Anti-cancer activity of compounds from Cassia garrettiana heartwood

The ethanol extract of Cassia garrettiana heartwood showed marked inhibitory activity against several cancer cell lines including HT-29, HeLa, MCF-7 and KB cells. Therefore, its extract and compounds were investigated for their anticancer effect using the Sulforhodamine B (SRB) assay. The ethanol extract of C. garrettiana heartwood was separated to give five compounds which are chrysophanol (1), piceatannol (2), aloe-emodin (3), emodin (4) and cassigarol E (5). Of the tested samples, chrysophanol (1) showed the highest anti-cancer activity against KB cells (IC50 = 0.045 g/mL), aloe emodin (3) was the most active against HT-29 (IC50 = 0.29 g/mL), emodin (4) was against HeLa cells (IC50 = 0.82 g/mL), and cassigarol E (5) was active against MCF-7 (IC50 = 0.021 g/mL), whereas piceatannol (2) was inactive in all tested cell lines. This is the first report of anti-cancer effect against HT-29, HeLa, MCF-7 and KB cells of C. garrettiana heartwood

DEVELOPMENT AND VALIDATION OF LC-MS METHOD FOR QUANTITATIVE ANALYSIS OF A TRADITIONAL THAI ANTIHYPERTENSIVE HERBAL RECIPE

Objective: To develop a new validated LC-MS method in which can be used for identification and quantification of the active pharmaceutical compounds in a traditional Thai antihypertensive herbal recipe (TTAH). Methods:  First, a quadrupole-ion trap MS was used to identify the active pharmaceutical compounds to facilitate a set of markers in the TTAH using multiple reactions monitoring (MRM) method. Coupling to LC in gradients mode, the chromatogram of the TTAH was established. Second, the method validation was conducted to observe several parameters, such as, carryover, linearity, a limit of detection, a limit of quantification, precision, accuracy, robustness, specificity, and system suitability. Results: Piperine, imperatorin, and pinostrobin were identified using the quadrupole-ion trap MS by comparison the mass spectrum of the TTAH samples and reference standards. The parent and product ions were optimized using MRM method. Good chromatographic peaks were achieved along with a simple and fast analysis. All parameters were validated and found that the method reported in this article can be used to quantify the amount of piperine, imperatorin, and pinostrobin in the TTAH. Conclusion: Piperine, imperatorin, and pinostrobin were selected as the markers in LC-MS analysis of the TTAH. This new validated LC-MS method is readily to use in a quality assurance of the TTAH

การศึกษาฤทธิ์ต้านเอนไซม์ HIV-1 integrase ในสมุนไพรไทย

Thesis (M.Sc., Herb Sciences)--Prince of Songkla University, 201

Anti - HIV-1 integrase activity of Thai Medicinal Plants

For the purpose of discovering anti-HIV-1 agents from natural sources, the aqueous and EtOH extracts of eight Thaiplants including Clerodendron indicum (whole plant), Tiliacora triandra (stem), Capparis micracantha (wood), Harrissoniaperforata (wood), Ficus glomerata (wood), Diospyros decandra (wood), Dracaena loureiri (heartwood), and Tinospora crispa (stem) were screened for their inhibitory activities against HIV-1 integrase (IN) using the multiplate integration assay(MIA). Of the EtOH extracts, Ficus glomerata (wood) was the most potent with an IC50 value of 7.8 g/ml; whereas the water extract of Harrisonia perforata (wood) was the most potent aqueous extract with an IC50 value of 2.3 g/ml. The isolation of active principles against HIV-1 IN from Ficus glomerata is now actively pursued

Anti-HIV-1 integrase activity of compounds from Cassia garrettiana heartwood

Abstract The ethanol extract of heartwood from Cassia garrettiana had strong anti-HIV-1 integrase (IN) activity with an IC 50 value of 3.0 µg/mL. Therefore, its fractions and compounds were investigated for their anti-HIV-1 IN effect using the multiplate integration assay (MIA). From bioassay-guided isolation, the ethyl acetate fraction was then separated to give five compounds which are chrysophanol (1), piceatannol (2), aloe-emodin (3), emodin (4) and cassigarol E (5). Of the tested samples, piceatannol (2) showed the highest activity against HIV-1 IN with an IC 50 of 17.9 µM, followed by cassigarol E (5, IC 50 = 72.9 µM), respectively. From the present study, this is the first report on anti-HIV-1 IN activity of Cassia garrettiana

Anti-HIV-1 integrase activity of compounds from Cassia garrettiana heartwood

Abstract The ethanol extract of heartwood from Cassia garrettiana had strong anti-HIV-1 integrase (IN) activity with an IC 50 value of 3.0 µg/mL. Therefore, its fractions and compounds were investigated for their anti-HIV-1 IN effect using the multiplate integration assay (MIA). From bioassay-guided isolation, the ethyl acetate fraction was then separated to give five compounds which are chrysophanol (1), piceatannol (2), aloe-emodin (3), emodin (4) and cassigarol E (5). Of the tested samples, piceatannol (2) showed the highest activity against HIV-1 IN with an IC 50 of 17.9 µM, followed by cassigarol E (5, IC 50 = 72.9 µM), respectively. This is the first report on anti-HIV-1 IN activity of Cassia garrettiana

