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抗肿瘤中药药效物质筛选与辨识的研究方法进展 被引量:2
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作者 张月华 蒋才武 《中南药学》 CAS 2020年第9期1517-1522,共6页
恶性肿瘤严重威胁人体的健康,且发病率持续增加,因此国内外高度重视抗肿瘤药物的研究与开发。抗肿瘤中药在传统中医药理论的指导下应用于肿瘤疾病的治疗,具有临床疗效显著、不良反应较少、延长生存质量等独特的优势,呈现了广阔的开发应... 恶性肿瘤严重威胁人体的健康,且发病率持续增加,因此国内外高度重视抗肿瘤药物的研究与开发。抗肿瘤中药在传统中医药理论的指导下应用于肿瘤疾病的治疗,具有临床疗效显著、不良反应较少、延长生存质量等独特的优势,呈现了广阔的开发应用前景。通过分析与总结抗肿瘤中药筛选与辨识药效物质的相关文献,发现目前的主要研究方法包括:生物活性追踪法、谱效关系法、血清药物化学法、代谢组学法、亲和色谱法、网络药理学法等方法。本文以抗肿瘤中药研究方法的应用进展进行综述,旨在为未来抗肿瘤药效物质的筛选、作用机制的阐明以及新药开发提供参考依据。 展开更多
关键词 中药 抗肿瘤药效物质 筛选及辨识
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肿瘤氧化还原微环境响应型小分子前药纳米粒的代谢与药效研究进展 被引量:4
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作者 赵耀 杨璨羽 +1 位作者 张强 王学清 《药学学报》 CAS CSCD 北大核心 2021年第2期476-486,共11页
与正常组织、细胞的微环境相比,肿瘤微环境具有显著差异,如谷胱甘肽相关代谢酶和活性氧在不同亚细胞结构中高表达,造成氧化还原状态失衡。根据这种特异性的氧化还原状态,可以设计一系列通过氧化还原响应型连接臂相连的小分子前药纳米粒... 与正常组织、细胞的微环境相比,肿瘤微环境具有显著差异,如谷胱甘肽相关代谢酶和活性氧在不同亚细胞结构中高表达,造成氧化还原状态失衡。根据这种特异性的氧化还原状态,可以设计一系列通过氧化还原响应型连接臂相连的小分子前药纳米粒。常见的连接臂有二硫键、硫醚键、硒键和硫缩酮键等。不同连接臂的小分子前药纳米粒具有不同的代谢方式和体内外药效作用。本篇综述将从肿瘤细胞特异性氧化还原状态、智能响应型小分子前药纳米粒的设计、不同连接臂的小分子前药纳米粒的代谢方式及其与药效的关系等方面来总结肿瘤氧化还原微环境响应型小分子前药纳米系统的研究进展。 展开更多
关键词 氧化还原响应 小分子前药纳米粒 二硫键 硫醚键 细胞药代动力学 抗肿瘤药效
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Radiomics in Antineoplastic Agents Development:Application and Challenge in Response Evaluation
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作者 Jiazheng Li Lei Tang 《Chinese Medical Sciences Journal》 CAS CSCD 2021年第3期187-195,共9页
The recent spring up of the antineoplastic agents and the prolonged survival bring both challenge and chance to radiological practice.Radiological methods including CT,MRI and PET play an increasingly important role i... The recent spring up of the antineoplastic agents and the prolonged survival bring both challenge and chance to radiological practice.Radiological methods including CT,MRI and PET play an increasingly important role in evaluating the efficacy of these antineoplastic drugs.However,different antineoplastic agents potentially induce different radiological signs,making it a challenge for radiological response evaluation,which depends mainly on one-sided morphological response evaluation criteria in solid tumors(RECIST)in the status quo of clinical practice.This brings opportunities for the development of radiomics,which is promising to serve as a surrogate for response evaluations of anti-tumor treatments.In this article,we introduce the basic concepts of radiomics,review the state-of-art radiomics researches with highlights of radiomics application in predictions of molecular biomarkers,treatment response,and prognosis.We also provide in-depth analyses on major obstacles and future direction of this new technique in clinical investigations on new antineoplastic agents. 展开更多
关键词 radiomics deep learning machine learning antineoplastic agents response evaluation
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Effect of bone marrow-derived monocytes transfected with RNA of mouse colon carcinoma on specific antitumor immunity 被引量:2
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作者 Xiao-YuanChu Long-BangChen JingZang Jing-HuaWang QunZhang Huai-ChengGeng 《World Journal of Gastroenterology》 SCIE CAS CSCD 2005年第5期760-763,共4页
