低场-高场核磁联用分析缔合态对平肺方中芒果苷提取分离的影响

目的采用低场-高场核磁联用技术探索缔合态对平肺方中芒果苷提取、分离行为的影响。方法以1-脱氧野尻毒霉素(DNJ)-柠檬酸成分为对照,以氢T_2弛豫时间及氢化学位移值的变化为指标,采用低场核磁分析缔合态氢的弛豫特征,结合高场核磁技术验证缔合物结构。结果 DNJ-芒果苷在溶液中以缔合态的形式存在,相对分子质量增大,从而抑制了成分从药材向溶液的迁移,透过率下降,图谱中T_2峰向左偏移,高场核磁中化学位移也发生变化。结论阐明了成分存在状态对芒果苷提取分离行为的影响机制,为研究中药复方煎煮方法及机制探索提供了技术支撑。     

Effects of NQO1 deficiency on levels of cyclopurines and other oxidative DNA lesions in liver and kidney of young mice

I-compounds are bulky indigenous DNA adducts that can be detected by (32)P-postlabeling. A subgroup, termed type II I-compounds, represents DNA lesions induced by oxidative stress. Several major type II I-compounds have been identified as dinucleotides containing 3'-terminal 8,5'-cyclo-2'-deoxyadenosine (cA). Levels of type II I-compounds depend on the pro-oxidant status of the cell. For example, enhanced formation of such oxidative DNA lesions in newborn rodents appears to be a consequence of incomplete development of neonatal antioxidant defense systems. We tested the hypothesis that young mice deficient in NAD(P)H:quinone oxidoreductase 1 (NQO1), an antioxidant enzyme catalyzing the detoxification of quinones and their derivatives, show increased formation of these oxidative DNA lesions. Type II I-compound levels were determined by (32)P-postlabeling in liver and kidney DNA of untreated male wild-type or NQO1-null C57BL/6 mice of different ages. NQO1 catalytic activities and contents were measured by spectrophotometric and Western blotting techniques, respectively. Elevated oxidative adduct levels including those containing cA were detected in NQO1-null compared to wild-type mice at 10, 30 and 90 days in liver and at 30 and 90 days in kidney DNA. Furthermore, there were statistically significant inverse relationships between type II I-compound levels and NQO1 activities in wild-type mice up to 30 days of age. Taken together, the results suggest that NQO1 plays an important role in attenuating endogenous oxidative DNA damage in vivo. Our results show also that type II I-compounds represent useful and sensitive biomarkers with utility in studies of oxidative DNA damage and its consequences.     

酮康唑β-环糊精包合物的制备

 目的 探讨应用β-环糊精包合技术提高酮康唑溶解度和稳定性的方法。方法 采用混合搅拌法制备酮康唑β-环糊精包合物,经薄层色谱、X-衍射及差热分析图谱等鉴定,确证为包合物。结果 制备包合物的最佳主客分子摩尔比为1∶1,最佳搅拌时间为5 h,6批包合物包合率在71.59%～73.63%之间。结论 酮康唑β-环糊精包合物可提高酮康唑的溶解度和稳定性。     

中药复方治疗绝经后骨质疏松症的临床研究概况

绝经后骨质疏松症为骨吸收大于骨形成的高转化型代谢性骨病,其并发症严重影响患者的生活水平及质量。中医认为本病与肝、脾、肾脏腑亏虚及血瘀等关系密切。近年来临床研究发现,中药复方治疗绝经后骨质疏松症效果明显,能够有效地改善患者的骨代谢水平,增加患者的骨密度,同时改善患者的临床症状。笔者就中药复方治疗绝经后骨质疏松的作用机制及临床疗效进行综述,旨在为中药复方治疗绝经后骨质疏松症提供数据支持及指导,为今后中药复方开发及靶向治疗绝经后骨质疏松症提供思路。以期指导临床辩证用方,提高对绝经后骨质疏松症的防治率。     

A novel antitumor compound,NC-190, induces topoisomerase II-dependent DNA cleavage and DNA fragmentation

