Search

Pseuduvaria phuyensis (Annonaceae), was collected from Kanchanaburi Province, western Thailand. The study aimed to evaluate the antibacterial, anti-HIV-1RT, anti-syncytium (MC99+1A2), and cytotoxic potentials of the crude hexane, ethyl-acetate, and methanol extracts of P. phuyensis leaf-twigs and stems, all in comparison with standard drugs. Also, the isolation and characterization of a compound from one of the active extracts as well as its antibacterial and cytotoxicity activities were carried out. The MIC and MBC values of selected bacterial strains ranged from 3.125 - 200 and 6.25 - 200 mg/mL, respectively for all the extracts, while the isolated compound was not active. The anti-HIV-1 RT and the anti-syncytium assay of the hexane and ethyl acetate extracts revealed they were very active, with % inhibitions of 90.50 and 89.36, respectively. The best inhibitory concentration at 50% (IC50) value was 44.33 µM as exhibited by the hexane extract of the stems of the reverse transcriptase assay, while, the best effective concentration at 50% (EC50) value was 10.4 µM (TI>4.83) as displayed by the ethyl acetate extract of the stems. The cytotoxicity study showed that the hexane extract of the stems displayed high cytotoxicity with ED50 value at 13.07 µg/mL against the FaDu cancer cell line, whil that of the isolated compound was not active. The structure of the isolated compound was characterized and elucidated as trans, trans-cyclohexane-1, 2, 4, 5-tetrol monohydrate using spectroscopic technique and X-ray crystallography analysis. [ABSTRACT FROM AUTHOR]

Zingiber Officinale Roscoe, a famous plant that has been used worldwide for the consumption and treatment of human ailments. In Thailand, ginger is grown in many areas throughout the country. Lampang is subjected to be one of the northern provinces where ginger growing had remarkably increased in recent years. This study aimed to determine the amounts of 6-gingerol and camphene from Z. Officinale Roscoe grown in Ban Pha-Daeng, Ngao District, Lampang Province in 2020 and 2021. Dried rhizome of Z. Officinale was extracted with hexane, ethyl acetate and methanol. 6-gingerol and camphene of three crude extracts were analyzed using High Performance Liquid Chromatography –Photo Diode Array (HPLC-PDA) method. The content of 6-gingerol in all extracts was found in the range of 1.95 to 13.85 mg/g while the content of camphene was found in the range of 1.39 to 51.97 mg/g. The level of 6-gingerol and camphene in ethyl acetate extracts was greater than the hexane and methanol extracts. The result indicated the amounts of 6-gingerol and camphene of Z. Officinale grown in 2020 was higher compared to the content in 2021. [ABSTRACT FROM AUTHOR]

Oxidative stress mediated apoptosis of renal tubular cells is a major pathology of gentamicin-induced nephrotoxicity, which is one of the prevailing causes of acute renal failure. Pinocembrin is a major flavonoid found in rhizomes of fingerroot (Boesenbergia pandurata). It has pharmacological and biological activities including antimicrobial, anti-inflammatory, and anti-oxidant effects. Preclinical studies have suggested that pinocembrin protects rat brain and heart against oxidation and apoptosis induced by ischemia-reperfusion. The aim of the current study was to investigate the mechanisms of renoprotection elicited by pinocembrin in gentamicin-induced nephrotoxicity. Nephrotoxicity was induced in rats by intraperitoneal injection (i.p.) of gentamicin, and pinocembrin was administered via i.p. 30 min before gentamicin treatment for 10 days. Gentamicin- induced nephrotoxicity was indicated by the reduced renal function and renal Oat3 function and expression. Gentamicin treatment also stimulated Nrf2, HO-1, and NQO1, as well as the pro-apoptotic proteins Bax and caspase-3, concomitant with the attenuation of Bcl-XL expression in the renal cortical tissues. Pinocembrin pretreatment improved renal function and renal Oat3 function and reduced oxidative stress and apoptotic conditions. These findings indicate that pinocembrin has a protective effect against gentamicin-induced nephrotoxicity, which may be due in part to its antioxidant and anti-apoptotic effects, subsequently leading to improved renal function. Key words: pinocembrin, nephrotoxicity, renal function, organic anion transporter, gentamicin, oxidative stress, apoptosis. L'apoptose dependant du stress oxydatif dans les cellules tubulaires renales est un effet nephrotoxique majeur de la gentamicine et une cause preponderante d'insuffisance renale aigue. La pinocembrine est un important compose flavonoide que l'on trouve dans les rhizomes de gingembre chinois (Boesenbergia pandurata). Son activite pharmacologique et biologique entraine des effets antimicrobiens, anti-inflammatoires et antioxydants. Les resultats des etudes precliniques laissent presumer que la pinocembrine permet de proteger les cellules du cerveau et du coeur contre l'apoptose dans un modele d'ischemie- reperfusion chez le rat. Les presents travaux visaient a etudier les mecanismes de nephroprotection mobilises par la pinocembrine contre la toxicite renale associee a la gentamicine. Nous avons induit la nephrotoxicite chez le rat en injectant de la gentamicine par voie intraperitoneale (i.p.) 30 min apres l'administration i.p. de pinocembrine pendant 10 jours. La nephrotoxicite induite par la gentamicine se manifestait par la diminution de la fonction renale de meme que de la fonction et de l'expression de l'Oat3. L'administration de gentamicine a aussi active Nrf2, HO-1 et NQO1 ainsi que la proteine pro-apoptotique Bax et la caspase 3, tout en attenuant l'expression de Bcl-XL dans le cortex renal. Le pretraitement par la pinocembrine a permis d'ameliorer la fonction renale et la fonction de l'Oat3 dans le rein et d'attenuer le stress oxydatif et de faire retroceder d'apoptose. Ces resultats montrent les effets protecteurs que la pinocembrine exerce contre la nephrotoxicite causee par la gentamicine. Ceux-ci pourraient etre en partie lies aux effets antioxydants et anti-apoptotiques du traitement qui permettent subsequemment d'ameliorer la fonction renale. [Traduit par la Redaction] Mots-cles: pinocembrine, nephrotoxicite, fonction renale, transporteur anionique organique, gentamicine, stress oxydatif, apoptose., Introduction Gentamicin, an aminoglycoside antibiotic, has been widely used as a bactericidal agent against severe Gram-negative infections (Edson and Terrell 1999; Noone et al. 1974). However, prolonged treatment of gentamicin [...]

