氯代同型异黄酮的氟、碘和羟基衍生物的药理研究

D. Gaikwad, R. Murkute, S. Gaikwad
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摘要

本研究对合成的取代类同型异黄酮衍生物进行体内/体外抗关节炎、体外抗炎和DPPH自由基清除活性的筛选。采用雄性Wistar大鼠,研究其体内抗CFA性关节炎的活性,评估其足部体积、血清标记酶(ALP、SGOT和SGPT)和膜稳定电位的变化。体外抗炎活性用蛋白变性法测定。采用DPPH法测定其体外自由基清除能力。结果表明,与其他取代的同型异黄酮衍生物相比,化合物HIFa具有明显的抗关节炎活性。取代的异黄酮衍生物具有明显的膜稳定作用和抑制蛋白变性的作用,具有体外抗关节炎和抗炎活性。取代的同型异黄酮衍生物具有剂量依赖性的DPPH自由基清除活性。从本研究中,我们观察到碘衍生物取代的同型异黄酮衍生物具有显著的药理活性相比,氟和羟基衍生物。
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Pharmacological Investigation of Fluoro, Iodo and Hydroxy Derivative of Chloro Substituted Homoisoflavonoids
In present study, the synthesized substituted homoisoflavonoid derivatives were screened for their in vivo/in vitro antiarthritic activity, in vitro anti-inflammatory and DPPH free radical scavenging activity. The male Wistar rats were used for investigation of in vivo antiarthritic activity against complete freund’s adjuvant (CFA) induced arthritis and assessment was done for change in paw volume, serum marker enzymes (ALP, SGOT and SGPT) and membrane stabilization potential. in vitro anti-inflammatory activity was assessed by the protein denaturation method. In vitro free radical scavenging activity was assessed by the DPPH method. The result indicated that compound HIFa showed a significant antiarthritic activity as compared to other substituted homoisoflavonoid derivatives. The significant membrane stabilization and inhibition of protein denaturation showed in vitro antiarthritic and antiinflammatory activity of substituted homoisoflavonoid derivatives. The substituted homoisoflavonoid derivatives showed dose dependent DPPH free radical scavenging activity. From the present study, it was observed that the iodo derivative of substituted homoisoflavonoid derivatives have significant pharmacological activities as compared to floro and hydroxyl derivatives.
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