Djaja Soejarto | University of Illinois at Chicago (original) (raw)
Papers by Djaja Soejarto
The ICBG (International Cooperative Biodiversity Groups) program, through which institutions loca... more The ICBG (International Cooperative Biodiversity Groups) program, through which institutions located in biotechnology-rich countries in the North collaborate with institutions located in the biodiversity-rich countries in the South (with the support of an industrial partner) to discover and develop natural-product drugs, is an experiment in the design of bioprospecting efforts. This chapter describes the general aims and organization of the ICBGs and describes in great detail the agreements that governed the University of Illinois at Chicago-Vietnam-Laos ICBG. The chapter includes material concerning IP (intellectual property) rights issues, informed consent, various forms of benefit sharing (including the sharing of short-and long-term, namely, royalty, benefits), capacity building, and community reciprocity. It offers a model for other such agreements.
SpringerBriefs in Plant Science, 2014
I. Previous studies indicate that tonically active neurons (TANS) are the cholinergic interneuron... more I. Previous studies indicate that tonically active neurons (TANS) are the cholinergic interneurons of the striatum and predict that their activity is synchronized. To test whether TANS do fire synchronously, and whether dopamine depletion affects their syn-chronization, we recorded the simultaneous activity of several TANS in the putamens of two vervet monkeys before and after l-methyl-4-phenyl- 1,2,3,6-tetrahydropyridine (MPTP) treatment. 2. Cross-correlation analysis revealed that most pairs of TANS (33 of 54; 61.1%) fire synchronously at-+60-ms delay. Correlated activity was more common between neurons with characteristic response to reward ( 17 of 19 pairs; 89.5%). 3. Cross-correlation study of 24 triplets of TANS showed syn-chronization of spiking activity of all 3 TANS in only 29.2 % of cases (7 of 24 triplets). Correlated activity of two of three possible pairs was found in 25 % of the cases. 4. After MPTP treatment and the development of parkinsonian symptoms, most TANS ’ au...
Pharmaceutical Biology, 2011
ContextWhether natural product drug discovery programs should rely on wild plants collected “rand... 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.
Journal of Natural Products, 2002
Phytochemistry, 2001
The pregnane steroid, (E)-aglawone, along with four known triterpenes, and a known sterol mixture... 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.
Botanical Museum leaflets, Harvard University
Progress in the Chemistry of Organic Natural Products, 2018
Many of the clinically used anticancer agents in Western medicine are derived from secondary meta... 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.
Phytochemistry Letters
Herbarium voucher specimens are used primarily for taxonomic confirmation. However, they also aff... 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.
Journal of medicinal plant research, 2017
The Vietnam-Laos International Cooperative Biodiversity Group (ICBG) based at the University of I... 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...
Molecules (Basel, Switzerland), Jan 31, 2016
The International Cooperative Biodiversity Groups (ICBG) Program based at the University of Illin... 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. ...
Journal of natural products, Jun 14, 2017
Justicia gendarussa, a medicinal plant collected in Vietnam, was identified as a potent anti-HIV-... 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...
Journal of natural products, Jan 16, 2016
Three new (1-3) and two known (4 and 5) cytotoxic cardiac glycosides were isolated and characteri... 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.
Phytochemistry, Jan 19, 2017
In a search for new anti-HIV active leads from over several thousands of plant extracts, we have ... 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...
Journal of Medicinal Plants Research, Nov 17, 2014
The Lao People's Democratic Republic (Lao PDR) or Laos has a long history in the use of medicinal... more The Lao People's Democratic Republic (Lao PDR) or Laos has a long history in the use of medicinal plants, as well as in the use of traditional medicines. The Government of Laos also supports the use of medicinal plants and traditional medicines in the prevention and treatment of diseases. As a government institution, the Institute of Traditional Medicine (ITM) has carried out surveys and inventories of medicinal plants as part of its mission since the beginning of its establishment in 1976, both by the staff of this institution, as well as in collaboration with national and international partners. The number of plant collections that have been made to date as a result of these activities, and those that have been deposited at the herbarium of ITM, reaches more than 14,000. Of these, 7,201 (51%) collections represent medicinal plant species, corresponding to an estimated number of between 2,000 and 3,000 species of Lao medicinal plants. A sizeable portion of this medicinal plant collection has been computerized in a database system called Natural Products Information System (NAPIS). Based on a number of criteria, some medicinal plant species are considered rare and endangered. Therefore, the Lao government issued the Prime Minister Decree No. 155 in 2003 and set guidelines for the cultivation of medicinal plants for domestic consumption and for exportation. The government also supports the initiative in the establishment of Medicinal Plant Preserves (MPPs) and Medicinal Biodiversity Preserves (MBPs), which today form a network of 10 such preserves throughout Laos.
Planta medica, Jan 9, 2016
Three new rotenoids (1-3), two new isoflavonoids (4 and 5), and six known analogues (6-11) were i... 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...
Advances in Natural Sciences, Feb 20, 2008
Seven (7) species of Araceae representing new records for the flora of Cuc Phuong National Park a... 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)
The American journal of Chinese medicine, 2016
Litsea verticillata Hance (Lauraceae), a Chinese medicine used to treat swelling caused by injury... 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...