One new clerodane-type diterpenoid, together with one known, was isolated from the leaves and twigs of C. krabas. The structures of these compounds were elucidated as krabasinolide A (1) and taraxerol (2) by spectroscopic methods (UV, IR, HRESIMS, 1 D, and 2 D NMR), and the relative stereochemistry was confirmed by X-ray diffraction analysis with graphite monochromated Mo-Kα (λ = 0.71073 Å) radiation at 296(2) K. Extracts and compounds 1-2 were evaluated for in vitro antiviral activity. [ABSTRACT FROM AUTHOR]

Problem statement: Medicinal plants derived anticancer were now being subjects of many research groups especially, the secondary metabolite triterpenoids trees which had enormous potential to inspire and influence modern antiproliferative research. The study aimed to investigate the chemical constitution and their potential use as antiproliferative activity of purified compounds derived from F. virosa. Approach: The F. virosa was selected and percolated with hexane, ethyl acetate, acetone and methanol. The extracts were purified and elucidated chemical structures. Furthermore, the isolated compounds were tested for biological activity. The bioassays were performed on two cancer cell lines, adriamycin-sensitive erythroleukemia cells (K562) and adriamycin-resistant erythroleukemia cells (K562/Adr) which overexpressed P-glycoprotein (MDR1/ABCB1). Results: Friedelin (1), epifriedelanol (3), stigmasterol (4) and betulinic acid (5) were isolated from the leaves and twigs of F. virosa. The molecular structures of these compounds were determined using several spectroscopic methods. The compounds i.e., 1, a chemically modified compound 1 heptanolide (2), 3 and 4 showed a limited cytotoxic activity towards human cancer cell lines mainly due to a low aqueous solubility which prevented their use in cell viability assays. Interestingly, compound 5 exhibited a high cytotoxicity characterized by an effective concentration value ([IC.sub.50]) equal to 9.7[+ or -]2.1 [micro][g.mL.sup.-1] (21.2[+ or -]4.6 [micro]M) and 7.1[+ or -]0.7 [micro][g.mL.sup.-1] (15.5[+ or -]1.5 [micro]M) for K562 and K562/Adr, respectively. Moreover, the antiproliferative activity of compound 5 was independent of the multidrug resistance phenotype exhibited by the K562/Adr cell line suggesting that compound 5 was not the effluxes out of the K562/Adr cells by MDR1 (ABCB1). Conclusion: The results clearly showed that the betulinic acid of the four isolated compounds from F. virosa could be considered as high potential source of cytotoxic activity. Key words: Triterpenoids, betulinic acid, antiproliferation, Flueggea virosa, INTRODUCTION Genus Flueggea, belonging to the Euphorbiaceae family, contains 4 species were F. acidoton, F. neowawraea, F. tinctoria and F. virosa, which are shrubs and widely distributed among the tropical [...]

A new ent-kaurane-type diterpenoid, crotonmekongenin A (1) together with two known compounds, epifriedelanol (2) and sitosterol glucoside (3) from the leaves and twigs of Croton mekongensis were isolated. The structure of these compounds was determined by spectroscopic analysis. The structure of the new ent-kaurane-type diterpenoid (1) was elucidated using spectroscopic technique and X-ray crystallography analysis. Moreover, the cytotoxicity of all extract and isolated compounds was tested for cytotoxicity against KKU-M213, FaDu, HT-29, MDA-MB-231, A-549, SH-SY5Y, and CL cell lines. Compound 1 showed significant cytotoxic activity (ED50) on FaDu (0.48 µg/ml), HT-29 (0.63 µg/ml), and SH-SY5Y (0.45 µg/ml). [ABSTRACT FROM AUTHOR]

Two new labdane diterpene derivatives, crotondecalvatin A (1) and crotondecalvatin B (2) were obtained from the leaves and twigs of Croton decalvatus. The structures of compounds were established on the basis of extensive spectroscopic data. [ABSTRACT FROM AUTHOR]