RESUMEN
This study was carried out to investigate the anti-fertility and anti-venom activities of the extract of the stem bark of Butea monosperma by inhibiting hyaluronidase, which is a spreading factor and plays a role in fertilisation. Among ethanol, methanol and water extracts, the ethanol extract dose-dependently inhibited the ovine, mouse testicular and Vipera russelli snake venom hyaluronidase enzyme activities, with IC50 values 12.00 ± 0.45, 49.40 ± 1.58 µg and 125.42 ± 2.82 µg mL⻹, respectively. In a zymogram assay, the extract showed differential inhibition towards hyaluronidase isoform preferentially with low-molecular weight isoforms. The V. russelli snake venom-induced hemorrhage was significantly reduced at 1:05 ratio of venom-to-extract in mouse. The high antioxidant activity and total phenolic content in the ethanolic extract strongly correlated with the hyaluronidase inhibition. The above results justify the traditional use of the stem bark of B. monosperma as a contraceptive and a strong antidote to snake venom.
Asunto(s)
Butea/química , Hialuronoglucosaminidasa/metabolismo , Corteza de la Planta/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Venenos de Serpiente/enzimología , Testículo/enzimología , Animales , Activación Enzimática/efectos de los fármacos , Masculino , Ratones , Daboia , OvinosRESUMEN
The halo 6-fatty acid esters of L-ascorbic acid 3a, 3b and 6-fatty acid esters of L-ascorbic acid 5a-g were achieved from L-ascorbic acid 1. Compounds 3a, 3b and 5a-g were evaluated for anti-oxidant, anti-lipid peroxidation, and secretory phospholipase A(2) (sPLA(2)) inhibition in vitro, and sPLA(2) induced mouse paw edema. All the derivatives retained their anti-oxidant property compared to ascorbic acid at 6 × 10(-4)M and are good inhibitors of lipid peroxidation at 1 mg ml(-1) as evaluated by 2, 2-Diphenyl-1-picrylhydrazyl radical and thio-barbituric acid methods, respectively. Compounds 5e and 5f significantly inhibited purified group I sPLA(2) from Naja naja and group II sPLA(2) from Vipera russelli, human synovial fluid and human pleural fluid with IC(50) value ranging from 64 ± 1.95 to 82 ± 1.3 and 48 ± 2.27 to 61 ± 2.23 µM, respectively. The compounds 5e and 5f also showed varying degree of potency in neutralizing indirect hemolytic activity of sPLA(2) at 50 µM concentration, and sPLA(2) induced mouse paw edema at the dose 3 mg/kg. Further docking studies also confirmed that compounds 5e and 5f have maximum interaction with increasing negative energy value. Single molecule possessing both anti-oxidant and anti-inflammatory activities is of great therapeutic significance in inflammatory disorders.