The ICBG (International Cooperative Biodiversity Groups) program, through which institutions loca... more The ICBG (International Cooperative Biodiversity Groups) program, through which institutions located in biotechnology-rich countries in the North collaborate with institutions located in the biodiversity-rich countries in the South (with the support of an industrial partner) to discover and develop natural-product drugs, is an experiment in the design of bioprospecting efforts. This chapter describes the general aims and organization of the ICBGs and describes in great detail the agreements that governed the University of Illinois at Chicago-Vietnam-Laos ICBG. The chapter includes material concerning IP (intellectual property) rights issues, informed consent, various forms of benefit sharing (including the sharing of short-and long-term, namely, royalty, benefits), capacity building, and community reciprocity. It offers a model for other such agreements.
SpringerBriefs in Plant Science, 2014
I. Previous studies indicate that tonically active neurons (TANS) are the cholinergic interneuron... more I. Previous studies indicate that tonically active neurons (TANS) are the cholinergic interneurons of the striatum and predict that their activity is synchronized. To test whether TANS do fire synchronously, and whether dopamine depletion affects their syn-chronization, we recorded the simultaneous activity of several TANS in the putamens of two vervet monkeys before and after l-methyl-4-phenyl- 1,2,3,6-tetrahydropyridine (MPTP) treatment. 2. Cross-correlation analysis revealed that most pairs of TANS (33 of 54; 61.1%) fire synchronously at-+60-ms delay. Correlated activity was more common between neurons with characteristic response to reward ( 17 of 19 pairs; 89.5%). 3. Cross-correlation study of 24 triplets of TANS showed syn-chronization of spiking activity of all 3 TANS in only 29.2 % of cases (7 of 24 triplets). Correlated activity of two of three possible pairs was found in 25 % of the cases. 4. After MPTP treatment and the development of parkinsonian symptoms, most TANS ’ au...
Pharmaceutical Biology, 2011
ContextWhether natural product drug discovery programs should rely on wild plants collected “rand... 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.
Journal of Natural Products, 2002
Phytochemistry, 2001
The pregnane steroid, (E)-aglawone, along with four known triterpenes, and a known sterol mixture... 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.
Botanical Museum leaflets, Harvard University
Progress in the Chemistry of Organic Natural Products, 2018
Many of the clinically used anticancer agents in Western medicine are derived from secondary meta... 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.
Phytochemistry Letters
Herbarium voucher specimens are used primarily for taxonomic confirmation. However, they also aff... 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.
Journal of medicinal plant research, 2017
The Vietnam-Laos International Cooperative Biodiversity Group (ICBG) based at the University of I... 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...
Molecules (Basel, Switzerland), Jan 31, 2016
The International Cooperative Biodiversity Groups (ICBG) Program based at the University of Illin... 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. ...
Journal of natural products, Jun 14, 2017
Justicia gendarussa, a medicinal plant collected in Vietnam, was identified as a potent anti-HIV-... 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...
Journal of natural products, Jan 16, 2016
Three new (1-3) and two known (4 and 5) cytotoxic cardiac glycosides were isolated and characteri... 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.
Phytochemistry, Jan 19, 2017
In a search for new anti-HIV active leads from over several thousands of plant extracts, we have ... 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...
Journal of Medicinal Plants Research, Nov 17, 2014
The Lao People's Democratic Republic (Lao PDR) or Laos has a long history in the use of medicinal... more The Lao People's Democratic Republic (Lao PDR) or Laos has a long history in the use of medicinal plants, as well as in the use of traditional medicines. The Government of Laos also supports the use of medicinal plants and traditional medicines in the prevention and treatment of diseases. As a government institution, the Institute of Traditional Medicine (ITM) has carried out surveys and inventories of medicinal plants as part of its mission since the beginning of its establishment in 1976, both by the staff of this institution, as well as in collaboration with national and international partners. The number of plant collections that have been made to date as a result of these activities, and those that have been deposited at the herbarium of ITM, reaches more than 14,000. Of these, 7,201 (51%) collections represent medicinal plant species, corresponding to an estimated number of between 2,000 and 3,000 species of Lao medicinal plants. A sizeable portion of this medicinal plant collection has been computerized in a database system called Natural Products Information System (NAPIS). Based on a number of criteria, some medicinal plant species are considered rare and endangered. Therefore, the Lao government issued the Prime Minister Decree No. 155 in 2003 and set guidelines for the cultivation of medicinal plants for domestic consumption and for exportation. The government also supports the initiative in the establishment of Medicinal Plant Preserves (MPPs) and Medicinal Biodiversity Preserves (MBPs), which today form a network of 10 such preserves throughout Laos.
Planta medica, Jan 9, 2016
Three new rotenoids (1-3), two new isoflavonoids (4 and 5), and six known analogues (6-11) were i... 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...
Advances in Natural Sciences, Feb 20, 2008
Seven (7) species of Araceae representing new records for the flora of Cuc Phuong National Park a... 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)
The American journal of Chinese medicine, 2016
Litsea verticillata Hance (Lauraceae), a Chinese medicine used to treat swelling caused by injury... 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...