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1.
Molecules ; 23(6)2018 Jun 12.
Article in English | MEDLINE | ID: mdl-29895732

ABSTRACT

We previously reported on the isolation and biological activities of plagiochiline A (1), a 2,3-secoaromadendrane-type sesquiterpenoid from the Peruvian medicinal plant, Plagiochila disticha. This compound was found to have antiproliferative effects on a variety of solid tumor cell lines, as well as several leukemia cell lines. Other researchers have also noted the cytotoxicity of plagiochiline A (isolated from different plant species), but there are no prior reports regarding the mechanism for this bioactivity. Here, we have evaluated the effects of plagiochiline A on cell cycle progression in DU145 prostate cancer cells. A cell cycle analysis indicated that plagiochiline A caused a significant increase in the percentage of cells in the G2/M phase when compared with control cells. When cells were stained and observed by fluorescence microscopy to examine progress through the mitotic phase, we found a significant increase in the proportion of cells with features of late cytokinesis (cells connected by intercellular bridges) in the plagiochiline A-treated samples. These results suggest that plagiochiline A inhibits cell division by preventing completion of cytokinesis, particularly at the final abscission stage. We also determined that plagiochiline A reduces DU145 cell survival in clonogenic assays and that it induces substantial cell death in these cells.


Subject(s)
Cytokinesis/drug effects , Embryophyta/chemistry , Epoxy Compounds/pharmacology , Prostatic Neoplasms/drug therapy , Pyrans/pharmacology , Cell Line, Tumor , Cell Proliferation/drug effects , Cell Survival/drug effects , Epoxy Compounds/chemistry , Epoxy Compounds/isolation & purification , Humans , Male , Plant Extracts/chemistry , Pyrans/chemistry , Pyrans/isolation & purification
2.
Anticancer Res ; 36(4): 1621-30, 2016 Apr.
Article in English | MEDLINE | ID: mdl-27069139

ABSTRACT

A series of (imidazo[1,2-a]pyrazin-6-yl)ureas were synthesized through 6-aminoimidazo[1,2-a]pyrazine as a key intermediate. 1-(Imidazo[1,2-a]pyrazin-6-yl)-3-(4-methoxy - phenyl)urea displayed a cytostatic activity against a non-small cell lung cancer cell line and was chosen for further mechanistic studies. Growth kinetics highlighted a selective dose-dependent response of P53-mutant NSCLC-N6-L16 cell line and overexpression of TP53 gene induced by this compound. These pharmacological data suggest a promising reactivation of p53 mutant in NSCLC-N6-L16 cell line.


Subject(s)
Antineoplastic Agents/pharmacology , Imidazoles/pharmacology , Pyrazines/pharmacology , Urea/analogs & derivatives , Urea/pharmacology , Animals , BALB 3T3 Cells , Carcinoma, Non-Small-Cell Lung/drug therapy , Carcinoma, Non-Small-Cell Lung/genetics , Cell Line, Tumor , Cell Proliferation/drug effects , Humans , Lung Neoplasms/drug therapy , Lung Neoplasms/genetics , Mice , Tumor Suppressor Protein p53/genetics
3.
Eur J Med Chem ; 103: 381-95, 2015 Oct 20.
Article in English | MEDLINE | ID: mdl-26383125

ABSTRACT

A series of original 2-phenyl-3-(pyridin-4-yl)imidazo[1,2-a]pyrazines and the 3-iodo precursors, bearing a polar moiety at the C-8 position, was synthesized and evaluated for their antileishmanial activities. Two derivatives exhibited very good activity against the promastigote and the amastigote forms of Leishmania major in the micromolar to submicromolar ranges, coupled with a low cytotoxicity against macrophages and 3T3 mouse fibroblast cells. Through LmCK1 inhibition assay, investigations of the putative molecular target of these promising antileishmanial compounds will be discussed.


