我院2009～2011年抗肿瘤中药注射剂使用情况分析

目的对我院2009~2011年抗肿瘤用中药注射剂的使用情况进行分析,为临床合理用药提供参考。方法采用回顾性调查方法对我院2009~2011年抗肿瘤中药注射剂的品种、金额、用药频度和不良反应等数据进行统计分析。结果 3年来我院抗肿瘤中药注射剂用药总金额和构成比均逐年上升,其中艾迪注射液、康莱特注射液稳居前列,复方苦参注射液的DDDs逐年增加。抗肿瘤中药注射剂的不良反应发生率逐年降低。结论我院抗肿瘤中药注射剂使用趋于合理,基本能做到合理用药,减少不良反应的发生。     

红曲E-70及洛伐他汀对乳腺癌细胞MCF-7的增殖影响

目的探讨红曲乙醇提取物（红曲E-70）及洛伐他汀对人乳腺癌细胞MCF-7增殖的影响。方法制备红曲E-70,利用高效液相检测其洛伐他汀的含量,应用MTT法检测不同浓度红曲E-70和其对应洛伐他汀的含量对人乳腺癌细胞MCF-7增殖情况的影响。结果红曲E-70在1~150μg/mL浓度范围抑制MCF-7增殖,而洛伐他汀只在0.15μg/ml浓度抑制MCF-7增殖（P〈0.05）。结论红曲E-70抑制MCF-7增殖,其抑制MCF-7增殖的作用比洛伐他汀更强。     

噻唑类化合物的活性研究

噻唑类化合物作为一种重要的生物学活性支架,具有广泛而强有力的生物学活性。本文着重突出阐述了最新噻唑类化合物的重要性,认为它具有十足的应用前景。     

中药注射剂在化疗科的应用分析

目的:分析连云港市第一人民医院抗肿瘤中药注射剂的临床使用情况,探讨抗肿瘤中药注射剂的合理使用问题.方法:对连云港市第一人民医院2010年住院患者使用抗肿瘤中药注射剂的情况进行统计分析;随机抽取同期化疗科住院病历,分析抗肿瘤中药注射剂的临床地位.结果:抗肿瘤中药注射剂销售金额占全部抗肿瘤药销售金额的28.55%;在抽查的...     

Characterization of the anticancer properties of monoglycosidic cardenolides isolated from Nerium oleander and Streptocaulon tomentosum

Aim of the study

For identification of the active constituents we investigated the anticancer activity of cardenolides from Streptocaulon tomentosum Wight & Arn. (Asclepiadaceae) and from Nerium oleander L. (Apocynaceae) which are both used against cancer in the traditional medicine in their region of origin.

Material, methods and results

The antiproliferative activity of cardenolides isolated from roots of Streptocaulon tomentosum (IC₅₀ < 1-15.3 μM after 2 days in MCF7) and of cardenolide containing fractions from the cold aqueous extract of Nerium oleander leaves (“Breastin”, mean IC₅₀ 0.85 μg/ml in a panel of 36 human tumor cell lines), their influence on the cellular viability and on the cell cycle (block at the G2/M-phase or at the S-phase in tumor cells, respectively) were determined using different cell lines. The murine cell line L929 and normal non-tumor cells were not affected. Bioactivity guided fractionation of Breastin resulted in the isolation of the monoglycosidic cardenolides oleandrine, oleandrigeninsarmentoside, neritaloside, odoroside H, and odoroside A (IC₅₀-values between 0.010 and 0.071 μg/ml).

Conclusions

The observed anticancer activities of extracts and isolated cardenolides are in agreement with the ethnomedicinal use of Streptocaulon tomentosum and Nerium oleander. The most active anticancer compounds from both species are monoglycosidic cardenolides possessing the 3β,14β-dihydroxy-5β-card-20(22)-enolide structure with or without an acetoxy group at C-16. The results indicate that the cytotoxic effects are induced by the inhibition of the plasma membrane bound Na⁺/K⁺-ATPase.     

胃癌组织中抑癌及相关基因的表达及其临床意义

目的探讨胃癌组织中抑癌基因nm23和E-cadherin及肿瘤相关基因CD44s表达及与其临床病理特征的关系。方法应用免疫组化SP法,检测50例胃癌组织及其癌旁组织中nm23和E-cadherin及CD44s基因的表达,应用统计学方法分析与其临床病理特征的相关性。结果胃癌组织中nm23和E-cadherin及CD44s基因阳性表达率分别为48.0%和44.5%及52.0%。nm23和E-cadherin基因阳性表达率与胃癌组织学分化程度、临床分期和淋巴结转移等密切相关,P均〈0.05。CD44s阳性表达与肿瘤是否有浆膜浸润、淋巴结转移和TNM分期相关,P〈0.05。CD44s表达与nm23表达呈一定程度的负相关性,nm23表达与E-cadherin表达呈正相关性。结论 nm23和E-cadherin及CD44s基因与胃癌的发生和转移相关,检测其表达可预测胃癌转移和侵袭程度。     

