汉防己甲素和长春新碱对人视网膜母细胞瘤细胞系HXO－Rb_（44）生长的抑制作用

用汉防己甲素（ｔｅｔｒａｎｄｒｉｎｅ，ＴＤＲ）、长春新碱（ｒｉｎｃｒｉｓｌｉｎｅ，ＶＣＲ）分别对人视网膜母细胞瘤细胞系ＨＸＯ－Ｒｂ＿（４４）生长的影响进行观察，结果显示：ＴＤＲ在１～４０μｇ／ｍｌ范围内对ＨＸＯ－Ｒｂ＿（４４）细胞有明显抑制作用（Ｐ＜０．０５），半数抑制浓度ＩＣ５０为２．４５μｇ／ｍｌ；ＶＣＲ对该细胞系也有较强的抑制作用，ＩＣ５０为０．３１μｇ／ｍｌ。提示ＴＤＲ与ＶＣＷ一样，在体外对Ｒｂ细胞有较强的抑制作用，可能成为治疗视网膜母细胞瘤的新药。     

雷公藤多甙对男子尿β2－微球蛋白的影响

 本研究对１２名３５～４０岁的男性轻型银屑病患者，每日口服雷公藤多甙２０ｇ（抗生育有效剂量，为临床常用剂量的１／３～１／４）。在用药前、用药３个月及停药后３个月采集尿液标本，用酶－免疫法测定尿液β＿２－微球蛋白的含量。结果表明：用药前尿β＿２－微球蛋白的含量平均为１４２．１±６．４μｇ／Ｌ，用药３个月尿β＿２－微球蛋白的平均含量为３３７．３±９．８μｇ／Ｌ，比用药前明显升高（Ｐ＜０．０５）。停药后３个月尿凡．檄球蛋白的平均含量为３４３．６±８．４μｇ／Ｌ，同用药３个月相比，差异无显著性意义（Ｐ＞０．０５），与用药前相比，差异有显著性意义（Ｐ＜０．０５）。     

雷公藤多甙对男子尿β＿2－微球蛋白的影响

本研究对１２名３５～４０岁的男性轻型银屑病患者，每日口服雷公藤多甙２０ｇ（抗生育有效剂量，为临床常用剂量的１／３～１／４）。在用药前、用药３个月及停药后３个月采集尿液标本，用酶－免疫法测定尿液β＿２－微球蛋白的含量。结果表明：用药前尿β＿２－微球蛋白的含量平均为１４２．１±６．４μｇ／Ｌ，用药３个月尿β＿２－微球蛋白的平均含量为３３７．３±９．８μｇ／Ｌ，比用药前明显升高（Ｐ＜０．０５）。停药后３个月尿凡．檄球蛋白的平均含量为３４３．６±８．４μｇ／Ｌ，同用药３个月相比，差异无显著性意义（Ｐ＞０．０５），与用药前相比，差异有显著性意义（Ｐ＜０．０５）。     

哌拉西林在胆道手术患者药代动力学的研究

本文研究了哌拉西林（ｐｉｐｅｒａｃｉｌｌｉｎ，ＰＩＰ）在８例施各类胆道手术附Ｔ型管引流患者的药代动力学，采用ＡＶＡＮＴＡＧＥ全能自动化微生物分析仪测定血清及胆汁哌拉西林浓度。结果表明，静滴哌拉西林３ｇ或２ｇ后即刻血药浓度分别可达到３２２．７±２８．４和２０４．５±１６．２μｇ／ｍｌ，８ｈ后仍保持７．４±３．０和１．８±０．７μｇ／ｍｌ；Ｔ型管胆汁药物峰浓度可达到２０７．９±８３．６和１４４．７±６．６μｇ／ｍｌ，达峰时间约２ｈ左右。该药体内在观分布容积大于血容量，提示体内分布广泛，因静滴哌拉西林后血药及胆药浓度均较高，故适用于防治胆道感染。     

