Evaluation of reversible contraceptive potential of Cordia dichotoma leaves extract

Evaluation of reversible contraceptive potential of Cordia dichotoma leaves extract
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DOI:
10.1590/s0102-695x2013005000020
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发表时间:
2013-04-01
期刊:
Revista Brasileira de Farmacognosia
影响因子:
--
通讯作者:
Saha, Achintya
Saha, Achintya
中科院分区:
其他
文献类型:
--
作者:
Bhattacharya, Plaban;Saha, Achintya

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考虑到甾体避孕药的安全风险比,本研究旨在评价民族避孕药-双果木的使用情况。福斯特,紫草科,叶(LCD)。对交配后雌性白化病大鼠进行初步药理学筛选。在800 mg/kg剂量水平下,叶提取物(LD 50 5.50 g/kg bw)显示出100%的抗着床活性(n=10)。以(2-羟丙基)-β-环糊精(BCD)为生物利用度增强剂,制备了LCD-BCD复合物。在250 mg/kg剂量水平下,LCD-BCD复合物(1:1,w/w)显示出100%妊娠拦截(n=20),并且还显示出强雌激素潜力和黄体期缺陷。进行了定性和定量的植物化学分析。LCD提取物通过经验证的HPTLC方法进行标准化,并分离出两种避孕植物成分,芹菜素和木犀草素。进行详细的药理学分析,然后进行慢性毒性研究,以预测所开发的植物药物的可逆性。组织学和生化指标检测停药后的可逆避孕潜力。结果表明,所开发的植物药具有潜在的抗生育活性,且具有安全性。
Considering the safety-risk ratio of steroidal contraceptives, the present work was carried out to evaluate ethno-contraceptive use of Cordia dichotoma G. Forst., Boraginaceae, leaves (LCD). Preliminary pharmacological screening was performed on post-coital female albino rats. The leaves extract (LD50 5.50 g/kg bw) showed 100% anti-implantation activity (n=10) at 800 mg/kg dose level. (2-hydroxypropyl)-beta-cyclodextrin (BCD) was used as bioavailability enhancer to form LCD-BCD complex, characterized by DLS, SEM and XRD analyses. The LCD-BCD complex (1: 1, w/w) exhibited 100% pregnancy interception (n=20) at the dose level of 250 mg/kg and also showed strong estrogenic potential with a luteal phase defect. Qualitative and quantitative phytochemical analyses were carried out. The LCD extract was standardized by a validated HPTLC method and two contraceptive phytoconstituents, apigenin and luteolin were isolated. A detailed pharmacological analyses followed by chronic toxicity study were performed to predict the reversible nature of the developed phytopharmaceutical. The histological and biochemical estimations detected the reversible contraceptive potential after withdrawal. The observations suggested that the developed phyto-pharmaceutical has potential antifertility activity with safety aspects.