Subject(s)
Antiprotozoal Agents/pharmacology , Fibroblasts/drug effects , Imidazoles/pharmacology , Leishmania major/drug effects , Macrophages/drug effects , Pyrazines/pharmacology , Animals , Antiprotozoal Agents/chemical synthesis , Antiprotozoal Agents/chemistry , Cell Line , Cell Proliferation/drug effects , Dose-Response Relationship, Drug , Humans , Imidazoles/chemical synthesis , Imidazoles/chemistry , Mice , Mice, Inbred BALB C , Molecular Structure , Pyrazines/chemical synthesis , Pyrazines/chemistry , Structure-Activity Relationship
4.
J Nat Prod ; 76(1): 2-7, 2013 Jan 25.
Article in English | MEDLINE | ID: mdl-23270478

ABSTRACT

Recently, our group reported the discovery of three new withanolides, physangulidines A-C, from Physalis angulata. In this study, the biological effects of physangulidine A (1), which was the most active and abundant of the three new constituents, are described. It was found that 1 significantly reduces survival in clonogenic assays for two hormone-independent prostate cancer cell lines. Flow cytometry and confocal microscopy studies in DU145 human prostate cancer cells indicated that 1 induces cell cycle arrest in the G(2)/M phase and causes defective mitosis. It was determined also that 1 produces programed cell death by apoptosis, as evidenced by biochemical markers and distinct changes in cell morphology. These results imply that the antimitotic and proapoptotic effects of 1 may contribute significantly to the biological activities and potential medicinal properties of its plant of origin.


Subject(s)
Antineoplastic Agents/isolation & purification , Antineoplastic Agents/pharmacology , Physalis/chemistry , Withanolides/isolation & purification , Withanolides/pharmacology , Antineoplastic Agents/chemistry , Apoptosis/drug effects , Cell Cycle/drug effects , Cell Division/drug effects , Drug Screening Assays, Antitumor , G2 Phase/drug effects , Humans , Male , Microscopy, Confocal , Molecular Structure , Prostatic Neoplasms/drug therapy , Withanolides/chemistry
5.
Org Lett ; 14(5): 1230-3, 2012 Mar 02.
Article in English | MEDLINE | ID: mdl-22329497

ABSTRACT

Bioassay-directed fractionation of the whole plant of Physalis angulata L. afforded three new antiproliferative withanolides with an unusual carbon framework: physangulidines A (1), B (2), and C (3). Structures of the three isomeric withanolides were determined by a combination of HRMS, NMR spectroscopic, and X-ray crystallographic methods. Each has shown significant antiproliferative activity against DU145 prostate cancer cells. Physangulidine A (1) was further tested against a wide range of additional cancer cell lines and found to exhibit significant antiproliferative activity.


Subject(s)
Antineoplastic Agents, Phytogenic/chemistry , Magnoliopsida/chemistry , Withanolides/chemistry , Animals , Antineoplastic Agents, Phytogenic/isolation & purification , Antineoplastic Agents, Phytogenic/pharmacology , Cell Line , Cell Proliferation/drug effects , Humans , Mice , Models, Molecular , Molecular Conformation , Withanolides/isolation & purification , Withanolides/pharmacology
6.
Planta Med ; 77(14): 1597-9, 2011 Sep.
Article in English | MEDLINE | ID: mdl-21472652

ABSTRACT

An anticancer-bioassay guided isolation of the ethanol extract and fractions of two plants from the Peruvian rainforest, Mikania decora and Cremastosperma microcarpum, led to the characterization of one abundant diterpene, ent-pimara-8(14),15-dien-19-oic acid (1), three thymol derivatives, 10-acetoxy-8,9-dehydro-6-methoxythymol butyrate (2), 10-acetoxy-8,9-epoxy-6-methoxythymol isobutyrate (3), and acetylschizoginol (4), as well as one neolignan, (±)-trans-dehydrodiisoeugenol (5). Only the latter was isolated from C. microcarpum. These compounds exhibited significant cytotoxic activity against a panel of human tumor cell lines. Compounds 3 and 4 were also investigated for their in vitro antileishmanial and trypanocidal activity against Leishmania amazonensis axenic amastigotes and Trypanosoma cruzi trypomastigotes.


