- Djaja D. Soejarto is Professor Emeritus at the University of Illinois at Chicago (UIC), College of Pharmacy, Chicago,... moreDjaja D. Soejarto is Professor Emeritus at the University of Illinois at Chicago (UIC), College of Pharmacy, Chicago, Illinois, USA. He earned his Ph.D. degree (Biology/Botany) in 1968 from Harvard University and served, shortly after, as Fellow of the Latin American Teaching Fellowships, Fletcher School of Law and Diplomacy, Tufts University, Medford, Massachusetts, USA, in a mission assignment to the Department of Biology, University of Antioquia, Medellin, Colombia (1969-1972). In 1969, he founded the Herbarium of the University of Antioquia (acronym: HUA). He served as a postdoctoral Fellow in Ethnopharmacology at Harvard University under the mentorship of Professor Richard Evans Schultes. He was the Principal Investigator of a National Cancer Institute (NCI) of the National Institutes of Health (NIH), USA, contract, on Plant Explorations and Collections under UIC (1986-2004) and was the Principal Investigator of a multinational, multidisciplinary program called the International Cooperative Biodiversity Groups (ICBG) Program of the Fogarty International Center, NIH (1998-2010). Under grants from the California Community Foundation (CCF) (2013-2014; 2019-2023) and the National Cancer Institute, NIH, USA (2015-2020), he carried out collaborative field research in Laos with colleagues at UIC and at the Institute of Traditional Medicine, Ministry of Health, Vientiane, Lao PDR (Laos) on medicinal plants, focusing on ethnobotanical inventory, medicinal plant conservation, community engagement and discovery of biologically active compounds from plants of Laos. He served as Editor of the Journal of Ethnopharmacology (1988-2004) and is recipient of a Plaque of Honor for his contribution "to the Development of the Science of Botany in Colombia" from the Colombian Association of Botany (2006); "Distinguished Economic Botanist Award" from the Society of Economic Botany (2012); “Norman R. Farnsworth Excellence in Botanical Research Award” from the American Botanical Council (2012); "The Tyler Prize Award" from the Amercan Society of Pharmacognosy (2022). He is author and co-author of more than 200 peer reviewed papers with a focus on plant taxonomy, medicinal plant studies, plant-derived sweetening agents, drug discovery from plants, and conservation of medicinal plants; 22 book chapters; and 26 symposium proceedings..edit
- Professor Andree Joph Kostermans (plant taxonomy), Professor Richard Evans Schultes (plant taxonomy; ethnobotany), and Professor Norman R. Farnsworth (drug discovery from plants). edit
ContextWhether natural product drug discovery programs should rely on wild plants collected “randomly” from the natural environment, or whether they should also include plants collected on the basis of use in traditional medicine remains... more
ContextWhether natural product drug discovery programs should rely on wild plants collected “randomly” from the natural environment, or whether they should also include plants collected on the basis of use in traditional medicine remains an open question.ObjectiveThis study analyzes whether plants with ethnomedical uses from Vietnam and Laos have a higher hit rate in bioassay testing than plants collected from a national park in Vietnam with the goal of maximizing taxonomic diversity (“random” collection).Materials and MethodsAll plants were extracted and subjected to bioassay in the same laboratories. Results of assays of plant collections and plant parts (samples) were scored as active or inactive based on whether any extracts had a positive result in a bioassay. Contingency tables were analyzed using χ2 statistics.ResultsRandom collections had a higher hit rate than ethnomedical collections, but for samples, ethnomedical plants were more likely to be active. Ethnomedical collections and samples had higher hit rates for tuberculosis, while samples, but not collections, had a higher hit rate for malaria. Little evidence was found to support an advantage for ethnomedical plants in HIV, chemoprevention and cancer bioassays. Plants whose ethnomedical uses directly correlated to a bioassay did not have a significantly higher hit rate than random plants.DiscussionPlants with ethnomedical uses generally had a higher rate of activity in some drug discovery bioassays, but the assays did not directly confirm specific uses.ConclusionsEthnomedical uses may contribute to a higher rate of activity in drug discovery screening.
