University Kolhapur (2009-2014). Member, Board of Studies in Life Sciences, North Maharashtra University, Jalgaon (1994-1999). Member, Faculty of Science, Bharti Vidyapeeth Pune (2013-2018). Member, Faculty of Science, North Maharashtra University, Jalgaon (1990-1999).

He was chairman of large number of committees of UGC, New Delhi such as 11th Plan Research Committee, Research Projects and Deemed University Status since 2008. Chairman, International Travel Grants, (2008-2013). He was Chairman of State Eligibility Test (SET) in Microbiology for Govt. of Maharashtra and Goa from (1997-2000). He has active an involvement in the national and international scientific organizations. He has been involved in University administration in the various capacities for more than 33 years, as a chairman and member of large number of development, finance, examination and administration committees of University of Pune.

He is member of research and recognition committees of numerous state and central universities in India. He also worked as a coordinator of DBT Potential Excellence Programme at the Department of Microbiology, University of Pune (1994-1998). He is nominee of Department of Biotechnology, Government of India for Reliance Industries limited Mumbai, Biorefinery of Somaiya Group of Industries in Karnataka and Agharkar Research Institute (ARI) Pune.

His vision for Dr.Babasaheb Ambedkar Marathwada University (BAMU), Aurangabad is to transform it as one of the best research and innovation Universities in India and subsequently develop as a world class University.

///////Gnidia glauca Phytochemistry Ethnomedicine, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad, Maharashtra, india,  Balu A Chopade

Analysis of African plant reveals possible treatment for aging brain


Salk scientists find that a plant used for centuries by healers of São Tomé e Príncipe holds lessons for modern medicine

August 01, 2014

LA JOLLA—For hundreds of years, healers in São Tomé e Príncipe—an island off the western coast of Africa—have prescribed cata-manginga leaves and bark to their patients. These pickings from the Voacanga africana tree are said to decrease inflammation and ease the symptoms of mental disorders.

Now, scientists at the Salk Institute for Biological Studies have discovered that the power of the plant isn’t just folklore: a compound isolated from Voacanga africana protects cells from altered molecular pathways linked to Alzheimer’s disease, Parkinson’s disease and the neurodegeneration that often follows a stroke.

“What this provides us with is a source of potential new drug targets,” says senior author Pamela Maher, a senior staff scientist in Salk’s Cellular Neurobiology Laboratory. The results were published this week in the…

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Asparagusic acid

Asparagusic acid is the organosulfur with the formula S2(CH2)2CHCO2H. The molecule contains both carboxylic acid and disulfide functional groups. It is present in the vegetable asparagus and may be the metabolic precursor to other odorous thiol compounds.

The material was originally isolated from an aqueous extract of asparagus.

Biosynthetic studies revealed that asparagusic acid is derived from isobutyric acid. This colorless solid has a melting point (m.p.) of 75.7–76.5 °C. The corresponding dithiol (m.p. 59.5–60.5 °C) is also known; it is called dihydroasparagusic acid or dimercaptoisobutyric acid.

File:Asparagusic-acid-3D-balls.png3D MODEL

Over the past forty years several papers have been published on the subject, and several studies undertaken, to try and determine the chemical compounds responsible, and though there is still no definitive verdict as to the manner in which these compounds are formed, it has been suggested that they all form from asparagusic acid.

Asparagus Chemistry

Asparagusic acid is, unsurprisingly considering the name, a chemical found exclusively in asparagus, and absent in other related vegetables.

The asparagus-pee molecules that you smell come mostly from the breakdown of a molecule known as asparagusic acid, which is present naturally in asparagus. When your body breaks down asparagusic acid it forms a wide variety of chemicals, all of which contain sulfur!

This has made it an obvious candidate for being the origin of the peculiar effect that asparagus has on urine. It has been suggested by recent studies that it could be metabolised in the body to produce the volatile compounds found in the urine after consuming the vegetable.

Steamed asparagus prepared with roasted pine nuts

Many chemicals that contain sulfur atoms smell horrible in similar ways, and I have no idea why this is. This is one chemical/biological mystery that, much to my chagrin, remains unsolved in my head (internet people, if the reason is known, please help!).

Aside from sulfur, the thing that all these smelly asparagus-pee chemicals have in common is that they are “light” enough (a.k.a. they are “volatile”, which means they have a relatively low boiling point) that they can float up into the air and into your nose. That is partly why asparagus doesn’t smell like asparagus-pee, because asparagusic acid is not volatile (remember that word). In fact, asparagusic acid boils above 300 °C (>600 °F), so there is no way any of it gets into your nose!