Subject(s)
Annonaceae/chemistry , Anti-Infective Agents/pharmacology , Mikania/chemistry , Plant Extracts/chemistry , Animals , Anti-Infective Agents/chemistry , Cell Line, Tumor , Cell Survival , Diterpenes/chemistry , Diterpenes/pharmacology , Female , Humans , Leishmania/drug effects , Lignans/chemistry , Lignans/pharmacology , Macrophages/drug effects , Male , Mice , Parasitic Sensitivity Tests , Peru , Plant Leaves/chemistry , Plant Roots/chemistry , Plant Stems/chemistry , Thymol/chemistry , Thymol/pharmacology , Trees , Trypanosoma cruzi/drug effects
7.
Chem Biodivers ; 7(4): 922-32, 2010 Apr.
Article in English | MEDLINE | ID: mdl-20397225

ABSTRACT

The antimycobacterial activities of eight diterpenes, 1-8, isolated previously from Plectranthus and eleven esters, 9-19, of 7alpha-acetoxy-6beta,12-dihydroxyabieta-8,12-diene-11,14-dione (5) were evaluated against the MTB strains H(37)Rv and MDR. Only diterpenoids with a quinone framework revealed anti-MTB activity. Abietane 5 and its 6,12-dibenzoyl, 12-methoxybenzoyl, 12-chlorobenzoyl, and 12-nitrobenzoyl esters, 9, 11, 12, and 13, respectively, showed potent activities against the MDR strain with MIC values between 3.12 and 0.39 microg/ml. Cytotoxic activities towards 3T3 and Vero cells were also evaluated. Compound 11, with the best selectivity index, may be a suitable lead for further chemical modifications. The complete structural elucidation of the new esters, 9-14, 16, 18, and 19, as well as the NMR data of known derivatives 15 and 17 are reported.


Subject(s)
Abietanes/chemistry , Anti-Bacterial Agents/chemistry , Mycobacterium tuberculosis/drug effects , Plectranthus/metabolism , 3T3 Cells , Abietanes/isolation & purification , Abietanes/toxicity , Animals , Anti-Bacterial Agents/isolation & purification , Anti-Bacterial Agents/toxicity , Chlorocebus aethiops , Drug Resistance, Multiple, Bacterial/drug effects , Mice , Microbial Sensitivity Tests , Plectranthus/chemistry , Vero Cells
8.
Bioorg Med Chem ; 18(8): 2880-6, 2010 Apr 15.
Article in English | MEDLINE | ID: mdl-20356752

ABSTRACT

The synthesis of 2-(5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-4-yl)hydrazone-derivatives (BTPs) and their in vitro evaluation against Trypanosoma cruzi trypomastigotes, Mycobacterium tuberculosis, Leishmania amazonensis axenic amastigotes, and six human cancer cell lines is described. The in vivo activity of the most active and least toxic compounds against T. cruzi and L. amazonensis was also studied. BTPs constitute a new family of drug leads with potential activity against infectious diseases. Due to their drug-like properties, this series of compounds can potentially serve as templates for future drug-optimization and drug-development efforts for use as therapeutic agents in developing countries.


Subject(s)
Antitubercular Agents/chemistry , Pyrimidines/chemistry , Antiprotozoal Agents/chemical synthesis , Antiprotozoal Agents/chemistry , Antiprotozoal Agents/toxicity , Antitubercular Agents/chemical synthesis , Antitubercular Agents/toxicity , Cell Line, Tumor , Humans , Mycobacterium tuberculosis/drug effects , Parasitic Sensitivity Tests , Pyrimidines/toxicity , Trypanosoma cruzi/drug effects
9.
Planta Med ; 76(7): 705-7, 2010 May.
Article in English | MEDLINE | ID: mdl-19960415

ABSTRACT

A pharmacological screening of the ethanol extract and fractions of two Peruvian medicinal plants, Plagiochila disticha and Ambrosia peruviana, led to the isolation and characterization of three ENT-2,3-secoaromadendrane-type sesquiterpenoids, named plagiochiline A ( 1), I ( 2), and R ( 3), as well as of two pseudoguaianolids, damsin ( 4) and confertin ( 5), which exhibited significant cytotoxic activity against a panel of human tumor cell lines. Compounds 1, 4, and 5 were also investigated for their in vitro antileishmanial, trypanocidal, and antituberculosis activity against Leishmania amazonensis axenic amastigotes and Trypanosoma cruzi trypomastigotes, as well as against MDR and sensitive strains of Mycobacterium tuberculosis, respectively.