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Plant Resources of South-East Asia 12: (2) Medicinal and Poisonous Plants 2 Edited by J. L. C. H. van Valkenburg (Prosea Publication Office, Indonesia) and N. Bunyapraphatsara (Mahidol University, Bangkok). Backhuys Publishers, Leiden, The Netherlands. 2001. 785 pp. 350 Dutch Guilders. ISBN 90-5...more
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The pregnane steroid, (E)-aglawone, along with four known triterpenes, and a known sterol mixture were isolated from the bark of Aglaia lawii (Wight) Saldanha ex Ramamoorty (Meliaceae). The structural determination/identification was... more
The pregnane steroid, (E)-aglawone, along with four known triterpenes, and a known sterol mixture were isolated from the bark of Aglaia lawii (Wight) Saldanha ex Ramamoorty (Meliaceae). The structural determination/identification was accomplished by a combination of 1D- and 2D-NMR spectroscopic techniques. The relative stereochemistry of the known triterpene, 20S,24S-epoxydammarane-3alpha,25-diol acetate, was also unequivocally determined for the first time by X-ray crystallography. The isolates were not active against various human cancer cell lines.
Research Interests: Chemistry, Phytochemistry, Medicinal Plants, Magnetic Resonance Spectroscopy, Medicine, and 11 moreMacromolecular X-Ray Crystallography, Biological Sciences, Cell line, CHEMICAL SCIENCES, Molecular Conformation, Phytosterols, Spectroscopic Techniques, X Ray Crystallography, Structure Determination, Molecular Structure, and Medical and Health Sciences
Many of the clinically used anticancer agents in Western medicine are derived from secondary metabolites found in terrestrial microbes, marine organisms, and higher plants, with additional compounds of this type being currently in... more
Many of the clinically used anticancer agents in Western medicine are derived from secondary metabolites found in terrestrial microbes, marine organisms, and higher plants, with additional compounds of this type being currently in clinical trials. If plants are taken specifically, it is generally agreed that the prospects of encountering enhanced small organic-molecule chemical diversity are better if tropical rather than temperate species are investigated in drug discovery efforts. Plant collection in tropical source countries requires considerable preparation and organization to conduct in a responsible manner that abides by the provisions of the 1992 Rio Convention of Biological Diversity and the 2010 Nagoya Protocol on Access to Genetic Resources. Correct taxonomic identifications and enhanced procedures for processing and documenting plant samples when collected in often difficult terrain are required. Phytochemical aspects of the work involve solvent fractionation, known compound dereplication, preliminary in vitro testing, and prioritization, leading to "activity-guided fractionation", compound structure determination, and analog development. Further evaluation of lead compounds requires solubility, formulation, preliminary pharmacokinetics, and in vivo testing in suitable models. Covering the work of the authors carried out in two sequential multidisciplinary, multi-institutional research projects, examples of very promising compounds discovered from plants acquired from Africa, Southeast Asia, the Americas, and the Caribbean region, and with potential anticancer activity will be mentioned. These include plant secondary metabolites of the diphyllin lignan, cyclopenta[b]benzofuran, triterpenoid, and tropane alkaloid types.
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Herbarium voucher specimens are used primarily for taxonomic confirmation. However, they also afford a record of the metabolic profile of a plant, potentially at the time it was collected, or at the very least, at the time of analysis.... more
Herbarium voucher specimens are used primarily for taxonomic confirmation. However, they also afford a record of the metabolic profile of a plant, potentially at the time it was collected, or at the very least, at the time of analysis. Even with the enhanced sensitivity of modern analytical techniques, analysis of the metabolites of a herbarium voucher requires removal and consumption of at least part of an entire specimen. We present herein a non-destructive method to analyze the metabolites of herbarium voucher specimens with the droplet-liquid microjunction-surface sampling probe (droplet probe) coupled to ultra-performance liquid chromatography and highresolution mass spectrometry. As proof of concept, a herbarium voucher specimen of Garcinia mangostana (mangosteen) was utilized due to the well-characterized xanthones biosynthesized by this plant, which are of interest as potential anticancer agents. Also, the juice of the fruits of this plant is used widely in the United States and in other countries as a botanical dietary supplement. Metabolite profiles of the sampled surfaces were compared to a subset of xanthone standards. Using this innovative method on the herbarium voucher specimen, we were able to readily identify cytotoxic prenylated xanthones while maintaining the integrity of the entire specimen.