Part 3: Pharmacogenetic variability in phase II anticancer drug metabolism

Equivalent drug doses may lead to wide interpatient variability in drug response to anticancer therapy. Known determinants that may affect the pharmacological response to a drug are, among others, nongenetic factors, including age, gender, use of comedication, and liver and renal function. Nonetheless, these covariates do not explain all the observed interpatient variability. Differences in genetic constitution among patients have been identified to be important factors that contribute to differences in drug response. Because genetic polymorphism may affect the expression and activity of proteins encoded, it is a key covariate that is responsible for variability in drug metabolism, drug transport, and pharmacodynamic drug effects. We present a series of four reviews about pharmacogenetic variability. This third part in the series of reviews is focused on genetic variability in phase II drug-metabolizing enzymes (glutathione S-transferases, uridine diphosphoglucuronosyl transferases, methyltransferases, sulfotransferases, and N-acetyltransferases) and discusses the effects of genetic polymorphism within the genes encoding these enzymes on anticancer drug therapy outcome. Based on the literature reviewed, opportunities for patient-tailored anticancer therapy are proposed.     

Development of a chemically stable 10-hydroxycamptothecin nanosuspensions

The purpose of this study was to prepare and characterize nanosuspensions loading the active lactone form of 10-hydroxycamptothecin (10-HCPT). Nanosuspensions were prepared in terms of microprecipitation–high-pressure homogenization method. As for the preparation processes, three important parameters, i.e. the agitation rate of stabilizer solution, homogenization pressure and cycle numbers, were investigated and optimized, and the optimal values were 1000 rpm, 1000 bar and 20 times, respectively. The particle size and zeta potential of the 10-HCPT-nanosuspensions were 131 nm and −25.5 mV. The particle morphology was determined by transmission electron microscopy and the 10-HCPT nanoparticles were baculine or trabecular in shape. The solid state of 10-HCPT in nanoparticles was analyzed using X-ray powder diffraction (XRD) and differential scanning calorimetry (DSC). The XRD and the DSC results both indicated that 10-HCPT was present as an amorphous state in the lyophilized powders for nanosuspension. The chemical stability tests demonstrated that near 90% lactone form of 10-HCPT was present in the nanosuspensions but it was easily transferred to the carboxylate form in the solution at pH 7.0–8.0. In vitro dissolution tests showed the dissolution rate of nanosuspensions, compared with the coarse suspensions, had been significantly increased.     

Design, synthesis and anticancer evaluation of novel tetrahydroquinoline derivatives containing sulfonamide moiety

Sulfonamides posses many types of biological activities and have recently been reported to show substantial antitumor activity in vitro and/or in vivo. There are a variety of mechanisms for the anticancer activity and the most prominent of these is through the inhibition of carbonic anhydrase isozymes. The present work reports the synthesis of some novel quinoline and pyrimido[4,5-b]quinoline derivatives bearing a substituted or unsubstituted sulfonamide moiety. The design of the structures of these compounds complies with the general pharmacophore of the sulfonamide compounds that act as carbonic anhydrase (CA) inhibitors as this may play a role in their anticancer activity. All the newly synthesized compounds were evaluated for their in vitro anticancer activity against breast cancer cell line (MCF7). Most of the screened compounds showed interesting cytotoxic activities compared to a reference drug.     

Characterization of the anti-Leishmania effect induced by cisplatin, an anticancer drug

The cis-diamminedichloroplatinum(II), known as cis-DDP or cisplatin is a widely used drug in cancer chemotherapy. Although a recent study has shown the anti-Leishmania activity of some cis-DDP derivatives, the cytotoxic properties were measured only on promastigotes, the insect vector form of the parasite. In this study the effect of cis-DDP on promastigotes and amastigotes, the vertebrate stage of the parasite is reported. The IC50, determined by flow cytometry, after 72 h of drug incubation was four times higher, 7.73+/-1.03 microM in the case of promastigotes compared to axenic amastigotes, 1.88+/-0.10 microM. In intracellular amastigotes the IC50, determined by counting the parasite index was 1.85+/-0.22 microM. By using flow cytometry, two patterns of cell cycle changes was observed: cis-DDP treated promastigotes and amastigotes accumulated in S phase and G2 phase, respectively. The cis-DDP response was also found to involve an "apoptosis-like" death of both promastigotes and amastigotes. However, DNA fragmentation was only detected in promastigote forms. In contrast mitochondrial transmembrane potential loss was observed for both stages of the parasite. Upon incubation of parasites with the drug an increase on GSH and GSSG levels and reactive oxygen species could be detected in the case of promastigote. Moreover, a slight increase of GSH level was detected on amastigote form. Taken together, these observations indicate that amastigotes are more sensitive to cis-DDP when compared to promastigotes. However, the signaling pathways leading to cell death could be different.