Asparagus has been used as a vegetable and medicine, owing to its delicate flavour, diuretic properties, and more. It is pictured as an offering on an Egyptian frieze dating to 3000 BC. Still in ancient times, it was known in Syria and in Spain. Greeks and Romans ate it fresh when in season and dried the vegetable for use in winter; Romans would even freeze it high in the Alps, for the Feast of Epicurus. Emperor Augustus tossed off the “Asparagus Fleet” for hauling the vegetable, and coined the expression “faster than cooking asparagus” for quick action. A recipefor cooking asparagus is in the oldest surviving book of recipes, Apicius’s third-century AD De re coquinaria, Book III.

The ancient Greek physician Galen (prominent among the Romans) mentioned asparagus as a beneficial herb during the second century AD, but after the Roman empire ended, asparagus drew little medieval attention. until al-Nafzawi‘s The Perfumed Garden. That piece of writing celebrates its (scientifically unconfirmed) aphrodisiacal power, a supposed virtue that the IndianAnanga Ranga attributes to “special phosphorus elements” that also counteract fatigue. By 1469, asparagus was cultivated in French monasteries. Asparagus appears to have been hardly noticed in England until 1538, and in Germany until 1542.

The finest texture and the strongest and yet most delicate taste is in the tips. The points d’amour (“love tips”) were served as a delicacy to Madame de Pompadour. Asparagus became available to the New World around 1850, in the United States.

German botanical illustration of asparagus


Asparagus foliage turns bright yellow in autumn

Certain compounds in asparagus are metabolized to yield ammonia and various sulfur-containing degradation products, including various thiols andthioesters, which give urine a characteristic smell.

Some of the volatile organic compounds responsible for the smell are:

Subjectively, the first two are the most pungent, while the last two (sulfur-oxidized) give a sweet aroma. A mixture of these compounds form a “reconstituted asparagus urine” odor. This was first investigated in 1891 by Marceli Nencki, who attributed the smell to methanethiol. These compounds originate in the asparagus as asparagusic acid and its derivatives, as these are the only sulfur-containing compounds unique to asparagus. As these are more present in young asparagus, this accords with the observation that the smell is more pronounced after eating young asparagus. The biological mechanism for the production of these compounds is less clear.

The onset of the asparagus urine smell is remarkably rapid. The smell has been reported to be detectable 15 to 30 minutes after ingestion.

Gas chromatography-mass spectrometry was used to analyse the ‘headspace’ of urine produced after consumption of asparagus. The headspace is the gas space immediately above the liquid surface, which is occupied by light, volatile compounds in the liquid, and analysis of this is useful in identifying odour-causing compounds. The analysis of the post-asparagus urine showed the presence of several compounds that were not present, or present in negligible amounts, in normal urine. The primary compounds present, in quantities a thousand times greater than in normal urine, were methanethiol and dimethyl sulfide. The compounds dimethyl sulfide and dimethyl sulfone were also present and it was suggested that they modify the aroma to give it a ‘sweet’ edge.

Nutritional value per 100 g (3.5 oz)
Energy 85 kJ (20 kcal)
Carbohydrates 3.88 g
– Sugars 1.88 g
– Dietary fibre 2.1 g
Fat 0.12 g
Protein 2.2 g
Vitamin A equiv. 38 μg (5%)
– beta-carotene 449 μg (4%)
– lutein and zeaxanthin 710 μg
Thiamine (vit. B1) 0.143 mg (12%)
Riboflavin (vit. B2) 0.141 mg (12%)
Niacin (vit. B3) 0.978 mg (7%)
Pantothenic acid (B5) 0.274 mg (5%)
Vitamin B6 0.091 mg (7%)
Folate (vit. B9) 52 μg (13%)
Choline 16 mg (3%)
Vitamin C 5.6 mg (7%)
Vitamin E 1.1 mg (7%)
Vitamin K 41.6 μg (40%)
Calcium 24 mg (2%)
Iron 2.14 mg (16%)
Magnesium 14 mg (4%)
Manganese 0.158 mg (8%)
Phosphorus 52 mg (7%)
Potassium 202 mg (4%)
Sodium 2 mg (0%)
Zinc 0.54 mg (6%)

Link to USDA Database entry
Percentages are roughly approximated
using US recommendations for adults.
Source: USDA Nutrient Database



African medicine-cyclotides as an aid during child birth

Oldenlandia affinis was used by native women in the Zaire as an aid during childbirth. A tea was made of the leaves and imbibed during labour.

Cyclotides are plant-derived peptides of approximately 30 amino acids. They have the characteristic structural features of a head-to-tail cyclized backbone and a cystine knot arrangement of their three conserved disulfide bonds. Their unique structural features lead to exceptional stability. This and their amenability to chemical synthesis have made it possible to use cyclotides as templates in protein engineering and drug design applications.