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The Vietnam-Laos International Cooperative Biodiversity Group (ICBG) based at the University of Illinois at Chicago (UIC) catalyzed a country-wide network of medicinal plant preserves (MPP) and medicinal biodiversity preserves (MBP) now... more
The Vietnam-Laos International Cooperative Biodiversity Group (ICBG) based at the University of Illinois at Chicago (UIC) catalyzed a country-wide network of medicinal plant preserves (MPP) and medicinal biodiversity preserves (MBP) now established in ten provinces of the Lao People's Democratic Republic (Lao PDR), which are relied upon as protected sources of ethnomedicines for local villagers and traditional healers. In collaboration with the Lao PDR's Institute of Traditional Medicine (ITM), our ongoing P01 Program Project (Ohio State University) examined the anticancer bioprospecting potential for two of the most exhaustively inventoried of these sites: the Bolikhamxay MPP and the Xiengkhouang MBP. Guided by prior voucher specimens sourced from these preserves with an overwhelming emphasis on plants employed in traditional medicine, 201 distinct samples from 96 species were collected along with proper herbarium documentation. Aliquots of these plant samples were extracte...
Research Interests: Botany, Ethnobotany, Complementary and Alternative Medicine, Traditional Medicine, Tropical Ecology, and 15 morePlant Biology, Cancer, Biological Activity Of Natural Products, Ethnopharmacology, Pharmacognosy, Medicinal Plants, Medicine, Economic botany, Medicinal plants and natural products, Bioprospecting, Tropical forest, Natural product research, Colon cancer, Medicinal Plant, and Pharmacology and pharmaceutical sciences
The International Cooperative Biodiversity Groups (ICBG) Program based at the University of Illinois at Chicago (UIC) is a program aimed to address the interdependent issues of inventory and conservation of biodiversity, drug discovery... more
The International Cooperative Biodiversity Groups (ICBG) Program based at the University of Illinois at Chicago (UIC) is a program aimed to address the interdependent issues of inventory and conservation of biodiversity, drug discovery and sustained economic growth in both developing and developed countries. It is an interdisciplinary program involving the extensive synergies and collaborative efforts of botanists, chemists and biologists in the countries of Vietnam, Laos and the USA. The UIC-ICBG drug discovery efforts over the past 18 years have resulted in the collection of a cumulative total of more than 5500 plant samples (representing more than 2000 species), that were evaluated for their potential biological effects against cancer, HIV, bird flu, tuberculosis and malaria. The bioassay-guided fractionation and separation of the bioactive plant leads resulted in the isolation of approximately 300 compounds of varying degrees of structural complexity and/or biological activity. ...
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Justicia gendarussa, a medicinal plant collected in Vietnam, was identified as a potent anti-HIV-1 active lead from the evaluation of over 4500 plant extracts. Bioassay-guided separation of the extracts of the stems and roots of this... more
Justicia gendarussa, a medicinal plant collected in Vietnam, was identified as a potent anti-HIV-1 active lead from the evaluation of over 4500 plant extracts. Bioassay-guided separation of the extracts of the stems and roots of this plant led to the isolation of an anti-HIV arylnaphthalene lignan (ANL) glycoside, patentiflorin A (1). Evaluation of the compound against both the M- and T-tropic HIV-1 isolates showed it to possess a significantly higher inhibition effect than the clinically used anti-HIV drug AZT. Patentiflorin A and two congeners were synthesized, de novo, as an efficient strategy for resupply as well as for further structural modification of the anti-HIV ANL glycosides in the search for drug leads. Subsequently, it was determined that the presence of a quinovopyranosyloxy group in the structure is likely essential to retain the high degree of anti-HIV activity of this type of compounds. Patentiflorin A was further investigated against the HIV-1 gene expression of th...