Subject(s)
Anti-Infective Agents/isolation & purification , Antineoplastic Agents, Phytogenic/isolation & purification , Asteraceae/chemistry , Azulenes/isolation & purification , Epoxy Compounds/isolation & purification , Pyrans/isolation & purification , Sesquiterpenes/isolation & purification , Cell Line, Tumor , Drug Evaluation, Preclinical , Humans , Peru , Plants, Medicinal/chemistry
10.
J Nat Prod ; 72(3): 524-6, 2009 Mar 27.
Article in English | MEDLINE | ID: mdl-19199646

ABSTRACT

A multidisciplinary and international team of scientists was assembled in the early 1990s to conduct an ethnobotanical study of plants used by the Aguaruna people of the Peruvian Amazon forest. The initial ethnobotanical project, carried out under the auspices of an International Cooperative Biodiversity Grant (ICBG), led to the collection of approximately 4000 plant species. Some members of the original team of scientists have continued this collaboration by focusing on potential sources of new anticancer, anti-infective, and wound-healing agents. This effort has uncovered several secondary metabolites representing a wide variety of chemical diversity. In this short review we describe some bioactive compounds of interest as part of our continuing collaboration.


Subject(s)
Plants, Medicinal/chemistry , Ethnobotany , Humans , Medicine, Traditional , Molecular Structure , Peru
11.
Rev. peru. med. exp. salud publica ; 25(4): 380-385, oct.-dic. 2008. tab, graf
Article in Spanish | LILACS, LIPECS | ID: lil-563979

ABSTRACT

Objetivos. Evaluar la actividad citotóxica de extractos etanólicos de raíces, tallos, hojas y flores de Gnaphalium spicatum sobre algunas líneas celulares tumorales humanas. Materiales y métodos. Las líneas celulares HT-29, H-460, MCF-7, M-14, PC-3, DU-145, K-562, y 3T3, fueron expuestas a cuatro concentraciones de extractos etanólicos de raíces, tallos, hojas y flores de Gnaphalim spicatum, asimismo, a diferentes concentraciones de cisplatino, que se usó como control positivo. Se halló los porcentajes de crecimiento en 48 horas. Luego se determinó la concentración inhibitoria 50 (CI50) mediante análisis de regresión lineal, el índice de selectividad de cada muestra y finalmente, la relación dosis-respuesta entre las concentraciones de los extractos y cisplatino, con los porcentajes de crecimiento. Resultados. El extracto etanólico de las raíces de Gnaphalium spicatum mostró mayor actividad citotóxica en la líneas celulares MCF-7 yK-562. Los CI50 en ¦Ìg/mL fueron de 98 (r= -0,98 p menor que 0,01) y 46 (r= -0,97 p menor que 0,01), respectivamente. Asimismo, su citotoxicidad en la l¨ªnea celular 3T3 fue de 215 (r= 0,97 p menor que 0,01). Los CI50 del cisplatino en ¦Ìg/mL fueron de 2 (r=-0,96 p menor que 0,01), 7,7 (r=-0,98 p menor que 0,01) y 3 (r=-0,97p menor que 0,01), para MCF-7, K-562 y 3T3, respectivamente. Los índices de selectividad del extracto de raíces y cisplatino fueron 2,2 y 0,3 para MCF-7, y 4,7 y 1,5 para K-562, respectivamente. Los extractos de tallos, hojas y flores obtuvieron CI50 mayor que a 0,250 mg/mL en todas la líneas celulares evaluadas. Conclusiones. Los extractos etanólicos de tallos, hojas y flores de Gnaphalium spicatum no mostraron actividadcitotóxica en este bioensayo. Los extractos de raíces mostraron citotoxicidad en las todas las líneas celulares tumorales, excepto en M-14. Además fueron menos citotóxicos en relación al cisplatino en la línea celular 3T3.