定量PCR检测黄芪A6组分与无环鸟苷联合抗1型单纯疱疹病毒的协同作用

目的：探讨抗疱疹病毒药物黄芪Ａ６组分（Ａ６）和无环鸟苷（ＡＣＶ）联合抗１型单纯疱疹病毒（ＨＳＶ１）的作用机制。方法：利用竞争ＰＣＲ检测Ａ６和ＡＣＶ联合抗ＨＳＶ１的协同作用，并与细胞病变（ＣＰＥ０抑制法进行比较。结果：竞争ＰＣＲ测定Ａ６、ＡＣＶ和Ａ６＿ＡＣＶ对ＨＳＶ１的最小抑制浓度（ＭＩＣ）分别为１．８８ｍｇ／ｍｌ、３．３７μｇ／ｍｌ、３．３７μｇ／ｍｌ和０．４７ｍｇ／ｍｌ＋０．８４μｇ／ｍｌ；ＣＰ     

自拟方配合联苯双酯治疗慢性乙型肝炎96例

目的：观察自拟方配合联苯双酯治疗慢性乙型肝炎临床疗效。方法：以自拟方配合联苯双酯治疗慢性乙型肝炎９６例,另以联苯双酯、云芝多糖、ＶｉｔＣ等治疗９０例作对照,２组均以３０ｄ为１疗程,治疗２～３疗程观察疗效。结果：治疗组有效率为９４．８％,明显优于对照组６２．２％（Ｐ〈０．０１）;且２组在ＨＢｅＡｇ、ＨＢＶ－ＤＮＡ阴转率比较上也有显著差异（Ｐ〈０．０５）。结论：自拟方配合联苯双酯治疗慢性乙型肝炎疗效肯     

穴位注射治疗小儿遗尿症

穴位注射治疗小儿遗尿症取穴：肾俞，直刺１～１．５寸；膀胱俞，直刺０．５～１寸；灸三焦俞、中极。药物：维生素Ｂ＿（１２）１００～２５０μｇ。方法：备２ｍｌ无菌注射器一具，５～６号针头１个。抽取维生素Ｂ＿（１２）１００～２５０μｇ。按常规消毒皮肤，于肾俞...     

中国中医研究院中药研究所

大黄乙醇提取物的细胞毒性极低，２００００μｇ／ｍｌ未见细胞毒性，反而能促进细胞生长；在细胞培养上有明显的抗病毒作用，对单纯疱疹病毒（ＨＳＶ）的有效抑制浓度为１００μｇ／ｍｌ，并对ＨＳＶ的感染有预防作用和对病毒颗粒有直接杀伤作用。     

HPLC测定前列腺中依诺沙星含量及药动学研究

 采用高效液相色谱法，对前列腺中依诺沙星的测定和药动学进行了研究。固定相：Ｓｈｉｍａｄｚ－ＯＤＳ柱，流动相：甲醇－乙腈－０．１ｍｏｌ／Ｌ柠檬殴（４．５：１：９），检测器：ＳＰＤ－６ＡＶ，检测波长：２７２ｎｍ，流速：１．５ｍｌ／ｍｉｎ，标准曲线线性范围：０．５～５μｇ／ｍｌ，ｒ＝０．９９９６，平均回收率为９８．８％，ＲＳＤ为０．７％，用３Ｐ８７实用药代动力学程序进行数据处理，在前列腺中各药代动力学参数Ｔ＿（１／２Ｋｅ），Ｔ＿（ｐ，ｃ＿（ｍａｘ）），ＡＵＣ，Ｃｌ／Ｆ（ｓ）和Ｖｃ／Ｆ（ｃ）分别为２．２３ｈ，２．３７ｈ，７．４３μｇ／ｍｌ，３９．４７（ｈ·μｇ）／ｍｌ，１．２７Ｌ／（ｋｇ·ｈ）和４．０７Ｌ／ｋｇ，结果表明，依诺沙星很容易透渗到前列腺组织中去，前列腺药物浓度很高，为临床应用依诺沙星治疗前列腺炎提供了理论依据。     

