共查询到18条相似文献,搜索用时 62 毫秒
1.
Racemic, (-) and (+) gossypol, provided by the Department of Organic Chemistry of our institute, was suspended in 2.5% tween 80 solution. Adult male Wistar rats 190~220 g in weight were allotted to 5 groups. Animals in group 1 received 2.5% tween 80 solution as control. Rats in group 2 were treated with racemic gossypol at the dosage of 30 mg/kg for 2 weeks. Animals in group 3 and 4 were given 15 mg/kg of (-) gossypol for 2 weeks and 30 mg/kg of (-) gossypol for 1 week respectively. Rats in group 5 were treated with (+) gossypol at the dosage of 30 mg/kg for 2 weeks.Four weeks from the beginning of gossypol treatment the rats were cohabited with adult females for 7 days. Then the motility of the sperms in the cauda epididymides was estimated The female rats were examined for pregnancy 7 days later.Treatment with (-) gossypol at 30 mg/kg caused significant decreases in body weight of the rats (P<0.05). One of the five rats died 7 days after the last administration, while (+) gossypol and racemic gossypol at the dosage employed had no effect on the body weight. (+) Gossypol at 30 mg/kg for 2 weeks had no effect on the motility of the sperms in the cauda epididymides and no effect on the fertility of the animals: nor was there any effect on the weights of the testis, epididymis, prostate and seminal vesicle. The sperms of the cauda epididymides were found to be dead in the groups treated with 15 and 30 mg/kg of (-)gossypol. Raccmic gossypol given for 2 weeks at 30 mg/kg caused loss of fertility of the male rats which confirmed our previous findings.(?)t may be postulated that (+) gossypol has no antifertility effect nor toxicity at the dosage employed. (-) Gossypol is the active stereoisomer of racemic gossypol. 相似文献
2.
3.
4.
5.
6.
一苯胺棉酚—棉酚中的一种杂质 总被引:1,自引:0,他引:1
本文介绍了棉酚中的一种杂质(苯胺法精制)一苯胺棉酚的研究。该化合物文献中未见报道。实验数据符合组成式C38H35O7N;质谱分子离子峰593,紫外光谱于439~440 nm有最大吸收(E1com1% 329±6 CHCl3);红外光谱在1610 cm-1有醛基和1590 cm-1碳氮吸收峰;核磁共振谱表明有—CHO和—HC=N质子峰,其峰面积比为1:1;熔点272~275℃(分解);硅胶薄层上Rf值界于二苯胺棉酚和棉酚之间。一苯胺棉酚的存在,干扰分光光度法测定棉酚含量的准确性。利用薄层层析法可检查棉酚中一苯胺棉酚的存在与否。本文还介绍了一苯胺棉酚的合成方法。 相似文献
7.
8.
9.
10.
11.
Wen Yan-Dong Remmel Rory P. Pham Phuong T. Vince Robert Zimmerman Cheryl L. 《Pharmaceutical research》1995,12(6):911-915
Purpose. Evaluate the ability of (-)-6-aminocarbovir ((-)-6AC) to improve the CNS exposure to (-)-carbovir ((-)-CBV).
Methods. Activation of (-)-6AC in vitro was assessed by incubations of rat brain tissue homogenates. The in vivo brain exposure to (-)-CBV was then examined in rats after iv infusions of either (-)-CBV (n = 4) or (-)-6AC (n = 5). The drugs were infused to steady-state via the jugular vein. At the end of the infusion, a bolus of [3H]inulin was injected via the femoral vein in order to obtain an estimate of the brain vascular space.
Results. (-)-6AC was converted to (-)-CBV by incubations of rat brain tissue homogenates. After iv infusion of (-)-CBV, the brain/ blood concentration ratio of (-)-CBV was 0.032 ± 0.009. The brain/ blood concentration ratio of (-)-CBV after iv infusion of (-)-6AC was 0.080 ± 0.020.