Objectives. To evaluate the cytotoxic activity ethanolic extracts of roots, stems, leaves and flowers of Gnaphalium spicatum in somehuman tumor cell lines. Material and methods. The following cell lines: HT-29, H-460, MCF-7, M-14, PC-3, DU-145, K-562, and 3T3, were exposed to four different concentrations of ethanolic extracts from roots, stems, leaves and flowers of Gnaphalium spicatum, and also to different concentrations of cisplatin, which was used as a positive control. Percentage growth was assessed after 48 hours. The minimalinhibitory concentration for 50 per cent of the cells (IC50) was determined using linear regression analysis; also, the selectivity index for each sample and the dose-response relationship between the extract concentrations and cisplatin, as well as growth percentages were determined. Results. The ethanolic extract of Gnaphalium spicatum roots showed its highest cytotoxic activity in MCF-7 and K-562 cell lines. IC50 values, expressed in ¦Ìg/mL, were 98 (r=-0.98; p <0.01) and 46 (r= -0.97; p minor that 0.01), respectively. Cytotoxicity against the 3T3 cellline was 215 (r= 0.97; p minor that 0.01). IC50 values for cisplatin were 2 (r= -0.96 p minor that 0.01), 7.7 (r= -0.98; p minor that 0.01), and 3 (r= -0.97; p minor that 0.01), for theMCF7, K562 and 3T3 cell lines, respectively. The selectivity index of the ethanolic extract from Gnaphalium spicatum roots and cisplatinwere 2.2 and 0.03 for the MCF-7 cell line, and 4,7 and 1.5 for the K-562 cell line, respectively. Extracts from stems, leaves and flowers of Gnapahlium spicatum acheived IC50 levels major that 0.250 mg/mL in every cell lines tested. Conclusions. The ethanolic extracts of stems, leaves and flowers of Gnaphalium spicatum did not show cytotoxic activity in this bioassay. The extract from roots showed cytotoxicity in all tumor cell lines, except in M-14. Furthermore, it was less cytotoxic than cisplatin in 3T3 cell line.


Subject(s)
Humans , Antineoplastic Agents , Phytotherapy , In Vitro Techniques , Plants, Medicinal , Cell Culture Techniques
12.
J Med Chem ; 51(19): 6230-4, 2008 Oct 09.
Article in English | MEDLINE | ID: mdl-18798609

ABSTRACT

Synthesis of a cytotoxic dihydrochalcone, first isolated from a traditional Amazonian medicinal plant Iryanthera juruensis Warb (Myristicaceae), followed by a comprehensive SAR analysis of saturated and unsaturated chalcone synthetic intermediates, led to the identification of analogues with selective and significant in vitro anti- Trypanosoma cruzi activity. Further SAR studies were undertaken with the synthesis of 21 new chalcones containing two allyloxy moieties that resulted in the discovery of 2',4'-diallyloxy-6'-methoxy chalcones with improved selectivity against this parasite at concentrations below 25 microM, four of which exhibited a selectivity index greater than 12.


Subject(s)
Antiprotozoal Agents/chemical synthesis , Antiprotozoal Agents/pharmacology , Chalcones/chemical synthesis , Chalcones/pharmacology , Trypanosoma cruzi/drug effects , 3T3 Cells , Animals , Antiprotozoal Agents/chemistry , Cell Line, Tumor , Cell Proliferation/drug effects , Chalcones/chemistry , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Fibroblasts/drug effects , Humans , Mice , Mice, Inbred BALB C , Molecular Structure , Myristicaceae/chemistry , Parasitic Sensitivity Tests , Plant Extracts/chemical synthesis , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plants, Medicinal/chemistry , Stereoisomerism , Structure-Activity Relationship
13.
Planta Med ; 74(4): 407-10, 2008 Mar.
Article in English | MEDLINE | ID: mdl-18484532

ABSTRACT

A pharmacological screening of the ethanol extract and fractions of Blepharodon nitidum led to the isolation of fourteen compounds, two of which, 24-hydroperoxycycloart-25-en-3beta-ol and 25-hydroperoxycycloart-23-en-3beta-ol, exhibited in vitro anti- Mycobacterium tuberculosis and antileishmanial activities, as well as significant cytotoxic activity against a panel of human tumor cell lines.


