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

Determination of Phytochemical Compounds, and Tyrosinase Inhibitory and Antimicrobial Activities of Bioactive Compounds from Streblus ilicifolius (S Vidal) Corner

Purpose: To determine the phytochemical content, and tyrosinase inhibitory and antimicrobial activities of the wood from Streblus ilicifolius (S. Vidal) CornerMethods: The dried wood of S. ilicifolius (8.70 kg) was extracted by maceration to give petroleum ether, ethyl acetate, ethanol and water extracts, respectively. Dopachrome method was used to determine antityrosinase activity. Agar disc diffusion and modified broth microdilution methods were used to determine antimicrobial activity. Chromatographic techniques were used for phytochemical investigation. The structures elucidation of isolated compounds were identified by physical properties and spectroscopic data including UV, IR, NMR and MS data and confirmed by comparison with previously reports.Results: The ethanol extract exhibited tyrosinase inhibition and antimicrobial activity against the Grampositive bacteria, Staphylococcus epidermidis and S. aureus. Phytochemical investigation showed five compounds, namely, (E)-2,4-dihydroxy-3 (3,7-dimethyl-2,6-octadienyl) benzaldehyde (1), phydroxybenzoic acid methyl ester (2), umbelliferone (3), moracin M (4), trans-resveratrol (5). Compound 4 exhibited tyrosinase inhibition with half maximal inhibitory concentration (IC50) of 67.69 μg/ml, while compound 1 displayed strong activity against S. epidermidis, S. aureus and methicillin-resistant S. aureus (MRSA) with minimum inhibitory concentration (MIC) of 8, 4 and 8 μg/ml, respectively and minimum bactericidal concentration (MBC) of 32, 16 and 64 μg/ml, respectively.Conclusion: This is the first report of the biological activities and phytochemical composition of S. ilicifolius and the results indicate the high potentials of the plant for commercial applications such as in facial whitening and anti-acne cream.Keywords: Streblus ilicifolius, Moraceae, Tyrosinase inhibition, Antimicrobial, Anti-acne, Methicillinresistant Staphylococcus aureu

BIO-ACTIVITIES AND PHYTOCHEMICAL INVESTIGATION OF CNESTIS PALALA (LOUR.) MERR.

Background: In traditional medicines, the root of Cnestis palala was used for the treatment of stomach ache, malaria, urinary track disorders and snakebite. The seed was used for poisoning rat and stray dogs. However, the bioactivities and chemical constituents have not been reported. So, this will be the first report. Material and Methods: Biological investigations of C. palala extracts against bacteria (Staphylococcus aureus, Staphylococcus epidermidis, Propionibacterium acnes, Escherichia coli, and Pseudomonas aeruginosa), fungi (Trichophyton mentagrophytes, Trichophyton rubrum and Microsporum gypseum), yeast (Candida albicans), tuberculosis (Mycobacterium tuberculosis), malaria (Plasmodium falciparum) and cancer cell lines (MCF-7 and HT-29) were evaluated. The chromatographic and spectroscopic techniques were used for the isolation and identification of pure compounds. Results: The results showed that the ethanol leaf and bark extracts were active against S. aureus and S. epidermidis. The hexane leaf and seed extracts and petroleum ether bark and root extracts showed strongly inhibition values against MCF-7. Moreover, the petroleum ether bark extract exhibited high inhibition value against HT-29. Seven compounds were isolated as β-sitosterol-glucoside (CP1), hydroquinone (CP2), β-sitosterol (CP3), mixture of fatty acids (CP4) and ethyl caffeate (CP5), scopoletin (CP6) and 2-nonenal (CP7). The CP2 was strongly active against S. aureus and S. epidermidis, the MIC was showed 30.10 µg/ml and 15.05 µg/ml and the MBC was showed 15 µg/ml and 7.5 µg/ml, respectively. Conclusion: These results suggested that C. palala is a great potential source of anti-microbial agents. Hence, this is the first study, which will be the database for chemical constituents and bioactivities of C. palala

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

Nitric oxide inhibitory substances from <i>Curcuma mangga</i> rhizomes

<i>Curcuma mangga</i> Val. & Zijp. is a member of the Zingiberaceae family commonly grown in Thailand. It is locally known as mango tumeric because of its mango-like smell when the fresh rhizomes are cut. C. mangga is a popular vegetable, the tips of the young rhizomes and shoots are consumed raw with rice. Medicinally, the rhizomes are used as a stomachic and for chest pains, fever, and general debility. It is also used in postpartum care. In the present study, we investigated the anti-inflammatory effect of the extract and compounds from C. mangga rhizomes against lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 cell line. From bioassay-guided fractionation, the chloroform fraction exhibited the most potent inhibitory activity with an IC50 value of 2.1 g/ml, followed by the hexane fraction (IC50 = 3.8 g/ml) and the ethyl acetate fraction (IC50 = 23.5 g/ml), respectively. Demethoxycurcumin (1) and 3-buten-2-one, 4-[(1R, 4aR, 8aR)-decahydro-5, 5, 8a-trimethyl-2-methylene-1-naphthalenyl]-, (3E)-rel- (2) were isolated from the chloroform- and hexane fractions, respectively. Bisdemethoxycurcumin (3) whose structure is similar to that of 1 was also tested for NO inhibitory activity. Of the tested compounds, compound 1 exhibited the highest activity with an IC50 value of 12.1 μM, followed by 3(IC50 = 16.9 M) and 2 (IC50 = 30.3 M). These results suggest that C. mangga and its compounds exert NO inhibitory activity and have a potential to be developed as a pharmaceutical preparation for treatment of inflammatory-related diseases. Moreover, this is the first report of compound 2 that was isolated from C. mangga rhizomes