EVALUATION OF PHYSICOCHEMICAL PROPERTIES OF A TRADITIONAL THAI ANTIHYPERTENSIVE HERBAL RECIPE IN VARIOUS PREPARATIONS

Objective: The purpose of this article was to prepare a new suitable dosage form of a traditional Thai antihypertensive herbal recipe (TTAH). All details in a preformulation study and physicochemical properties of the preparations were reported. Methods: Three different formulations were prepared and evaluated for their physicochemical properties. The preformulation studies were investigated including angle of repose, bulk density, tapped density, Carr's index, and Hausner ratio before further formulation.The appropriate formulations were evaluated in their physicochemical properties such as weight variation, friability, thickness, hardness, disintegration time, and content uniformity. Results: The C1 capsule contained 400 mg of herbal powder was the best dosage form because of its good results in physicochemical properties evaluation such as weight variation (489.2±10.84 mg), disintegration time (4.02±1.20 min), and content uniformity (piperine98.38±1.78%, imperatorin98.60±1.08%, and pinostrobin102.44±1.29%). Conclusion: Considering to formulation of the TTAH as a capsule, a tablet, or a pill, many parameters were evaluated. Pills and tablets failed on at least one criterion, with difficulties in manufacturing or disintegrating ability being recorded. Capsules passed all tested criteria and became the formulation of choice for TTAH

Anti-HIV-1 integrase and anti-allergic activities of Bauhinia strychnifolia

A stem ethanol extract of Bauhinia strychnifolia and its compounds were investigated for their anti-HIV-1 integrase (IN) and anti-allergic activities. From bioassay-guided isolation, five compounds including quercetin (1), 3,5,7,3',5' pentahydroxyflavanonol-3-O-α-L-rhamnopyranoside (2), 3,5,7-trihydroxychromone-3-α-L-rhamnopyranoside (3) and a mixture of β-sitosterol (4) and stigmasterol (5) were isolated. Of the tested samples, compound 1 (quercetin) showed the highest activity against HIV-1 IN with an IC50 value of 15.2 µM, followed by 3 (3,5,7-trihydroxychromone-3-α-L-rhamnopyranoside), 4+5 (mixture of β-sitosterol and stigmasterol) and 2 (3,5,7,3',5'-pentahydroxyflavanonol-3-O-α-L-rhamnopyranoside) with % inhibition of 28.2, 26.2 and 6.7 at 100 µM, respectively. With regard to anti-allergic activity, quercetin (1) possessed the highest anti-allergic activity with an IC50 of 8.1 µM, followed by 3 (3,5,7-trihydroxychromone-3-α-L-rhamnopyranoside) and 4+5 (mixture of β-sitosterol and stigmasterol) with IC50 values of 52.1 and 77.5 µM, respectively. Whereas compound 2 (3,5,7,3',5'-pentahydroxyflavanonol-3-O-α-L-rhamnopyranoside) was inactive. The present study is the first report of chemical constituents and biological activities of Bauhinia strychnifolia

Alpha-glucosidase inhibitory activities of astilbin contained in Bauhinia strychnifolia Craib. stems: an investigation by in silico and in vitro studies

Abstract Introduction Bioactive compounds from traditional medicines are good alternatives to standard diabetes therapies and may lead to new therapeutic discoveries. The stems of Bauhinia strychnifolia Craib. (BC) have a possible antihyperglycemic effect; However, the extraction of astilbin from BC has never been recorded in alpha-glucosidase inhibitory activities. Methods Using liquid chromatography–mass spectrometry (LC–MS/MS), 32 compounds were detected in the BC extract. The screening was based on peak area. Seven compounds found. PASS recognized all seven compounds as potential alpha-glucosidase (AG) inhibitors. Astilbin and quercetin 3-rhamnoside were the most likely inhibitors of AG. Arguslab, AutoDock, and AutoDock Vina investigated the binding of the two compounds and AG. The binding stability was confirmed by molecular dynamics (MD). In addition, the optimum solvent extraction was studied via CosmoQuick, and extracts were examined with 1H-NMR prior to testing with AG. Results All three software programs demonstrated that both compounds inhibit AG more effectively than acarbose. According to the sigma profile, THF is recommended for astilbin extraction. The BC extract with THF showed outstanding AG inhibitory action with an IC50 of 158 ± 1.30 µg mL-1, which was much lower than that of the positive control acarbose (IC50 = 190 ± 6.97 µg mL-1). In addition, astilbin from BC was found to inhibit AG strongly, IC50 = 22.51 ± 0.70 µg mL-1 through the extraction method of large-scale astilbin with THF has the best extraction capacity compared to other solvents, hence the initial stage of extraction employs THF to extract and precipitate them with ethyl acetate and water. Conclusion In silico and in vitro studies reveal that astilbin inhibits AG and is superior to acarbose, validating its promise as an AG inhibitor. Overall, astilbin was the most bioactive component of BC for antidiabetic action

The potency of herbal extracts and its green synthesized nanoparticle formulation as antibacterial agents against Streptococcus mutans associated biofilms

This study aims to determine the effects of the extracts of Streblus asper, Cymbopogon citratus, Syzygium aromaticum and its formulation of green synthesized silver nanoparticle (AgNPs) on Streptococcus mutans growth and biofilm formation. The ethanolic extracts of S. asper, C. citratus, S. aromaticum, and a mix of the three herbs demonstrated antibacterial activity against S. mutans isolates by reducing bacterial biofilm formation and decreasing bacterial cell surface hydrophobicity. The formulated AgNPs from the ethanolic extracts could enhance the antibacterial activities of the plant extracts. Molecular docking found the best interaction between luteolin isolated from C. citratus and glucosyltransferase protein (GtfB), assuming the promising anti-biofilm activity. The scanning electron microscopy revealed morphological changes in the biofilm structure and a significant decrease in the biofilm area of the AgNPs treated. The study suggested that the extracts and its application could be used as natural alternative agents with multi-action against S. mutans infections