David J Craik, University of Queensland, Brisbane, Australia, whose laboratory is working over 20 years in the field, summarizes the history of cyclotides

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more info on cyclotides

This is how it was discovered: a physician working in the Democratic Republic of Congo noticed that laboring women were drinking tea made from Oleanda affinis to induce childbirth. Theactive ingredient was the first cyclotide to be discovered. Since then, cyclotides have been shown to be antibiotic, antiviral and insecticidal.

Cyclotide structure.jpg
Figure 1. Structure and sequence of the prototypic cyclotide kalata B1

Cyclotides are small disulfide-rich proteins that have the unusual feature of a cyclic backbone (hence the name cyclo – peptides). They contain six conserved cystine residues that are arranged in a cystine knot topology in which two disulfide bonds and their connecting backbone segments form an embedded ring in the structure that is penetrated by a third disulfide bond, as shown below.

Cyclotides have a range of interesting biological activities including anti-HIV and neurotensin inhibition, anti-microbial activity and insecticidal activity. They are found in a variety of tropical plants from the Rubiaceae and Violaceae families.

The structure of kalata B1 showing the distorted beta-sheet topology and the loop nomenclature enabled by the cyclic backbone.

Cyclotides are small disulfide rich peptides isolated from plants.Typically containing 28-37 amino acids, they are characterized by their head-to-tail cyclised peptide backbone and the interlocking arrangement of their three disulfide bonds. These combined features have been termed the cyclic cystine knot (CCK) motif (Figure 1). To date, over 100 cyclotides have been isolated and characterized from species of the RubiaceaeViolaceae, and Cucurbitaceae families. Cyclotides have also been identified in agriculturally important families such as the Fabaceae and Poaceae.,

Cyclotides have been reported to have a wide range of biological activities, including anti-HIVinsecticidal, anti-tumour, antifouling, anti-microbialhemolyticneurotensinantagonism, trypsin inhibition, and uterotonic activities. An ability to induceuterine contractions was what prompted the initial discovery of kalata B1.

The potent insecticidal activity of cyclotides kalata B1 and kalata B2 has prompted the belief that cyclotides act as plant host-defence agents (Figure 2). The observations that dozens or more cyclotides may be present in a single plant and the cyclotide architecture comprises a conserved core onto which a series of hypervariable loops is displayed suggest that, cyclotides may be able to target many pests/pathogens simultaneously.

The cyclotides have been recognised as a family of novel circular proteins only in the last few years but the discovery of the first member of this family may be traced back to reports of native medicine applications in the early 1970s.

Kalata B1, was discovered because it is an active ingredient in a herbal medicine used by African women to assist childbirth . While on a Red Cross relief effort in the Congo region in the 1960s a Norwegian doctor, Lorents Gran, noted that during labour African women often ingested a tea made from leaves of the plant Oldenlandia affinis because of its uterotonic effects. The active ingredient was determined to be a peptide that was named kalata B1, after the local name for the native medicine. Subsequent in vivo studies in rats confirmed uterotonic activity of the purified peptide but it was not characterised as a macrocyclic peptide until some 20 year later.

The mid-1990�s was a key period in the discovery of macrocyclic peptides, with several independent groups discovering such peptides while screening for various biological activities and our group determining the three dimensional structure of kalata B1 . In the first fortuitous discovery Sch�pke et al., examined Viola arvensis and V. tricolor in a study aimed at the discovery of new saponins. While assaying for the usual hemolytic activity of saponins they discovered a macrocyclic peptide, violapeptide I, with hemolytic activity. At around the same time bio-assay driven screens for anti-HIV and anti-neurotensin activity led to the discovery of the circulins and cyclopsychotride A respectively.

Viola arvensis a cyclotide containing plant. Member of the violaceae family and found in temperate regions of Australia and Europe.

With our report of the three dimensional structure of kalata B1 in 1995 and its sequence homology with the circulins and cyclopsychotride A, we became convinced that macrocyclic peptides might be more common than had earlier been thought and we began searching for other examples. Several other macrocyclic peptides were found in the late 1990s and it became clear that the peptides formed part of a family that we subsequently named the cyclotides.

Several novel cyclotide sequences have been discovered in the last few years , with the known sequences now exceeding 45 and many more currently being characterized in our laboratories. A large proportion of the new cyclotides have been discovered based on their structural properties rather than biological activities. The cyclotides are relatively hydrophobic and can be readily identified from crude plant extracts by their characteristically late elution on RP-HPLC.