Flavonoid Constituents and Alpha-Glucosidase Inhibition of Solanum stramonifolium Jacq. Inflorescence with In Vitro and In Silico Studies

Solanum stramonifolium Jacq. (Solanaceae) is widely found in South East Asia. In Thailand, it is used as vegetable and as a component in traditional recipes. The results of an alpha-glucosidase inhibitory screening test found that the crude extract of S. stramonifolium inflorescence exhibited the potential effect with IC50 81.27 &mu;g/mL. The separation was performed by the increasing solvent polarity method. The ethyl acetate, ethanol, and water extracts of S. stramonifolium inflorescence showed the synergistic effect together with acarbose standard. The phytochemical investigation of these extracts was conducted by chromatographic and spectroscopic techniques. Six flavonoid compounds, myricetin 3, 4&prime;, 5&prime;, 7-tetramethyl ether (1), combretol (2), kaempferol (3), kaempferol 7-O-glucopyranoside (4), 5-hydroxy 3-7-4&prime;-5&prime;-tetramethoxyflavone-3&prime;-O-glucopyranoside (5), and a mixture (6) of isorhamnetin 3-O-glucopyranoside (6a) and astragalin (6b) were isolated. This discovery is the first report of flavonoid-glycoside 5. Moreover, the selected flavonoids, kaempferol and astragalin, were representatives to explore the mechanism of action. Both of them performed mixed-type inhibition. The molecular docking gave a better understanding of flavonoid compounds&rsquo; ability to inhibit the alpha-glucosidase enzyme

Inhibitors of HIV-1 integrase from Dioscorea bulbifera

A search for HIV-1 integrase (IN) inhibitors from natural sources has led to the isolation of compounds from Dioscorea bulbifera bulbils. From the bioassay-guided isolation, the chloroform fraction was then fractionated to obtain one new clerodane diterpenoid (diosbulbin E acetate, 4), two known clerodane diterpenoids (1-2), four flavonoids (5-8) and one sterol glucoside (3). Quercetin (7) exhibited the strongest anti-HIV-1 IN activity with an IC50 value of 16.28 µM, followed by kaempferol (8, IC50 = 37.71 µM), whereas (+)-catechin (6) possessed moderate activity (IC50 = 62.36 µM). Moreover, the clerodane-type diterpenoids (1 and 4) also exhibited moderate inhibitory effects with IC50 values of 70.39 and 73.49 µM, respectively. The flavonoid compounds (5-8) were also investigated for their interactions with the IN active sites using a molecular docking method. They interacted with Thr66, His67, Gln148, Glu152 and Lys159, which are important amino acid residues for inhibition of HIV-1 IN activity

In vivo evaluation of analgesic and antipyretic activities of piceatannol-rich extract from Senna garrettiana heartwood

A methanolic extract from Senna garrettiana (S. garrettiana) heartwood was prepared and then a fractionation process was performed to obtain hexane, dichloromethane, ethyl acetate, and aqueous fractions. An antinociceptive screening of each fraction was carried out using the acetic acid-induced writhing in mice. Among all the fractions, the ethyl acetate fraction showed the highest activity on the writhing test. The ethyl acetate fraction was separated to obtain a piceatannol-rich extract. The S. garrettiana extract contains 11.70 % w/w and 39.16 % w/w piceatannol in the ethyl acetate fraction and the piceatannol-rich extract, respectively. The analgesic activities of the ethyl acetate fraction (50, 100 and 200 mg/kg) and the piceatannol-rich extract (10, 20 and 40 mg/kg) were evaluated by the acetic acid-induced writhing test, hot-plate test and formalin test. The antipyretic activity of these extracts was assessed on yeast’s-induced pyrexia in rats. The acute toxicity was also investigated. In the acute toxicity study, no lethality was observed after the oral administration of methanolic extract of S. garrettiana heartwood even at a high dose of 5 g/kg in mice. The oral administration of the ethyl acetate fraction decreased the number of writhings in a dose dependent manner with 54.9 %, 68.5 %, and 71.0 % inhibition, respectively. A similar result was also observed after the oral administration of the piceatannol-rich extract with 53.1%, 69.2% and 80.3% inhibition, respectively. In the formalin test, either the ethyl acetate fraction or the piceatannol-rich extract significantly diminished the licking time in both the early and late phases. Neither the ethyl acetate nor the piceatannol-rich extract had any effect on heat-induced pain. The ethyl acetate fraction at the same dosage range significantly decreased the rat rectal temperature at 2, 3 and 4 hrs. The piceatannol-rich extract at a dose of 20 and 40 mg/kg suppressed the rectal temperature over the same time intervals. These results demonstrated that the ethyl acetate fraction and the piceatannol-rich extract from S. garrettiana heartwood possessed analgesic and antipyretic activities with an apparently similar efficacy. The probable mechanism(s) of analgesic actions might be mediated by both the peripheral and central mechanisms

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