豚鼠外周血淋巴细胞β肾上腺素能受体系统在实验性过敏性哮喘时的动态变化及相互关系(摘要)

哮喘是一种常见病,阐明其发病机理具有重要的意义。目前,关于哮喘豚鼠外周血淋巴细胞β肾上腺素能受体(β受体)的动态变化,在国内外尚未见报道。本研究采用放射配基结合法,结合测定淋巴细     

~(14)C-棉酚在大鼠睾丸亚细胞组分中的定量分布及作用位点的研究

~(14)C-棉酚在大鼠睾丸五种亚细胞组分中,以线粒体中含量最高,放射活性较其他组分高2～3倍,差别显著。~(14)C-棉酚和~3H-哇巴因双标记实验也表明,双标记的放射活性高峰均集中于线粒体,其次为细胞膜。这二种细胞组分的~(14)C和~3H放射活性均分别较其他组分高,差异显著。这有力地支持线粒体蛋白质容易与解偶联物质结合的论点,并为线粒体是棉酚的敏感靶子细胞器以及棉酚通过干扰线粒体功能而中断精子发生过程的假说提供了直接证据。     

棉酚对大鼠支持细胞蛋白质合成的影响

本文以同位素放射自显影方法测定了棉酚对大鼠支持细胞(sertoli cell)蛋白质合成过程中亮氨酸参入活动的影响。实验组及对照组各有大鼠20及10只,实验组取醋酸棉酚(30mg/kg/d)以混悬液灌服,服药第 4及 6周各取实验及对照10及 5只,断头处死并取睾丸分离培养支持细胞,对照组培养液内分别加入棉酚0、2、5、8μg/ml,取培养96小时已成单层的各组细胞(以不加棉酚组为对照),分别测定各组细胞~(14)C-亮氨酸放射自显影结果。结     

豚鼠外周血淋巴细胞β肾上腺素能受体的检测

本实验对放射配基结合法进行改良,检测了外周血淋巴细胞β受体,并证实了淋巴细胞β受体为β_2型。用本法测定的结果稳定、可靠、简便易行,便于临床推广应用。     

~(14)C-醋酸棉酚在大鼠睾丸中亚细胞定位的电镜放射自显影研究(摘要)

<正> 棉酚的抗精子作用,在细胞水平上是以变态期精子细胞和中、晚期精母细胞受损而实现的,而在亚细胞水平上则以线粒体损伤最剧。放射化学研究表明,~(14)C-棉酚在大鼠睾丸5种亚细胞组分中以线粒体含量最高。本研究旨在以电镜放射自显影技术探讨棉酚的亚细胞作用位点,进一步阐明棉酚的生物学作用机理。     

前列腺增生症患者血清性激素结合球蛋白结合容量的改变

作者应用放射配基结合分析法测定了良性前列腺增生症(BPH)患者及不同年龄健康男性血清性激素结合球蛋白(SHBG)结合容量。结果发现 BPH 组短程乙烯雌酚(DES)治疗前后自身配对 SHBG 结合容量差值     

过敏性哮喘豚鼠肺组织β受体和cAMP—PDE活力的变化

本实验采取放射配基结合法、放射酶测定法和放射免疫法观察了过敏性哮喘豚鼠肺组织β受体、cAMP-PDE活力和cAMP的变化。哮喘组与对照组比较:肺组织细胞膜β受体减少25％,肺组织cAMP下降36％,而cAMP-PDE活力上升35％,相关分析表明肺组织cAMP与β受体呈正相关,与cAMP-PDE呈负相关。     

~(14)C—醋酸棉酚在大鼠体内代谢的研究

(一)大鼠内分布、定位的整体及组织放射自显影的动态观察(摘要)以~(14)C 标记的醋酸棉酚喂饲成年雄性大鼠,一次口服组的剂量为94微居里/35毫克/动物;累加服药(每日连续口服)组为4.45微居里/日/动物。分别于服药后不同时期取材制成整体及组织放射自显片。追踪标记棉酚在体内各脏器和组织中的吸收、分布和累积的定位变化动态。相应的组织切片用 H·E 染色,作细胞病理观察。结果摘述如下:     

醋酸棉酚对大鼠肾脏的影响

棉酚在临床上引起低血钾的原因是肾性失钾,但其作用于肾脏的哪个环节还不清楚,作者就此问题进行探索. 体外实验表明.醋酸棉酚(GAA)可引起肾微粒体超氧自由基(O_2~-)生成.GAA浓度小于0.1mmol/L时,O_2~-的生成量与药物浓度呈明显的剂量反应关系;而GAA浓度大于0.1mmol/L时,O_2~-的生成量趋于平稳,呈饱和现象.GAA可与肾线粒体、细胞膜和微粒体发生不可逆结合,其结合率占总放射量的     

