Cytotoxicity, antimicrobial and antioxidant activity of eight compounds isolated from Entada abyssinica (Fabaceae)

BACKGROUND : Entada abyssinica is a plant traditionally used against gastrointestinal bacterial infections. Eight compounds including three flavonoids, three terpenoids, a monoglyceride and a phenolic compound isolated from E. abyssinica were investigated for their cytotoxicity, antibacterial and antioxidant activity. RESULTS : Compounds 7 and 2 had remarkable activity against Salmonella typhimurium with the lowest respective minimum inhibitory concentration (MIC) values of 1.56 and 3.12 μg/mL. The antioxidant assay gave IC50 values varied from 0.48 to 2.87 μg/mL in the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, from 2.53 to 17.04 μg/mL in the 2,2′-Azinobis (3-ethylbenzothiazoline-6-sulphonic acid) diammonium salt (ABTS) assay and from 1.43 to 103.98 μg/mL in the FRAP assay. Compounds had relatively low cytotoxicity (LC50 values ranging from 22.42 to 80.55 μg/mL) towards Vero cells. Ursolic acid had the most potent cytotoxicity against THP-1 and RAW 264.7 cells with LC50 values of 9.62 and 4.56 μg/mL respectively, and selectivity index values of 7.32 and 15.44 respectively. CONCLUSION : Our findings suggest that among the terpenoid and flavonoid compounds studied, entadanin (compound 7) possess tremendous antibacterial activity against S. typhimurium and could be developed for the treatment of bacterial diseases.The National Research Foundation (NRF) and Medical Research Council (MRC).The University of Pretoria provided a postdoctoral fellowship to JPD.http://www.biomedcentral.com/bmcpublichealtham2017Paraclinical Science

Cytotoxicity, nitric oxide and acetylcholinesterase inhibitory activity of three limonoids isolated from Trichilia welwitschii (Meliaceae)

BACKGROUND: Limonoids are highly oxygenated compounds with a prototypical structure. Their occurrence in the plant kingdom is mainly confined to plant families of Meliaceae and Rutaceae. Owing to their wide range of pharmacological and therapeutic properties, this study was aimed at investigating the potential nitric oxide (NO) and acetylcholinesterase (AChE) inhibitory activity and the cytotoxicity of three limonoids: trichilia lactone D5 (1), rohituka 3 (2) and dregeanin DM4 (3), isolated from Trichilia welwitschii C.DC RESULTS: Results indicated that the three limonoids had low cytotoxicity towards Vero cells with LC50 values ranging from 89.17 to 75.82 (μg/L. Compounds (2) and (3) had lower cytotoxicity compared to puromycin and doxorubicin used as reference cytotoxic compounds. Compound (1) (LC50 of 23.55 (μg/L) had good antiproliferative activity against RAW 264.7 cancer cells. At the lowest concentration tested (0.5 μg/mL), compound (2) and (3) released the lowest amount of nitric oxide (2.97 and 2.93 μM, respectively). The three limonoids had anti-AChE activity with IC50 values ranged of 19.13 (μg/L for (1), 34.15 (μg/L for (2) and 45.66 (μg/L for (3), compared to galantamine (IC50 of 8.22 ( g/mL) used as positive control CONCLUSION: The limonoid compounds studied in this work inhibited nitric oxide production in LPS-stimulated macrophages and had anti-AChE activity. Trichilia lactone D5 had potential antiproliferative activity against RAW 264.7 cancer cells. The limonoids had low cytotoxicity towards Vero cells lines. This study provided further examples of the importance of limonoids compounds as potential AChE inhibitors and anti-inflammatory agents targeting the inhibition of NO productio

Rubescins I and J, further limonoid derivatives from the stem bark of <i>Trichilia rubescens</i> (Meliaceae)