Conclusions. (-)-6AC improved the brain delivery of (-)-CBV, although the absolute exposure of the brain tissue to (-)-CBV was still quite low. 相似文献
12.
目的采用HPLC法测定(S)-4-苯基-2-噁唑烷酮(SPO)的纯度。方法采用Welchrom C18色谱柱,流动相为0.02 mol·L-1磷酸二氢钾(KOH调p H5)-乙腈(60∶40),检测波长210 nm,流速1.0 m L·min-1,柱温35℃。结果 SPO0.3036~6.072μg·m L-1与峰面积的线性关系良好(r=0.9999),检测限和定量限分别为0.9099、3.033 ng。结论所用方法准确、灵敏、快速,适用于检测SPO中的微量杂质。 相似文献
13.
The group of Prof. Yanxing Jia have realized the first total synthesis of natural product (-)-glaucocalyxin A 下载免费PDF全文
Shuxiang Song 《中国药学》2020,29(6):439
The group of Prof. Yanxing Jia have realized the first total synthesis of natural product (-)-glaucocalyxin A. 相似文献
14.
酞丁安对映体合成及其抗单纯疱疹病毒活性评价 总被引:1,自引:0,他引:1
酞丁安(3-酞酰亚胺-2-氧-正丁醛双缩氨硫脲,TDA)是药物研究所创制的抗病毒新药。为了研究其对映异构体(R),(S)-TDA对病毒活性及毒性是否有差异,并与消旋酞丁安(RS)-TDA的抗病毒活性及毒性进行比较,本文分别用已知构型的(R)-与(S)-丙氨酸为原料,通过缩合等6步反应,得到光学活性的(R)-,(S)-TDA,并与外消旋酞丁安比较其抗病毒活性及毒性。三者的抗单纯疱疹病毒活性与对细胞的毒性差别不大,说明消旋酞丁安临床使用是安全有效的。 相似文献
15.
甘草中三萜皂甙元的分离和结构鉴定 总被引:7,自引:0,他引:7
自乌拉尔甘草(Glycyrrhiza uralensis Fisch)根茎中提取出粗皂甙。经盐酸甲醇水解反应,柱层分离,共分离出七个皂甙元,其中四个化合物经化学方法和光谱解析,分别鉴定为甘草次酸甲酯(A),甘草内酯(c),3β,24-二羟基齐墩果-11,13(18)-二烯-30羧酸甲酯(D),24-羟基甘草次酸甲酯(F),化合物C系首次得自乌拉尔甘草中。化合物G的结构经测定为24-羟基甘草内酯,尚未见文献报道。本文报道新成分24-羟基甘草内酯的结构测定工作以及四个已知化合物的鉴定。 相似文献
16.
17.
18.
The reversal effects of piperine and (R)-(+)-citronellal on multidrug resistant breast cancer cells 下载免费PDF全文
Multidrug resistance (MDR) in tumor cells can reduce the efficacy of chemotherapy. Overexpression of transporters is an important mechanism for MDR. P-glycoprotein (P-gp) is an ATP-binding cassette transporter frequently expressed in multidrugresistant tumor cells, inducing MDR. To reverse P-gp dependent MDR, anticancer drugs can be administered with P-gp inhibitors. Piperine and (R)-(+)-citronellal both are P-gp inhibitors from dietary sources. In the present study, we aimed to evaluate the MDR reversal effects of piperine and (R)-(+)-citronellal in multidrug resistant MCF-7/DOX cells. The results of cytotoxicity studies indicated that piperine and (R)-(+)-citronellal both could abate the resistance of MCF-7/DOX after 72-h incubation. After 72-h incubation, piperine could dose-dependently down-regulate the MDR1 expression at the mRNA level, while (R)-(+)-citronellal had no effect on the MDR1 expression. Therefore, piperine and (R)-(+)-citronellal both could reverse MDR in MCF-7/DOX cells, and the reversal effect of piperine was related to dose-dependent down-regulation of the MDR1 expression at the mRNA level. 相似文献