Postcoital Antifertility Activity of the Plant Striga densiflora (Scrophulariaceae) on Female Albino Rats

The ethanol and petroleum ether (60–80°C) extracts of S. densiflora, Benth. (Scrophulariaceae), were administered orally to pregnant albino rats for 7 days at the dose of 10 and 20 mg/100 g body weight and showed significant antifertility and estrogenic activity. Histological studies of uterus were carried out to confirm the estrogenic activity of plant extracts. The antifertility activity was reversible on withdrawal of the plant extract treatment.     

Pharmacological effects and pharmacokinetics properties of Radix Scutellariae and its bioactive flavones

Radix Scutellariae is the dried root of the medicinal plant Scutellariae baicalensis Georgi. It exhibits a variety of therapeutic effects and has a long history of application in traditional formulations as well as in modern herbal medications. It has been confirmed that flavonoids are the most abundant constituents and induce these therapeutic effects. Six flavones are proven to be the major bioactive flavones in Radix Scutellariae existing in the forms of aglycones (baicalein, wogonin, oroxylin A) and glycosides (baicalin, wogonoside, oroxylin A-7-glucuronide). All six flavones are pharmacologically active and show great potential in the treatment of inflammation, cancers and virus-related diseases. The current review covers the preparation of the herb Radix Scutellariae, quantification of its major bioactive ingredients, and pharmacological effects of the proposed six bioactive flavones. In addition, this review summarizes the pharmacokinetic profiles of the bioactive flavones reported so far that could be used for further improvement of their pharmacokinetic study. Moreover, due to abundant co-occurring bioactive components in Radix Scutellariae, our review further documents the pharmacokinetic interactions among them.     

Cancer chemopreventive properties of orally bioavailable flavonoids--methylated versus unmethylated flavones

Poor oral bioavailability has been a major limitation for the successful use of dietary flavonoids as cancer chemopreventive agents. In this study, we examined fully methylated flavones as promising improved agents. In the human oral SCC-9 cancer cells, 5,7-dimethoxyflavone and 5,7,4'-trimethoxyflavone were both 10 times more potent inhibitors of cell proliferation (IC(50) values 5-8 microM) than the corresponding unmethylated analogs chrysin and apigenin. Flow cytometry indicated that both methylated flavones arrested the SCC-9 cells in the G1 phase with a concomitant decrease in the S phase, dramatically different from the unmethylated analogs, which promoted G2/M phase arrest. Both methylated compounds inhibited the proliferation of two other cancer cell lines with very little effect on two immortalized normal cell lines. Examination of additional flavone structures indicated that methylated flavones in general have antiproliferative properties. Finally, we demonstrated that 5,7-dimethoxyflavone, in contrast to its unmethylated analog chrysin, was well absorbed and had high oral bioavailability as well as tissue accumulation in vivo in the rat. Thus, fully methylated flavones appear to have great potential as cancer chemopreventive/chemotherapeutic agents, in particular in oral cancer.     

Antifertility principle of Ruta graveolens

Chloroform extracts of the root, stem and leaf of Ruta graveolens L. showed significant anti-fertility activity in rats when administered intragastrically on days 1-10 post-coitum. Fractionation of the extracts led to the isolation of chalepensin as the active component with some toxicity. Time-dosing experiments demonstrated that chalepensin acts at the early stages of pregnancy. It is not clear at this stage if the anti-fertility effect is a direct manifestation of chalepensin toxicity.     

Antifertility activity of striga lutea--Part I

The petroleum ether and chloroform extracts of the whole plant striga lutea have been found to possess significant antifertility activity in mice. Both these extract exhibited complete and partial resorption of implants at a dose of 100 mg/kg and 50 mg/kg body weight, respectively. Histological studies of the uterus and ovary were carried out to confirm the antifertility activity of these extracts.     

双炔失碳酯类似物的结构修饰及抗生育活性

为了探索双炔失碳酯类Ａ－失碳－５ａ－雄甾烷衍生物的结构与抗生育活性的关系。寻找抗早孕有效的甾体化合物，本文设计合成了７个炔氢被氯原子陬代的双炔失碳酯类似物，其结构经元素分析，质谱，红外，核磁共振等确证，小鼠抗早孕试验结果表明，此类化合物的抗早孕活性较双炔失碳酯低，作者对共可能的构效关系进行了分析。     

Antifertility effect of progesterone antibodies in mice

Early embryo development and implantation were arrested in ICR mice which were passively immunized with a mouse monoclonal progesterone antibody given as a single intraperitoneal injection at 12 hrs or 60 hrs post coitum (p.c.). Unimplanted embryos were recovered from the reproductive tract of the antibody-treated mice and none of these progressed to the blastocyst stage. The most pronounced effect was an arrest of embryonic development at a stage prior to cavitation. The plasma progesterone concentration in the blood taken by cardiac puncture increased greatly after the treatment by virtue of high affinity binding by the antibody in circulation. The results showed that passive immunization against progesterone shortly after mating interfered with early hormone dependent steps which were essential for normal embryonic development.     