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Three new (1-3) and two known (4 and 5) cytotoxic cardiac glycosides were isolated and characterized from a medicinal plant, Streblus asper Lour. (Moraceae), collected in Vietnam, with six new analogues and one known derivative (5a-g)... more
Three new (1-3) and two known (4 and 5) cytotoxic cardiac glycosides were isolated and characterized from a medicinal plant, Streblus asper Lour. (Moraceae), collected in Vietnam, with six new analogues and one known derivative (5a-g) synthesized from (+)-strebloside (5). A preliminary structure-activity relationship study indicated that the C-10 formyl and C-5 and C-14 hydroxy groups and C-3 sugar unit play important roles in the mediation of the cytotoxicity of (+)-strebloside (5) against HT-29 human colon cancer cells. When evaluated in NCr nu/nu mice implanted intraperitoneally with hollow fibers facilitated with either MDA-MB-231 human breast or OVCAR3 human ovarian cancer cells, (+)-strebloside (5) showed significant cell growth inhibitory activity in both cases, in the dose range 5-30 mg/kg.
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In a search for new anti-HIV active leads from over several thousands of plant extracts, we have identified a potent plant lead. The active plant is determined as Justicia gendarussa (Acanthaceae), a medicinal plant that has been used for... more
In a search for new anti-HIV active leads from over several thousands of plant extracts, we have identified a potent plant lead. The active plant is determined as Justicia gendarussa (Acanthaceae), a medicinal plant that has been used for the treatment of injury, arthritis and rheumatism in Asia including China. Our bioassay-guided fractionation of the methanol extract of the stems and barks of the plant led to the isolation of two anti-HIV compounds, justiprocumins A and B. The compounds are identified as new arylnaphthalide lignans (ANL) glycosides. We further determined that the ANL glycosides are the chemical constituents that contribute to the anti-HIV activity of this plant. Justiprocumin B displayed potent activity against a broad spectrum of HIV strains with IC50 values in the range of 15-21 nM (AZT, IC50 77-95 nM). The compound also displayed potent inhibitory activity against the NRTI (nucleoside reverse transcriptase inhibitor)-resistant isolate (HIV-11617-1) of the analo...
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Three new rotenoids (1-3), two new isoflavonoids (4 and 5), and six known analogues (6-11) were isolated from an n-hexane partition of a methanol extract of the fruits of Millettia caerulea, with the structures of the new compounds... more
Three new rotenoids (1-3), two new isoflavonoids (4 and 5), and six known analogues (6-11) were isolated from an n-hexane partition of a methanol extract of the fruits of Millettia caerulea, with the structures of the new compounds elucidated by analysis of their spectroscopic data. The relative configurations of the rotenoids were determined by interpretation of their NMR spectroscopic data, and their absolute configurations were established using electronic circular dichroism spectra and specific rotation values. All compounds isolated were evaluated for their cell growth inhibitory activity against the HT-29 human colon cancer cell line, and the known compounds, (-)-3-hydroxyrotenone (6) and (-)-rotenone (7), were found to be potently active. When tested in an NF-κB inhibition assay, compound 6 showed activity. This compound, along with the new compound, (-)-caeruleanone D (1), and the known compound, ichthynone (8), exhibited K-Ras inhibitory potency. Further bioactivity studies...