RP－HPLC分析白花前胡根和茎叶中花椒毒素的含量

建立了ＲＰ－ＨＰＬＣ分离和测定白花前胡根和茎叶中活性成分花椒毒素含量的方法，采用Ｃ＿（１８）柱，甲醇－水（６５：３５）为流动相，ＵＶ检测波长为２９７ｎｍ，花椒毒素在浓度为１～４μｇ／ｍｌ范围内（进样１μｌ），进样浓度（μｇ／ｍｌ）与峰面积呈直线相关，回归方程Ａ＝－０．１４１×１０￣３＋２．６１６×１０￣３Ｘ，ｒ＝０．９９９８。回收率为９９．９％，ＲＳＤ为０．６８％（ｎ＝５）。该方法步骤简便，重现性好，结果准确，分析速度快，可望成为分析白花前胡根和茎叶中花椒毒素含量的常规方法。     

Activation of lucidin-3-O-primveroside mutagenicity by hesperidinase

At the maximum dose tested, 100 μg/plate, lucidin-3-O-primveroside (LUC-Prv) exhibited mutagenic potential in Salmonella typhimurium TA100 without S9 mix but not with the addition of this preparation. When the pH of the tested system was reduced from 7.4 to 6.5, the same results were obtained. However, after hesperidinase treatment at pH 6.5, higher mutagenicity was demonstrated, and the mutagenicity of the hydrolysis product in TA100 decreased in the presence of S9 mix. When the preincubation time of the mixture was kept longer, i.e. 30, 60 and 120 min, the number of revertants in TA100 without S9 mix became higher. When the concentration of hesperidinase was varied from 5 × 10^?5 to 2.5 × 10^?2 unit, no change in the number of revertants was observed. In contrast, LUC-Prv and its hydrolysis products demonstrated no mutagenicity in TA98 by the same tested system.     

The antimutagenic effect of mistletoe lectin (Viscum album L. var. coloratum agglutinin)

A galactose- and N-acetyl-D-galactosamine-specific lectin (Viscum album L. var. coloratum agglutinin, VCA), which is known for its anticancer activity, was isolated from mistletoe. In this study, we investigated the antimutagenic potentials of VCA by using the pre-incubation method of the Ames test (Salmonella typhimurium TA98 and TA100) in the presence or absence of S9 mixture. Viscum album L. var. coloratum agglutinin was assessed for its antimutagenic properties against the mutagens 2-aminoanthracene (2AA) and furylfuramide (AF-2) for strain TA98, and sodium azide (NaN(3) ) and 2-aminoanthracene (2AA) for strain TA100. The concentrations used for this test compound were 100, 200 and 400 μg per plate. Viscum album L. var. coloratum agglutinin showed moderate, but not negligible, protective effects regarding the antimutagenic properties against the direct-acting mutagens NaN(3) and AF-2. Furthermore, VCA was more effective in preventing the mutagenicity of the indirect-acting mutagen 2-AA (in the presence of S9) when tested with both TA98 and TA100. In conclusion, this report has shown broad ranging antimutagenic effects of VCA to numerous mutagens in TA98 and TA100 Salmonella typhimurium strains. Although the data presented here cannot be applied in vivo, they can support other antimutagenic and anticarcinogenic findings for VCA.     

Assessment of mutagenicity in Parthenium hysterophorus L

The mutagenic potential of a crude extract of Parthenium hysterophorus L. was assessed in the Salmonella/microsome (Ames) assay and the mouse bone marrow micronucleus test. Results in the bacterial mutagenicity assay were negative for the five strains employed, e.g. TA 1535, TA1537, TA 98, TA 100 and TA 102, while cytotoxicity was evident in all cases at 5000 microg per plate, the highest concentration assayed. A decrease in toxicity was observed with exogenous mammalian metabolic activation (S9) or glutathione (5 micromol per plate). When mutagenicity was monitored after column chromatography fractionation of the crude, fraction 1 was mutagenic in strain TA 98 (+S9). Besides, cytotoxicity was found in fraction 5, where parthenin was eluted. The micronucleus test was negative in mice upon oral administration, at doses up to 96 mg of crude per kg. Bone marrow toxicity was not observed. The crude extract exhibited some in vitro pro-oxidant activity. It also inhibited lipid peroxidation (IC(50)=4.1 microg/ml) but failed to act as .OH scavenger.     