 A novel benzophenazine derivative, NC-190, is a potent antitumor compound. NC-190 has been shown to inhibit the DNA strand-passing activity of DNA topoisomerase II. We investigated further the mode of action of NC-190 against DNA topoisomerase II and DNA fragmentation. NC-190 inhibited the decatenation activity of purified topoisomerase II, but had only a weak inhibitory effect against topoisomerase I. A topoisomerase II-dependent DNA cleavage assay showed that NC-190 inhibited the enzyme activity by stabilizing a topoisomerase II–DNA cleavable complex. NC-190 induced growth inhibition, protein-linked DNA breaks, and DNA fragmentation in cultured HL-60 cells in a dose-dependent manner. These activities of NC-190 in HL-60 cells were comparable to those of etoposide (VP-16). These results demonstrate a good correlation among growth inhibition, topoisomerase II-dependent DNA cleavage, and DNA fragmentation induced by NC-190. A DNA unwinding assay showed that NC-190 had intercalating activity, but its activity appeared to be weaker than those of ethidium bromide and adriamycin. These results indicate that the mechanism by which NC-190 exhibits antitumor activity may be the inhibition of topoisomerase II. Received: 23 September 1994/Accepted: 2 August 1995     

基于中医传承辅助平台挖掘中药复方专利中治疗抑郁的用药规律＊

目的 通过挖掘中药复方专利中治疗抑郁的用药规律,为中药新方研发和临床应用提供参考。方法 登录中国专利公布公告网站,检索治疗抑郁的中药复方专利数据,采用中医传承辅助平台（V2.5）建立数据库,并对其进行频次统计、关联规则、复杂网络及熵层次聚类分析。结果 纳入2003年－2018年治疗抑郁的中药复方专利343项,涉及药物685味,最常用单味药为柴胡,高频药物归经以心、肝两经为主,功效多为安神、补气、活血、理气;最常用药对为白芍-柴胡,最常用角药为当归-白芍-柴胡;置信度最高的关联规则为“甘草,当归,茯苓→柴胡”;核心药物为柴胡、白芍、郁金、茯苓、甘草等; 熵层次聚类分析得到核心组合20个,新处方10首。结论 治疗抑郁的中药复方专利中常见证型为“肝郁脾虚证”,以疏肝解郁健脾为主要治则,同时根据症状辅以安神、益气、理气、活血、燥湿、清热等治法,多以逍遥散为基础方,常配伍心、肝两经药。     

眼底激光联合复方樟柳碱治疗视网膜静脉阻塞的临床观察

目的:比较单独眼底激光(半导体激光或多波长氪离子激光)以及联用复方樟柳碱治疗视网膜静脉阻塞的临床疗效。方法:采用半导体激光及多波长氪离子激光对43例43眼视网膜静脉阻塞的患者,根据病变的性质、部位和屈光间质情况选择不同种类及波长激光进行局部或全视网膜光凝,部分有条件的患者同时接受患侧眼颞浅动脉旁皮下注射复方樟柳碱3～4个疗程,术前进行视力、裂隙灯、眼底和眼底荧光血管造影检查,术后随访期至少3mo。结果:所有患者中,眼底荧光血管造影证实70%(30/43)病情明显好转,29例视力提高;眼底激光联用复方樟柳碱治疗组患者视力提高率(75%)好于单独眼底激光治疗组(58%)。其间未见严重并发症。结论:眼底激光联用复方樟柳碱治疗能够更好改善或保存视网膜静脉阻塞患者的视力。     

血管交联剂预处理异体颈静脉重建大鼠腹主动脉

目的 评估新型血管交联剂－－多聚环氧化合物（ｐｏｌｙｅｐｏｘｙ ｃｏｍｐｏｕｎｄ，ＰＣ）的应用价值。方法 分别用ＰＣ和传统交联剂戊二醛（ｇｌｕｔａｒａｌｄｅｈｙｄｅ，ＧＡ）对取自ＤＳ大鼠的颈静脉进行预处理，并移植于同种大鼠的肾下腹主动脉，观察两种静脉植入动脉环境报的组织学变化。结果 两种静脉植入动脉环境后通畅率无统计学差异（Ｐ〉０．０５）；ＰＣ组的瘤样扩张率低于ＧＡ组（Ｐ〈０．０５）；两组内膜愈合     

中药口腔溃疡复合膜的研制

中药口腔溃疡复合膜为一中药新剂型,由药膜与覆盖膜构成。对不同配方和材料的成膜性,粘附性及释药性的比较表明,以PVA_17-88-CMCNa(1:1)为药膜基质,PVA_17-88为覆盖膜材料较为理想。     

高血压病患者红细胞钠离子转运及其对降压的反应

本文观察了高血压病(EH)患者的红细胞钠离子转运和血浆内源性类洋地黄物质(EDLC)的变化及硝苯啶和哌唑嗪对其影响,结果:EH患者红细胞的钠泵功能和Na~+-K~+内向协同转运明显低于正常,血浆EDLC显著升高,但其与钠泵非平行改变。经降压治疗,EH患者的钠泵和EDLC明显改善。本文对钠离子转运与EH的关系,及降压药物对其作用作了初步探讨。