AIM: To investigate the effect of bone marrow-derived monocytes transfected with RNA of CT-26 (a cell line of mouse colon carcinoma) on antitumor immunity. METHODS: Mouse bone marrow-derived monocytes were incubated w... AIM: To investigate the effect of bone marrow-derived monocytes transfected with RNA of CT-26 (a cell line of mouse colon carcinoma) on antitumor immunity. METHODS: Mouse bone marrow-derived monocytes were incubated with mouse granulocyte macrophage colony stimulating factor (mGM-CSF) in vitro, and the purity of monocytes was detected by flow cytometry. Total RNA of CT-26 was obtained by TRIzol's process, and monocytes were transfected by TransMessenger in vitro. The activity of cytotoxic T lymphocytes (CTL) in vivo was estimated by the modified lactate dehydrogenase (LDH) release assay. Changes of tumor size in mice and animal's survival time were observed in different groups. RESULTS: Monocytes from mouse bone marrow were successfully incubated, and the positive rate of CDllb was over 95%. Vaccination of the monocytes transfected with total RNA induced a high level of specific CTL activity in vivo, and made mice resistant to the subsequent challenge of parental tumor cells. In vivo effects induced by monocytes transfected with total RNA were stronger than those induced by monocytes pulsed with tumor cell lysates. CONCLUSION: Antigen presenting cells transfected with total RNA of CT-26 can present endogenous? tumor antigens, activate CTL, and effectively induce specific antitumor immunity. 展开更多
关键词 Colon carcinoma RNA Bone marrow-derived monocytes Cytotoxic T lymphocytes
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Basic and clinical study of increased effect of partial anti-tumor agents by infusing sodium bicarbonate through target artery 被引量:3
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作者 Pingsheng Fan Shicun Wang Lin Xiu Jide Li Kehai Feng Feihu Chen Xinmin Lin Jiansheng Zhuang 《The Chinese-German Journal of Clinical Oncology》 CAS 2007年第1期13-17,共5页
Objective: To observe the influence of pH value on the proliferation of LAK cells and on the killing effect of rlL-2, IFN-α2b, TNF-α, LAK cells and doxorubicin on malignant tumor cells, and investigate the possibil... Objective: To observe the influence of pH value on the proliferation of LAK cells and on the killing effect of rlL-2, IFN-α2b, TNF-α, LAK cells and doxorubicin on malignant tumor cells, and investigate the possibility of increasing the efficacy of rlL-2 or IFN-α2b and doxorubicin by infusing sodium bicarbonate (NaHCO3) through target arteries. Methods: Separating single nucleus cells from peripheral blood of healthy men, and observing the influence of pH on the activation of single nucleus cells by rlL-2. MTT assay was used to measure the killing effect of rlL-2, IFN-α2b and TNF-α on 7404 cells and the increased effect of doxorubicin on rlL-2 and IFN-α2b, the cytotoxity of LAK cells in different pH. Forty-two patients with advanced primary liver cancer were obtained by stratified random, NaHCO3, rIL-2/IFN-α2b and doxorubicin were infused through target arteries. The efficacy was estimated after two cycles. Results: The conditions of pH 7.3 and pH 7.6 in vitro helped the proliferation of LAK cells and the killing effect of rIL-2, IFN-α2b and LAK cells on 7404 cells. In the condition of pH 6.8 there was almost no killing effect for LAK cells. In the condition of pH 7.0, 