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Seven (7) species of Araceae representing new records for the flora of Cuc Phuong National Park are communicated: Aglaonema tunuipes , Alocasia odora , Amorphophallus coaetaneus , Amorphophallus dzui , Amorphophallus interruptus ,... more
Seven (7) species of Araceae representing new records for the flora of Cuc Phuong National Park are communicated: Aglaonema tunuipes , Alocasia odora , Amorphophallus coaetaneus , Amorphophallus dzui , Amorphophallus interruptus , Schismatoglottis harmandii and Steudnera colocasiifolia . Schimatoglottis Zoll. et Moritzi and Steudnera C. Koch represent new genus-records for the park, while Steudnera colocasiifolia represents a new species-record for the flora of Vietnam. For each species, the correct nomenclature, brief descriptions, specimen record, habitat and taxonomic relationships were discussed. Advances in Natural Sciences Vol.4, No.4 (2003) (317-330)
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Litsea verticillata Hance (Lauraceae), a Chinese medicine used to treat swelling caused by injury or by snake bites, was the first plant identified by our National Institutes of Health (NIH)-funded International Cooperative Biodiversity... more
Litsea verticillata Hance (Lauraceae), a Chinese medicine used to treat swelling caused by injury or by snake bites, was the first plant identified by our National Institutes of Health (NIH)-funded International Cooperative Biodiversity Group (ICBG) project to exhibit anti-HIV activities. From this plant, we discovered a class of 8 novel litseane compounds, prototypic sesquiterpenes, all of which demonstrated anti-HIV activities. In subsequent studies, 26 additional compounds of different structural types were identified. During our continuing investigation of this plant species, we identified two new litseanes, litseaverticillols L and M, and a new sesquiterpene butenolide, litseasesquibutenolide. Litseaverticillols L and M were found to inhibit HIV-1 replication, with an IC[Formula: see text] value of 49.6[Formula: see text][Formula: see text]M. To further determine the antiviral properties of this plant, several relatively abundant isolates, including a litseane compound, two eud...
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Tuberculosis (TB) is a highly contagious disease mainly caused by Mycobacterium tuberculosis H37 RV . Antitubercular (anti-TB) bioassay-guided isolation of the CHCl3 extract of the leaves and stems of the medicinal plant Ardisia... more
Tuberculosis (TB) is a highly contagious disease mainly caused by Mycobacterium tuberculosis H37 RV . Antitubercular (anti-TB) bioassay-guided isolation of the CHCl3 extract of the leaves and stems of the medicinal plant Ardisia gigantifolia led to the isolation of two anti-TB 5-alkylresorcinols, 5-(8Z-heptadecenyl) resorcinol (1) and 5-(8Z-pentadecenyl) resorcinol (2). We further synthesized 15 derivatives based on these two natural products. These compounds (natural and synthetic) were evaluated for their anti-TB activity against M. tuberculosis H37 RV . Resorcinols 1 and 2 exhibited anti-TB activity with MIC values at 34.4 μM and 79.2 μM in MABA assay, respectively, and 91.7 μM and 168.3 μM in LORA assay, respectively. Among these derivatives, compound 8 was found to show improved anti-TB activity than its synthetic precursor (2) with MIC values at 42.0 μM in MABA assay and 100.2 μM in LORA assay. The active compounds should be regarded as new hits for further study as a novel cl...
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In an effort to preserve traditional medicine knowledge and to uncover information about disease patterns and treatment in the Lao People's Democratic Republic (PDR), linguistic experts have scanned centuries-old medical palm leaf... more
In an effort to preserve traditional medicine knowledge and to uncover information about disease patterns and treatment in the Lao People's Democratic Republic (PDR), linguistic experts have scanned centuries-old medical palm leaf manuscripts for disease entries. A list of more than 7000 diseases has resulted, shedding valuable light onto the medical history and traditional medicine heritage of the people of Laos, as well as providing an index for faster research into specific diseases and their traditional treatments.
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A field survey was launched to identify medicinal plants growing in the Khiat Ngong wetlands and surrounding forested areas of Pathoumphone District, Champasak Province in southern Laos. In this area, 418 plants representing approximately... more
A field survey was launched to identify medicinal plants growing in the Khiat Ngong wetlands and surrounding forested areas of Pathoumphone District, Champasak Province in southern Laos. In this area, 418 plants representing approximately 250 species, belonging to at least 200 genera in 93 families of vascular plants, are used by traditional healers to treat more than 95 symptoms. A large number of species are used for treating fever. At least 14 plant species have not been previously reported for having medicinal properties. At least 10 have previously been investigated and have shown interesting biological activity by other researchers, signaling promising candidates for income-generating activities.