Mutagenic and antimutagenic activities of aqueous and methanol extracts of Euphorbia hirta

Euphorbia hirta (E. hirta) is a weed commonly found in tropical countries and has been used traditionally for asthma, bronchitis and conjunctivitis. However, one of the constituents in this plant, quercetin, was previously reported to be mutagenic. This work aimed to determine the level of quercetin in the aqueous and methanol plant extracts and to investigate the mutagenic effects of quercetin and the extracts in the Ames test utilising the mutant Salmonella typhimurium TA98 and TA100 strains. The antimutagenic activity of Euphorbia hirta aqueous and methanol extracts was also studied in Salmonella typhimurium TA98. HPLC analyses showed that quercetin and rutin, a glycosidic form of quercetin, were present in the acid-hydrolysed methanol extract and non-hydrolysed methanol extract respectively. The quercetin concentration was negligible in both non-hydrolysed and acid-hydrolysed aqueous extracts. The total phenolic contents in Euphorbia hirta were determined to be 268 and 93 mg gallic acid equivalent (GAE) per gram of aqueous and methanol extracts, respectively. Quercetin (25 μg/mL) was found to be strongly mutagenic in Salmonella typhimurium TA98 in the absence and presence of S-9 metabolic activation. However, both the aqueous and methanol extracts did not demonstrate any mutagenic properties when tested with Salmonella typhimurium TA98 and TA100 strains at concentrations up to 100 μg/mL in the absence and presence of S-9 metabolic activation. In the absence of S-9 metabolic activation, both the extracts were unable to inhibit the mutagenicity of the known mutagen, 2-nitrofluorene, in Salmonella typhimurium TA98. On the other hand, the aqueous extracts at 100 μg/mL and methanol extracts at 10 and 100 μg/mL exhibited strong antimutagenic activity against the mutagenicity of 2-aminoanthracene, a known mutagen, in the presence of S-9 metabolic activating enzymes. The results indicated that these extracts could modulate the xenobiotic metabolising enzymes in the liver at the higher concentrations.     

Antimutagenic Potential and Modulation of Carcinogen‐Metabolizing Enzymes by Ginger Essential Oil

Essential oil extracted from ginger (GEO) was evaluated for its mutagenicity to Salmonella typhimurium TA 98, TA 100, TA 102, and TA 1535 strains with and without microsomal activation. GEO was found to be non‐mutagenic up to a concentration of 3 mg/plate. It was also assessed for antimutagenic potential against direct acting mutagens such as sodium azide, 4‐nitro‐o‐phenylenediamine, N‐methyl‐N′‐nitro‐N‐nitrosoguanidine, tobacco extract, and 2‐acetamidoflourene, which needs microsomal activation. GEO significantly inhibited (p < 0.001) the mutagenicity induced by these agents in a concentration‐dependent manner. The effect of GEO to modulate the action of phase I carcinogen‐metabolizing enzymes was investigated by studying its effect on various isoforms of microsomal cytochrome P450 enzymes. Significant inhibition of CYP1A1, CYP1A2, and CYP2B1/2, aniline hydroxylase (an indicator of CYP 2E1 activity), and aminopyrine‐N‐demethylase (indicator of CYP 1A, 2A, 2B, 2D, and 3A activity) was shown by GEO both in vitro and in vivo. GEO gave an IC₅₀ value of 30, 57.5, and 40 µg for CYP1A1, CYP1A2, and CYP2B1/2, respectively, 55 µg for aniline hydroxylase, and 37.5 µg for aminopyrene‐N‐demethylase. GEO also significantly increased the levels of phase II carcinogen‐metabolizing enzymes uridine 5′‐diphospho‐glucuronyl transferase and glutathione‐S‐transferase in vivo indicating the use of GEO as an antimutagen and as a potential chemopreventive agent. Copyright © 2013 John Wiley & Sons, Ltd.     