L-型钙通道在急性脑缺血和再灌流时的作用

应用新型钙离子荧光指标剂 Fura-2/AM 测定海马突触体内游离钙离子浓度在脑缺血及再灌注时的变化规律,并应用[~3H]PN200—110作为放射性配基,尼莫地平为非标记化合物,放射配体结合法测定了海马组织 L—型钙通道生物学特性。结果显示:大鼠脑缺血及再灌注后,海马脑区突触体内游离 Ca~(2+)浓度显著增加,其 L—型钙通道的 B_(max)和 Kd 值均显著上升,与对照组相比相差十分显著。说明游离 Ca~(2+)浓度的增加参与了脑缺血损伤,其中 L-型钙通道的开放数多,是 Ca~(2+)超载产生的原因之一。     

醋酸棉酚诱导鼠前列腺癌细胞凋亡的研究

目的研究醋酸棉酚对鼠前列腺癌RM-1细胞的抑制作用和诱导凋亡作用,探讨其作用机制。方法将不同浓度的醋酸棉酚作用于鼠前列腺癌RM-1细胞,利用MTT法检测其有效作用浓度,分别采用电子显微镜及流式细胞仪观察和检测RM-1细胞凋亡和bax蛋白表达情况,RT-PCR检测mRNA表达水平变化。结果MTT法测得其IC50值为34.56mg／L,浓度为30mg／L的醋酸棉酚具有诱导鼠前列腺癌RM-1细胞凋亡的作用,且随药物作用时间的延长,凋亡率逐渐增加,同时bax蛋白表达也逐渐增加;RT-PCR显示bax-mRNA水平逐渐升高。结论醋酸棉酚能诱导鼠前列腺癌细胞凋亡,其作用机制之一是上调bax-mRNA水平、增加bax蛋白表达,且具有时间依赖性。     

棉酚（—,＋,＋）对佛波酯和A23187刺激巨噬细胞前列腺...

Previously, gossypol was found to have a wide range of cellular effects. In the present study, the effects of racemic, (-) and (+) gossypol on prostaglandin synthesis by mouse peritoneal macrophages were examined. The synthesis of prostacyclin, thromboxane A2 and prostaglandin F2 alpha was stimulated by phorbol-12-myristate-13-acetate (PMA), A23187 and arachidonic acid. Racemic, (-) and (+) gossypol dose-dependently inhibited PMA or A23187-stimulated prostaglandin synthesis, but failed to affect arachidonic acid stimulated prostaglandin synthesis. It is therefore possible that both (-) gossypol and (+) gossypol inhibit prostaglandin synthesis at the level of arachidonic acid release. Our studies point out two possibilities: 1) the inhibition of (+) and (-) gossypol on prostaglandin synthesis may not be the main mode of the contraceptive action of gossypol; 2) (+) gossypol, which also inhibits prostaglandin synthesis, may have antifertility effects.     

棉酚对纯化LDH-X作用的分析

用纯化的大鼠LDH-X和LDH 1～5,以定量测定酶活性和凝胶电泳相配合的分析方法,发现棉酚对LDH-X的抑制作用显著大于LDH1～5,与在人体内的试验结果基本一致,再次证实了棉酚对LDH-X的抑制有特异性,进一步明确通过抑制精子特异的LDH-X酶,中断 精子的能量供给,损害线粒体功能,阻断生精过程是棉酚抗生育作用机理的一个重要方面。     

棉酚金刚烷胺Schiff碱的合成、光谱分析及PM6半经典计算

目的解析棉酚金刚烷胺Schiff碱的结构。方法制备棉酚金刚烷胺Schiff碱,并采用红外光谱,二维核磁波谱技术和PM6半经典计算方法对其结构进行分析。结果光谱分析表明棉酚金刚烷胺Schiff碱具有烯胺-烯胺结构特征并归属了所有的碳原子和氢质子的化学位移;PM6研究表明棉酚金刚烷胺Schiff碱的烯胺-烯胺和亚胺-亚胺构型的生成热分别为-1160.00kJ.mol^-1和-1008.319kJ.moL^-1,其烯胺-烯胺构型在能量上更有利。结论棉酚金刚烷胺Schiff碱以烯胺-烯胺形式存在,分子内氢键的存在使烯胺-烯胺结构更稳定。     

2种甘氨酸棉酚Schiff碱的光谱分析及PM6半经典计算研究

目的 解析2种甘氨酸棉酚Schiff碱的结构及优势构象.方法 制备2种甘氨酸棉酚Schiff碱,并采用红外光谱、二维核磁波谱技术和PM6半经典计算方法进行结构解析.结果 光谱分析表明2种甘氨酸棉酚Schiff碱具有烯胺-烯胺结构特征,并归属了所有的碳原子和氢原子的化学位移;PM6研究表明2种甘氨酸棉酚衍生物以烯胺-烯胺构型存在,在能量上更有利,并确定了优势构象.结论 2种甘氨酸棉酚Schiff碱均以烯胺-烯胺形式存在,分子内氢键使烯胺-烯胺结构更稳定.     