The cyclotides described above, all come from plants in the Rubiaceae or Violaceae families but the prevalence of macrocyclic peptides has recently been expanded to include the Cucurbitaceae family. This is based on the discovery of the trypsin inhibitors MCoTI-I and MCoTI-II, 34 residue macrocyclic peptides, from Momordica cochinchinensis . They have no sequence homology to the previously characterized cyclotides, with the exception of the six cysteine residues, but are of a similar size and contain a cystine knot motif (Felizmenio-Quimio, 2001). The MCoTI peptides were originally isolated based on their trypsin inhibitory activity and are homologous to linear cystine knot peptides from the squash family of trypsin inhibitors such as EETI-II and CMTI.


Bokesch HR, Pannell LK, Cochran PK, Sowder RC, 2nd, McKee TC and Boyd MR: A novel anti-HIV macrocyclic peptide from Palicourea condensata. J. Nat. Prod. (2001) 64:249-250.

Broussalis AM, Goransson U, Coussio JD, Ferraro G, Martino V and Claeson P: First cyclotide from Hybanthus (Violaceae). Phytochemistry (2001) 58:47-51.

Claeson P, G�ransson U, Johansson S, Luijendijk T and Bohlin L: Fractionation protocol for the isolation of polypeptides from plant biomass. J. Nat. Prod. (1998) 61:77-81.

Craik DJ, Daly NL, Bond T and Waine C: Plant cyclotides: A unique family of cyclic and knotted proteins that defines the cyclic cystine knot structural motif. J. Mol. Biol. (1999) 294:1327-1336.

G�ransson U, Luijendijk T, Johansson S, Bohlin L and Claeson P: Seven novel macrocyclic polypeptides from Viola arvensis. J. Nat. Prod. (1999) 62:283-286.

Gran L: Isolation of oxytocic peptides from Oldenlandia affinis by solvent extraction of tetraphenylborate complexes and chromatography on sephadex LH-20. Lloydia (1973a) 36:207-208.

Gran L: On the effect of a polypeptide isolated from “Kalata-Kalata” (Oldenlandia affinis DC) on the oestrogen dominated uterus. Acta Pharmacol. Toxicol. (1973b) 33:400-408.

Gustafson KR, Sowder II RC, Henderson LE, Parsons IC, Kashman Y, Cardellina II JH, McMahon JB, Buckheit Jr. RW, Pannell LK and Boyd MR: Circulins A and B: Novel HIV-inhibitory macrocyclic peptides from the tropical tree Chassalia parvifolia. J. Am. Chem. Soc. (1994) 116:9337-9338.

Hallock YF, Sowder RCI, Pannell LK, Hughes CB, Johnson DG, Gulakowski R, Cardellina JHI and Boyd MR: Cycloviolins A-D, anti-HIV macrocyclic peptides from Leonia cymosa. J. Org. Chem.(2000) 65:124-128.

Hernandez JF, Gagnon J, Chiche L, Nguyen TM, Andrieu JP, Heitz A, Trinh Hong T, Pham TT and Le Nguyen D: Squash trypsin inhibitors from Momordica cochinchinensis exhibit an atypical macrocyclic structure. Biochemistry (2000) 39:5722-5730.

Saether O, Craik DJ, Campbell ID, Sletten K, Juul J and Norman DG: Elucidation of the primary and three-dimensional structure of the uterotonic polypeptide kalata B1. Biochemistry (1995) 34:4147-4158.

Sch�pke T, Hasan Agha MI, Kraft R, Otto A and Hiller K: H�molytisch aktive komponenten aus Viola tricolor L. und Viola arvensis Murray. Sci. Pharm. (1993) 61:145-153.

Witherup KM, Bogusky MJ, Anderson PS, Ramjit H, Ransom RW, Wood T and Sardana M: Cyclopsychotride A, A biologically active, 31-residue cyclic peptide isolated from Psychotria Longipes. J. Nat. Prod. (1994) 57:1619-1625.

Study Finds Substances from African Medicinal Plants Could Help Stop Tumour Growth



Sections of the root of the giant globe thistle.

photo: Victor Kuete, Institute of Pharmaceutical Sciences and Biochemistry

African medicinal plants contain chemicals that may be able to stop the spread of cancer cells. This is the conclusion of researchers following laboratory experiments conducted at Johannes Gutenberg University Mainz (JGU). The plant materials will now undergo further analysis in order to evaluate their therapeutic potential.

“The active substances present in African medicinal plants may be capable of killing off tumour cells that are resistant to more than one drug. They thus represent an excellent starting point for the development of new therapeutic treatments for cancers that do not respond to conventional chemotherapy regimens,” explained Professor Thomas Efferth of the Institute of Pharmaceutical Sciences and Biochemistry – Therapeutic Life Sciences at Mainz University. For the past four years, Efferth and biochemist Dr. Victor Keute of the University of Dschang in Cameroon have been studying the active substances in African plants such as the giant globe thistle, wild pepper, speargrass, and Ethiopian pepper.

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