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As a part of the UIC-based ICBG project in Laos, plants were collected based on ethnomedical interviews and evaluated for antimalarial activity. A CHCl3 extract from the vine of Gongronema napalense (Wall.) Decne. (Asclepiadaceae) showed... more
As a part of the UIC-based ICBG project in Laos, plants were collected based on ethnomedical interviews and evaluated for antimalarial activity. A CHCl3 extract from the vine of Gongronema napalense (Wall.) Decne. (Asclepiadaceae) showed promising anti-malarial activity while exhibiting low levels of cytotoxicity and was thus followed up with further fractionation and biological evaluation. Bioassay-guided fractionation led to the isolation of a new steroidal glycoside, gongroneside A, which showed antimalarial activity in vitro with an IC50 value of 1.60 and 1.39 μM against the Plasmodium falciparum D6 and W2 clones, respectively.
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(+)-Gossypol was isolated from the bark of Thespesia populnea and tested for its ability to inhibit the fertility of male hamsters. Male hamsters of proven fertility were treated orally for 54 days with 40 mg/kg of (+)-gossypol, 40 mg/kg... more
(+)-Gossypol was isolated from the bark of Thespesia populnea and tested for its ability to inhibit the fertility of male hamsters. Male hamsters of proven fertility were treated orally for 54 days with 40 mg/kg of (+)-gossypol, 40 mg/kg of racemic gossypol, or 5% gum acacia (vehicle control) and were mated with estrous female hamsters during the fourth and seventh weeks of treatment. Both the control and the (+)-gossypol-treated animals exhibited normal fertility throughout the experiment. The racemic gossypol-treated animals were infertile when evaluated during both the fourth and seventh weeks of treatment. Morphologic examination of the testicular tissue could not explain the loss of fertility. These data demonstrate the inability of (+)gossypol to decrease male fertility and suggest that the activity of racemic gossypol may be due primarily to the presence of the (-) optical isomer.
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It is an accepted fact that the tropical rain forests are the richest biome on earth. It is also an accepted fact that the tropical rain forests still represent one of the last and true great frontiers of wilderness, which still evoke awe... more
It is an accepted fact that the tropical rain forests are the richest biome on earth. It is also an accepted fact that the tropical rain forests still represent one of the last and true great frontiers of wilderness, which still evoke awe and wonderment. Sadly, however, this state of affairs may not last long enough into the future for man to unlock all their secrets. In view of the fact that our institution is currently involved with the U.S. National Cancer Institute's recently resurrected plant program [1], and mindful of warnings from conservationists that the tropical rain forests or tropical moist forests or simply rain forests [2] may be decimated within the next decade or so, in addition to a concern brought by personal knowledge of the situation through a number of years of field and laboratory experience, we consider it timely to put into perspective the prospect that this tropical biome may still contribute to the alleviation of human sufferings, before it vanishes from the face of the earth. It terms of human existence, the tropical rain forests represent a store of renewable natural resources, which have for eons, by virtue of their richness in both animal and plant species, contributed a myriad of items for the survival and well-being of man. These include basic food supplies, clothing, shelter, fuel, spices, industrial raw materials, and medicine. It is to this last item, medicinal or ethical drugs, that this essay is addressed.
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A dichapetalin-type triterpenoid and a dibenzylbutyrolactone-type lignan, together with five known lignans, a known aromatic diterpenoid, and a known acylated phytosterol, were isolated from the aerial parts of Phyllanthus songboiensis,... more
A dichapetalin-type triterpenoid and a dibenzylbutyrolactone-type lignan, together with five known lignans, a known aromatic diterpenoid, and a known acylated phytosterol, were isolated from the aerial parts of Phyllanthus songboiensis, collected in Vietnam. Their structures were determined by interpretation of the spectroscopic data, and the inhibitory activity toward HT-29 human colon cancer cells of all isolates was evaluated by a cytotoxicity assay. The known arylnaphthalene lignan, (+)-acutissimalignan A, was highly cytotoxic toward HT-29 cells, with an IC50 value of 19 nM, but this compound was inactive as a DNA topoisomerase IIα (topo IIα) poison. The known phytosterol, (-)-β-sitosterol-3-O-β-d-(6-O-palmitoyl)glucopyranoside, was found to stimulate natural killer (NK) cells at a concentration of 10μM in the presence of interleukin 12 (IL-12).