醋酸棉酚对Raji细胞增殖和凋亡的影响

目的 观察醋酸棉酚对人Burkitt淋巴瘤细胞株Raji细胞增殖和凋亡的影响.方法 采用台盼蓝染色和噻唑蓝(MTT)法观察醋酸棉酚对Raji细胞生长存活的影响,瑞氏染色法观察药物处理后细胞形态学变化,琼脂糖凝胶电泳和Annexin V-FITC标记流式细胞仪检测细胞凋亡,流式细胞仪分析细胞周期、检测细胞凋亡率及Bcl-2蛋白表达水平变化,比色法测定Raji细胞Caspase-3样蛋白酶活性.结果 5 μmol/L以上浓度醋酸棉酚能抑制Raji细胞生长增殖并诱导其凋亡,效应与药物浓度及给药时间呈正相关.醋酸棉酚作用后,Raji细胞被阻滞于G_0/G_1期.比色法显示Caspase-3样蛋白酶活化.流式细胞仪检测到Bcl-2蛋白表达下调,且与Caspase-3活化在时间上存在同步趋势.结论 醋酸棉酚能抑制aaji细胞增殖并诱导凋亡,其原因可能与调节细胞周期及下调Bcl-2蛋白表达有关.     

如何降低食用棉子油中棉酚的含量

目的:为了有效地提取棉籽中有毒物棉酚.方法:采用萃取法且加以碱洗可提取棉酚.结果:此法可得到较高产率、高质量的食用棉子油.结论:工艺较简单,效果好,宜于推广应用.     

棉酚及其衍生物抗肿瘤机制的研究进展

棉酚具有多种药理活性,近年来其抗肿瘤作用越来越受到重视。棉酚的抗肿瘤机制尚未完全明确,通过体外和动物实验及一些初步的临床试验证实,棉酚的抗肿瘤机制有线粒体途径、调控细胞的周期蛋白、抑制Bcl-2蛋白的过度表达。亦有研究表明棉酚可以通过使高甲基化的抑癌基因去甲基化达到抗肿瘤作用。     

Clinical effects and experimental study on gossypol in endometriosis

Effects of the gossypol on endometriosis in 12 cases of control were observed. The results showed that the gossypol administered orally was effective in endometriosis patients. The basal body temperature changed from biophase to monophase. Dysmenorrhea disappeared in 11/12 patients. Amenorrhea occurred in 10/12 patients and the ovarian endometrial cyst was shrinkable. Serum progesterone and estradiol were decreased after gossypol administration, but follicle-stimulating hormone and luteinizing hormone were increased evidently. Histochemical and cytochemical observations revealed that the activity of acid phosphate (ACP), nonspecific esterase (NSE) and alkaline phosphate (AKP) in both aberrant uterine endometrium and uterine endometrium in situ were decreased evidently. The above results suggest that the satisfactory therapeutic effect of gossypol on endometriosis may be due to not only the indirect but also the direct action on uterine endometrium.     

Drug synergistic antifertility effect of combined administration of low-dose gossypol with steroid hormones in rats

Background Our previous studies suggested that low-dose gossypol combined with steroid hormones has a reversible antifertility role in adult male rats, and the course of treatment was shorter than that of either gossypol or steroid hormones alone. This result suggested that low-dose gossypol and steroid hormones have a drug synergistic effect on antifertility. The aim of the study was to find the target organs of the antifertility synergistic effect of the combined regimen.Methods Thirty-two adult male rats were divided into four groups randomly: group GH, rats were fed orally with group H, the same dosage of DSG/EE/TU as in group GH were administered; group C, rats were treated with vehicle (1% methyl cellulose) as control. Testes and epididymis were removed at 8 weeks post-treatment for evaluating their weight,volumes, volume fraction, and total volume of testicular tissue structures and the seminiferous tubule diameter using stereological assay. Sperm cell numbers and the motility of epididymal sperm were quantitated by flow cytometry and morphological methods.Results Compared with group C, spermatogenesis was normal in group G and suppressed in groups H and GH.Similar changes of testicular tissue structures and sperm number were found in groups H and GH. The decreases of epididymal sperm number and motility in group GH were greater than that of the low-dose gossypol or steroid hormones alone group.Conclusions The suppression of spermatogenesis was induced by steroid hormones in the combined regimen, and the epididymis was the target organ of low-dose gossypol. Combined use of low-dose gossypol and steroid hormones played a comprehensive antifertility role in their synergistic effect on reducing the number and motility of epididymal sperm.