7.2, 7.4 and 7.6, the killing rate of TNF-α to 7404 cells increased by degrees, and in pH 7.4 the killing effect was the optimum. After two cycles treatments in the 42 patients with advanced primary liver cancer, the response rate (CR+PR) was 88% (37/42). The median overall response and median overall survival were increased, and no complication associated with infusing sodium bicarbonate was observed. Conclusion: The killing effect of rIL-2, IFN-α2b, TNF-α and doxorubicin on malignant tumor cells was enhanced by increasing the pH value. 展开更多
关键词 acid-base balance primary liver cancer sodium bicarbonate RIL-2 DOXORUBICIN MICROENVIRONMENT tumor immunity
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高载药量雷公藤红素纳米混悬剂的制备及体外评价 被引量:14
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作者 黄甜甜 沈一平 +2 位作者 路丽康 孙雪晴 王向涛 《中草药》 CAS CSCD 北大核心 2020年第8期2125-2133,共9页
目的以泊洛沙姆188(P188)为稳定剂制备高载药量的雷公藤红素纳米混悬剂(Cel-NSps),提高药物的溶解度、释放度和抗肿瘤药效。方法采用微型化介质研磨法和沉淀法制备Cel-NSps,通过动态光散射法、透射电子显微镜和X射线衍射(XRD)法对粒径... 目的以泊洛沙姆188(P188)为稳定剂制备高载药量的雷公藤红素纳米混悬剂(Cel-NSps),提高药物的溶解度、释放度和抗肿瘤药效。方法采用微型化介质研磨法和沉淀法制备Cel-NSps,通过动态光散射法、透射电子显微镜和X射线衍射(XRD)法对粒径、形貌和晶型进行表征并考察其稳定性,透析袋法考察体外释放情况;MTT法评价其对小鼠乳腺癌细胞4T1、人肝癌细胞HepG2、人皮肤恶性黑色素瘤细胞SK-MEL-28、人乳腺癌细胞MCF-7的细胞毒性。结果微型介质研磨法制备的Cel-NSps平均粒径为(215.7±0.7)nm,多分散指数(PDI)为0.17±0.02,Zeta电位为(-18.0±0.6)m V,平均载药量为(87.62±1.02)%,形状不规则,药物在纳米混悬剂中以晶形态存在;在磷酸盐缓冲液(PBS)、0.9%NaCl、5%葡萄糖、血浆和人工肠液中能稳定存在,但在人工胃液中不稳定;沉淀法制备的Cel-NSps平均粒径为(133.1±0.8)nm,PDI为0.13±0.02,Zeta电位为(-16.9±1.2)m V,平均载药量为(86.39±0.21)%,近乎球形,药物在纳米混悬剂中以无定形态存在,在各种生理介质中都能稳定存在,可用于口服或静脉注射给药。微型化介质研磨法制备的Cel-NSps呈匀速缓慢的释放,144 h累积释放54.40%;沉淀法制备的纳米混悬剂呈两相释放,前48 h快速均匀释放,之后非常缓慢释放,144h累积释放73.12%,而原料药144 h仅释放11.09%。MTT实验表明,Cel-NSps对4T1、Hep G2、SK-MEL-28、MCF-7细胞具有显著的生长抑制作用且呈剂量依赖性,对4种细胞的IC50在0.92~1.96μg/m L。结论以P188为稳定剂用2种不同方法制备了小粒径、高载药量的Cel-NSps,成功解决了溶解度差和释放度低的难题,且制备方法简单,易于工业化生产,为雷公藤红素的新药研发奠定了基础。 展开更多
关键词 雷公藤红素 纳米混悬剂 介质研磨法 反溶剂沉淀法 载药量 体外评价 溶解度 释放度 抗肿瘤药效 MTT法 细胞毒性
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Preparation and characterization of zinc oxide nanoparticles 被引量:1
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作者 Man Liu Shuang Zhang +3 位作者 Zhuoyue Li Guangxue Wang Jingru Wang Xuan Zhang 《Journal of Chinese Pharmaceutical Sciences》 CAS CSCD 2020年第9期617-625,共9页
In the present study, the zinc oxide nanoparticles(ZnO NPs) were prepared by using a sol-gel method. The characterization of ZnO NPs, such as particle size, morphology, crystal form, optical properties and p H-respons... In the present study, the zinc oxide nanoparticles(ZnO NPs) were prepared by using a sol-gel method. The characterization of ZnO NPs, such as particle size, morphology, crystal form, optical properties and p H-responsive behavior, was carried out. The in vitro anti-tumor activity of ZnO NPs was evaluated on PC-3M and 4T1 cell lines. The results indicated that ZnO NPs were spherical NPs with uniform particle size, excellent fluorescence properties, and p H-responsive behavior. The in vitro anti-tumor activity of ZnO NPs was observed on PC-3M and 4T1 cell lines. Considering to above characteristics, Zn O NPs could be used as drug delivery carries for loading active compound performing therapeutic and diagnostic effect. 展开更多
关键词 Zinc oxide nanoparticles Sol-gel method Size and morphology Optical properties In vitro anti-tumor activity
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