Effects of compounds of plant origin on the mutagenicity and metabolism of the tobacco-specific nitrosamine NNK

We have investigated the effects of five phytochemicals on the microsomal-dependent mutagenicity and metabolism of the tobacco-specific nitrosamine, 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK). Two compounds, d-limonene and silymarin, had no effect on NNK-induced mutagenesis in Salmonella typhimurium TA1535 over the concentration range of 0.1–0.4 μmol/plate. Diallyl sulphide was weakly antimutagenic at a concentration of 0.4 μmol/plate. Both capsaicin and tannic acid showed a dose-dependent inhibition of mutagenesis in TA1535. Metabolism studies using [³H]NNK indicated that the effects of the phytochemicals on NNK-induced mutagenesis did not always correlate with the effects on NNK metabolism. α-Carbon hydroxylation reactions are considered the most significant pathways involved in the metabolic activation of NNK to mutagenic and carcinogenic species. D-Limonene and silymarin (0,4 μmol) had the least inhibitory effect on the total α-carbon hydroxylation reactions, 19% and 28%. Capsaicin and diallyl sulphide inhibited these pathways by 74% and 70%. Tannic acid, the most potent phytochemical tested in this study, inhibited total α-carbon hydroxylation pathways by 99%.     

In vitro activity and mutagenicity of bisbenzylisoquinolines and quinones against Trypanosoma cruzi trypomastigotes

The accidental transmission of Chagas' disease by donor blood is recognized as a serious problem in the Latin America. This paper describes the screening of natural products as possible new chemoprophylactic additives in blood banks. Ten plant-derived alkaloids, three terpenes, three quinones and 14 crude plant extracts were tested against bloodstream forms of Trypanosoma cruzi Y strain in vitro at 4°C at a concentration of 250 μg/mL, using gentian violet as the baseline drug. The bisbenzylisoquinoline alkaloids, cocsuline, daphnandrine, daphnoline, isochondodendrine, gyrocarpine, limacine and pheanthine and the naphthoquinone, plumbagin completely lysed the trypomastigote forms of T. cruzi at a concentration of 250 μg/mL, this activity was verified by the subculture of the treated medium during 4 months. The active alkaloids, pheanthine, daphnoline and limacine were evaluated for mutagenicity by the sister chromatid exchange assay (SCE) in peripheral lymphocytes. Daphnoline and pheanthine elicited no significant increase of the SCE up to 50 μg/mL, while limacine significantly increased the SCE values at a concentration of 25 μg/mL, and 50 μg/mL.     

真菌植物松茸提取物体外抑制苯并(a)芘致突变作用研究

目的:寻找安全有效的抗突变生物资源,为利用生物资源预防肿瘤提供科学依据.方法:采用修改的Ames试验,研究松茸提取物PME对强致癌物B(a)P致突变作用的影响.结果:PME能显著性抑制B(a)P的致突变作用(P＜0.01),对测试菌株TA97、TA98和TA100的诱发回变菌落形成抑制率最高分别达到91.0%、97.8%和90.5%,PME可使B(a)P的诱发回变菌落数下降至阴性范围.PME抑制B(a)P致突变作用存在明显的剂量反应关系.结论:松茸提取物PME对B(a)P致突变作用具有显著的抑制作用,PME具有抗突变作用,在肿瘤预防方面具有应用前景.     

Synthesis and biological activity of analogs of fecapentaene-12

Analogs of the potent fecal mutagen fecapentaene-12 have been prepared and tested both for mutagenicity and for their ability to serve as biological precursors of 1. It was found that mutagenicity in three different Salmonella tester strains TA96, TA100, and TA104, decreased rapidly as the number of conjugated double bonds was reduced. The aldehyde 8, analogous to the hydrolysis product of 1, showed only low mutagenicity, even in the aldehyde-sensitive strain TA104. None of the polyenes prepared was able to function as a direct biological precursor of 1 under the conditions employed.     

Evaluation of the mutagenic and antimutagenic effects of South African plants

Dichloromethane and 90% methanol extracts of 42 South African plants were screened for mutagenicity and antimutagenicity using the Salmonella/microsome mutagenicity assay (Ames) against Salmonella typhimurium TA98 and TA100 bacterial strains in the presence and absence of metabolic activator S9. The methanol extracts from whole plants of Helichrysum simillimum, Helichrysum herbaceum and Helichrysum rugulosum indicated mutagenicity. These are the first reported tests on the mutagenicity of Helichrysum species. Six species indicated antimutagenic properties, all in the presence of S9: methanol leaf extract of Bauhinia galpinii, and dichloromethane leaf extracts of Bauhinia galpinii, Clerodendrum myricoides, Datura stramonium, Buddleja saligna, Millettia sutherlandii and Sutherlandia frutescens.