<p>Two new tetranorterpenoid derivatives named rubescins I (<b>1</b>) and J (<b>2</b>), were isolated along with six known compounds including rubescin D (<b>3</b>), lichexanthone (<b>4</b>), scopoletin (<b>5</b>), scopoletin <i>O</i>-glycoside (<b>6</b>), <i>β</i>-sitosterol (<b>7</b>) and stigmasterol (<b>8</b>) from the stem bark of <i>Trichilia rubescens</i> (Meliaceae). The structures of the compounds were determined by means of MS, different NMR and by comparison with related data reported in the literature.</p

Cytotoxicity, nitric oxide and acetylcholinesterase inhibitory activity of three limonoids isolated from Trichilia welwitschii (Meliaceae)

BACKGROUND: Limonoids are highly oxygenated compounds with a prototypical structure. Their occurrence in the plant kingdom is mainly confined to plant families of Meliaceae and Rutaceae. Owing to their wide range of pharmacological and therapeutic properties, this study was aimed at investigating the potential nitric oxide (NO) and acetylcholinesterase (AChE) inhibitory activity and the cytotoxicity of three limonoids: trichilia lactone D5 (1), rohituka 3 (2) and dregeanin DM4 (3), isolated from Trichilia welwitschii C.DC RESULTS: Results indicated that the three limonoids had low cytotoxicity towards Vero cells with LC50 values ranging from 89.17 to 75.82 (μg/L. Compounds (2) and (3) had lower cytotoxicity compared to puromycin and doxorubicin used as reference cytotoxic compounds. Compound (1) (LC50 of 23.55 (μg/L) had good antiproliferative activity against RAW 264.7 cancer cells. At the lowest concentration tested (0.5 μg/mL), compound (2) and (3) released the lowest amount of nitric oxide (2.97 and 2.93 μM, respectively). The three limonoids had anti-AChE activity with IC50 values ranged of 19.13 (μg/L for (1), 34.15 (μg/L for (2) and 45.66 (μg/L for (3), compared to galantamine (IC50 of 8.22 ( g/mL) used as positive control CONCLUSION: The limonoid compounds studied in this work inhibited nitric oxide production in LPS-stimulated macrophages and had anti-AChE activity. Trichilia lactone D5 had potential antiproliferative activity against RAW 264.7 cancer cells. The limonoids had low cytotoxicity towards Vero cells lines. This study provided further examples of the importance of limonoids compounds as potential AChE inhibitors and anti-inflammatory agents targeting the inhibition of NO productio

Cytotoxicity, antioxidant and antibacterial activity of four compounds produced by an endophytic fungus Epicoccum nigrum associated with Entada abyssinica

Four compounds including beauvericin, parahydroxybenzaldehyde, indole-3-carboxylic acid and quinizarin were isolated from endophytic fungus Epicoccum nigrum and their cytotoxicity, antibacterial and antioxidant activity were evaluated. Beauvericin had remarkable activity against two Gram-negative strains (Bacillus cereus and Salmonella typhimurium) with respective MIC values of 3.12 and 6.25 μg/ml. All the compounds had weak cytotoxic effect on both normal and tumor cells. LC50 values ranged from 40.42 to 86.56 μg/ml, 31.87 to 86.57 μg/ml and 21.59 to 67.27 μg/ml on Vero cells, THP-1 and RAW 264.7 respectively. The present study showed that these compounds could be developed for the formulation of antioxidant-rich therapeutic diets and as a therapeutic agent against bacterial infections. Keywords: Antimicrobial, Free radical scavenging, Cytotoxicity, Endophytic fungi, Epicoccum nigru

Neomacrodione: a new degraded diterpenoid from the roots of <i>Neoboutonia macrocalyx</i> Beng (Euphorbiaceae)

<p>One new degraded diterpenoid 3,6-dihydroxy-1,7-dimethyl-9,10-phenantroquinone (neomacrodione) (<b>1</b>) together seven known compounds were isolated from the roots of <i>Neoboutonia macrocalyx</i> (Euphorbiaceae). The structures of the compounds were established based on their NMR and mass spectrometric data in conjunction with those previously reported in the literature. Compound (<b>1</b>) displayed moderate antibacterial activities.</p