Subject(s)
Anti-Infective Agents/chemistry , Anti-Infective Agents/pharmacology , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/pharmacology , Apocynaceae/chemistry , Cell Line, Tumor , Humans , Molecular Structure
14.
J Nat Prod ; 71(1): 102-5, 2008 Jan.
Article in English | MEDLINE | ID: mdl-18163590

ABSTRACT

The antiproliferative bioassay-guided fractionation of five Peruvian plants, Doliocarpus dentatus, Picramnia sellowii, Strychnos mitscherlichii, Iryanthera juruensis, and Croton alnifolius, led to the isolation and identification of their different major cytotoxic constituents, betulinic acid (1), nataloe-emodin (2), bisnordihydrotoxyferine (4), 2',4'-dihydroxy-6'-methoxy-3,4-methylenedioxydihydrochalcone (5), and 2',4'-dihydroxy-4,6'-dimethoxydihydrochalcone (6) and 12-O-tetradecanoylphorbol-13-acetate (7), respectively. Eight human tumor cell lines and two nontumorigenic cell lines were used in this investigation. Their in vitro activity against Mycobacterium tuberculosis is also reported.


Subject(s)
Antineoplastic Agents, Phytogenic/isolation & purification , Antineoplastic Agents, Phytogenic/pharmacology , Mycobacterium tuberculosis/drug effects , Plants, Medicinal/chemistry , Strychnos/chemistry , Triterpenes/isolation & purification , Triterpenes/pharmacology , Antineoplastic Agents, Phytogenic/chemistry , Drug Screening Assays, Antitumor , Humans , Microbial Sensitivity Tests , Molecular Structure , Pentacyclic Triterpenes , Peru , Triterpenes/chemistry , Tumor Cells, Cultured , Betulinic Acid
15.
J Nat Prod ; 69(6): 978-9, 2006 Jun.
Article in English | MEDLINE | ID: mdl-16792424

ABSTRACT

Anredera diffusa is used as a wound-healing agent in traditional Peruvian medicine. Acid hydrolysis of the bioactive ethanolic extract, followed by in vivo activity-guided fractionation, yielded oleanolic acid, with a wound-healing activity equivalent to 42.9% (p < 0.01) above the control. The highest cicatrizant activity in mice was obtained by applying 40 microg of oleanolic acid per gram of body weight.


Subject(s)
Caryophyllaceae/chemistry , Oleanolic Acid , Plants, Medicinal/chemistry , Wound Healing/drug effects , Animals , Medicine, Traditional , Mice , Molecular Structure , Oleanolic Acid/analogs & derivatives , Oleanolic Acid/chemistry , Oleanolic Acid/isolation & purification , Oleanolic Acid/pharmacology , Peru
16.
J Nat Prod ; 69(5): 845-6, 2006 May.
Article in English | MEDLINE | ID: mdl-16724857

ABSTRACT

An ethanol extract of the Peruvian plant Clavija procera, a member of the rare Theophrastaceae family, was fractionated using a colorimetric bioassay-guided protocol against Mycobacterium tuberculosis (MTB), yielding the oleanane triterpenoid aegicerin (1) as the active constituent. Its MIC values ranged between 1.6 and 3.12 microg/mL against 37 different sensitive and resistant MTB strains (1 H37Rv, 21 susceptible clinical isolates, 2 INH-resistant clinical isolates, and 13 MDR clinical isolates).