双炔失碳酯抗生育作用与其雌激素活性的关系

本文证明抗孕53号有降低妊娠大鼠血浆孕酮水平的作用,血浆孕酮水平的下降发生在胎仔死亡前。用去卵巢大鼠,以孕激素维持妊娠,抗孕53号及SIPPR-113的抗孕激素的维持妊娠作用与它们的雌激素活性有密切关系,雌激素活性是这类化合物的抗生育作用的主要但不是唯一因素。     

附睾内注射三羟基丙烷的抗生育作用

将THP直接注入大鼠附睾头部,对其抗生育作用进行了初步研究。于注射后14,30,60及90d分别以鼠数1:1合笼。给药组生育力明显下降,至少持续2个月,3个月后略有恢复趋势。注入THP24,44d,附睾尾部精子数骤减,甚至无精子,90d时部分鼠精子计数恢复至对照水平。放射免疫法测定血清睾酮水平与对照组比较无显著差别。组织学检查可见睾丸形态正常,但附睾头内精子明显减少,出现退行性变化。     

Antifertility and antiproteolytic activity of activated N-carbobenzoxy amino acid esters.

N-Carbobenzoxy L-phenylalanine, glycine, L-leucine, and L-proline derivatives, their vinyl esters, and their 1,2-dibromoethyl esters were tested for antifertility activity in mice. Intraperitoneal administration reduced the pregnancy percentage and the number of fetuses per litter. Intravaginal administration reduced the pregnancy percentage significantly, with N-carbobenzoxyglycine vinly ester, N-carbobenzoxyglycine-1,2-dibromoethyl ester, N-carbobenzoxyl-L-leucine-1,2-dibromoethyl ester, and N-carbobenzoxy-L-proline-1,2-dibromoethyl ester producing 100% inhibition at 10 mg/kg/day. Sperm enzyme hydrolysis of the nonspecific substrate azocasein was inhibited significantly by certain N-carbobenzoxy amino acid esters in vitro. Specific substrate N-benzoyl-L-arginine ethyl ester hydrolysis was also inhibited. Compounds that inhibited N-benzoyl-L-arginine ethyl ester hydrolysis also demonstrated in vivo intravaginal antifertility activity.     

Vascular and anti-oxidant actions of flavonols and flavones

1. Flavonols and flavones are plant-derived polyphenolic compounds that are commonly consumed in the diet. Epidemiological studies indicating that high dietary intake of flavonols reduces the risk of mortality due to coronary heart disease have provoked interest in the mechanism of this cardioprotective effect. 2. We have investigated the structure-activity relationships of a range of flavonols and flavones with regard to their vascular relaxant and anti-oxidant activity. In rat isolated thoracic aorta, the synthetic flavonol 3',4'-dihydroxyflavonol (DiOHF) was found to be a significantly more potent vasorelaxant than the naturally occurring compounds chrysin, apigenin, luteolin, quercetin and fisetin. Similarly, DiOHF was significantly more potent than those compounds in the inhibition of calcium-induced contraction of the rat aorta. 3. 3',4'-Dihydroxyflavonol was also found to significantly inhibit superoxide radical generation in a cell-free system in the presence of xanthine/xanthine oxidase or by rat isolated aorta in the presence of NADPH. In the presence of oxidant stress generated by pyrogallol or xanthine/xanthine oxidase, endothelium-dependent relaxation of rat aortic rings was impaired. 3',4'-Dihydroxyflavonol was able to significantly improve endothelium-dependent relaxation in the presence of those oxygen radical generators. 4. In addition, DiOHF was found to significantly improve dilatation in the rat hindquarters vasculature after exposure to ischaemia and reperfusion. 3',4'-Dihydroxyflavonol was found to be equally effective whether applied before ischaemia or during ischaemia just before reperfusion. 5. In conclusion, DiOHF is an effective vasodilator and anti-oxidant that is able to prevent vascular reperfusion injury. We suggest that DiOHF may be useful as an adjunct to thrombolytic therapy in the management of reperfusion injury.