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The leaves of Stevia rebaudiana (Bertoni) Bertoni (Asteraceae)(henceforth referred to as stevia), a South American plant, have been known for over a century in the border regions of Paraguay and Brazil for their sweet taste, but their... more
The leaves of Stevia rebaudiana (Bertoni) Bertoni (Asteraceae)(henceforth referred to as stevia), a South American plant, have been known for over a century in the border regions of Paraguay and Brazil for their sweet taste, but their specific use as a sweetener in ...
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Two new (1 and 2) and four known arylnaphthalene lignan lactones (3-6) were isolated from different plant parts of Phyllanthus poilanei collected in Vietnam, with two further known analogues (7 and 8) being prepared from phyllanthusmin C... more
Two new (1 and 2) and four known arylnaphthalene lignan lactones (3-6) were isolated from different plant parts of Phyllanthus poilanei collected in Vietnam, with two further known analogues (7 and 8) being prepared from phyllanthusmin C (4). The structures of the new compounds were determined by interpretation of their spectroscopic data and by chemical methods, and the structure of phyllanthusmin D (1) was confirmed by single-crystal X-ray diffraction analysis. Several of these arylnaphthalene lignan lactones were cytotoxic toward HT-29 human colon cancer cells, with compounds 1 and 7-O-[(2,3,4-tri-O-acetyl)-α-L-arabinopyranosyl)]diphyllin (7) found to be the most potent, exhibiting IC50 values of 170 and 110 nM, respectively. Compound 1 showed activity when tested in an in vivo hollow fiber assay using HT-29 cells implanted in immunodeficient NCr nu/nu mice. Mechanistic studies showed that this compound mediated its cytotoxic effects by inducing tumor cell apoptosis through activation of caspase-3, but it did not inhibit DNA topoisomerase IIα activity.
Research Interests: Chemistry, Natural Products, Complementary and Alternative Medicine, Plant Biology, Biology, and 15 moreVietnam, Medicine, Biological Sciences, Humans, Mice, Animals, Lignans, Caspase, CHEMICAL SCIENCES, Phyllanthus, Lactones, Glycosides, Molecular Structure, Medical and Health Sciences, and Pharmacology and pharmaceutical sciences
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Bioassay-guided fractionation was conducted on a CHCl3-soluble extract of the stem bark of Alstonia angustifolia (Apocynaceae) collected in Vietnam using the HT-29 human colon cancer cell line, and led to the isolation of a new... more
Bioassay-guided fractionation was conducted on a CHCl3-soluble extract of the stem bark of Alstonia angustifolia (Apocynaceae) collected in Vietnam using the HT-29 human colon cancer cell line, and led to the isolation of a new sarpagine-type indole alkaloid (1), together with nine known alkaloids, including four macroline-derived alkaloids (2-5), a sarpagine-type alkaloid (6), and four macroline-pleiocarpamine bisindole alkaloids (7-10). The structure of the new compound (1) was determined on the basis of spectroscopic data interpretation. Compounds 1-10 were evaluated in vitro for their NF-κB (p65) inhibitory activity against the Hela cells in an ELISA assay. The new sarpagine alkaloid, N(4)-methyltalpinine (1), was found to show significant NF-κB inhibitory activity (ED50 = 1.2 µM). Furthermore, all the isolates (1-10) were evaluated in vitro for their antileishmanial activity, and compounds (1-4, 6 and 8-10) exhibited leishmaniacidal activity against promastigotes of Leishmania mexicana.
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ABSTRACT ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select... more
ABSTRACT ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
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Global Importance of Medicinal Plants Norman R. Farnsworth and Djaja D. Soejarto Program for Collaborative Research in the Pharmaceutical Sciences, College of Pharmacy, University of Illinois at Chicago, Chicago, Illinois, USA.... more
Global Importance of Medicinal Plants Norman R. Farnsworth and Djaja D. Soejarto Program for Collaborative Research in the Pharmaceutical Sciences, College of Pharmacy, University of Illinois at Chicago, Chicago, Illinois, USA. Introduction Ancient Man is known to have ...