Subject(s)
Antitubercular Agents , Mycobacterium tuberculosis/drug effects , Oleanolic Acid/analogs & derivatives , Plants, Medicinal/chemistry , Triterpenes , Animals , Antitubercular Agents/chemistry , Antitubercular Agents/isolation & purification , Antitubercular Agents/pharmacology , Chlorocebus aethiops , Drug Resistance, Multiple, Bacterial , Microbial Sensitivity Tests , Oleanolic Acid/chemistry , Oleanolic Acid/isolation & purification , Oleanolic Acid/pharmacology , Triterpenes/chemistry , Triterpenes/isolation & purification , Triterpenes/pharmacology , Vero Cells
17.
Phytochemistry ; 66(1): 5-29, 2005 Jan.
Article in English | MEDLINE | ID: mdl-15649507

ABSTRACT

The Uncaria genus is an important source of medicinal natural products, particularly alkaloids and triterpenes. The collected information is an attempt to cover the more recent developments in the ethnobotany, pharmacology and phytochemistry of this genus. During the past 20 years, alkaloids, terpenes, quinovic acid glycosides, flavonoids and coumarins have been isolated from Uncaria. Fifty-three novel structures are reported in this review. The species in which the largest number of compounds has been identified is the Peruvian Uncaria tomentosa or 'cat's claw.' Pharmacological studies are described according to cytotoxicity, anti-inflammatory, antiviral, immunostimulation, antioxidant, CNS-related response, vascular, hypotensive, mutagenicity and antibacterial properties. The potential for development of leads from Uncaria continues to grow, particularly in the area of immunomodulatory, anti-inflammatory and vascular-related conditions. The information summarized here is intended to serve as a reference tool to practitioners in the fields of ethnopharmacology and natural products chemistry.


Subject(s)
Uncaria/chemistry , Adjuvants, Immunologic/chemistry , Animals , Anti-Infective Agents/chemistry , Anti-Inflammatory Agents/chemistry , Antineoplastic Agents, Phytogenic/chemistry , Antioxidants/chemistry , Cardiovascular Agents/chemistry , Central Nervous System Agents/chemistry , Ethnobotany , Humans , Medicine, Traditional , Mutagens/chemistry , Plant Extracts/chemistry , Plant Extracts/pharmacology
18.
J Agric Food Chem ; 51(12): 3541-5, 2003 Jun 04.
Article in English | MEDLINE | ID: mdl-12769521

ABSTRACT

Bioactivity-guided fractionation of cranberry fruit was used to determine the identity of triterpenoid esters from Vaccinium macrocarpon, which inhibit tumor cell growth and may play a role in cancer prevention. In our previous study, a fraction from whole fruit exhibited tumor cell growth inhibition in vitro. The major components of this fraction were isolated by chromatographic separation of ethyl acetate extracts, purified by semipreparative HPLC, and identified by NMR as cis- (1) and trans- (2) isomers of 3-O-p-hydroxycinnamoyl ursolic acid. These triterpenoid esters have not been previously reported in Vaccinium fruit. Bioassay of the purified triterpene cinnamates in tumor cell lines in vitro showed slightly greater activity of compound 1 in most cell lines, with GI(50) values of approximately 20 microM in MCF-7 breast, ME180 cervical and PC3 prostate tumor cell lines. Quercetin was slightly less active than 1, while cyanidin-3-galactoside exhibited much lower cytotoxicity, with GI(50) greater than 250 microM in all cell lines. Phenylboronic acid (3) was also isolated from the fruit but showed insignificant antitumor activity.


Subject(s)
Antineoplastic Agents, Phytogenic/analysis , Coumaric Acids/analysis , Neoplasms/prevention & control , Triterpenes/analysis , Vaccinium macrocarpon/chemistry , Antineoplastic Agents, Phytogenic/pharmacology , Cell Division/drug effects , Chromatography, High Pressure Liquid/methods , Coumaric Acids/pharmacology , Humans , In Vitro Techniques , Magnetic Resonance Spectroscopy , Plant Extracts/analysis , Triterpenes/chemistry , Triterpenes/isolation & purification , Tumor Cells, Cultured
19.
J Ethnopharmacol ; 79(1): 133-8, 2002 Jan.
Article in English | MEDLINE | ID: mdl-11744307

ABSTRACT

Extracts of eight medicinal plants from the Callejon de Huaylas in Peru were screened for antibacterial activity in eighteen bacterial strains by the agar-diffusion method; six of these were active against a variety of bacteria.


Subject(s)
Anti-Bacterial Agents/pharmacology , Plant Extracts/pharmacology , Plants, Medicinal , Ethnobotany , Microbial Sensitivity Tests , Peru
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