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Evaluation and SAR analysis of the cytotoxicity of tanshinones in colon cancer cells

chinese Journal of Natural Medicines 2014年第3期12卷 167-171页

作者： WANG Lin LIU An ZHANG Fei-Long Yeung John H.K. LI Xu-Qin cho chi-hin School of Biomedical Sciences Faculty of MedicineThe Chinese University of Hong Kong Institute of chinese Materia Medica China Academy of Chinese Medical Sciences Department of Chemistry University of Science and Technology Beijing

AIM:This study was designed to evaluate the anti-cancer actions of tanshinone I and tanshinone IIA,and six derivatives of tanshinone IIA on normal and cancerous colon *** activity relationship(SAR) analysis was conducted to delineate the significance of the structural modifications of tanshinones for improved anti-cancer ***:Tanshinone derivatives were designed and synthesized according to the *** cytotoxicity of different compounds on colon cancer cells was determined by the MTT *** activity of the tanshinones was measured by flow cytometry(FCM).RESULTS:Tanshinone I and tanshinone IIA both exhibited significant cytotoxicity on colon cancer *** are more effective in p53+/+ colon cancer cell *** was also noted that the anti-cancer activity of tanshinone I was more potent and *** of the derivatives of tanshinone IIA(N1 and N2) also exhibited cytotoxicity on colon cancer ***:The anti-colon cancer activity of tanshinone I was more potent and selective than tanshinone IIA,and is p53 *** derivatives obtained by structural modifications of tanshinone IIA exhibited lower cytotoxicity on both normal and colon cancer *** steric and electronic characteristics point of view,it was concluded that structural modifications of ring A and furan or dihydrofuran ring D on the basic structure of tanshinones influences the *** increase of the delocalization of the A and B rings could enhance the cytotoxicity of such compounds,while a non-planar and small sized D ring region would provide improved anti-cancer activity.

关键词： Tanshinones Synthetic derivatives Colon cancer Cytotoxicity SAR analysis

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Cathelicidin stimulates colonic mucus synthesis by up-regulating MUC1 and MUC2 expression through a mitogen-activated protein kinase pathway

Cathelicidin stimulates colonic mucus synthesis by up-regula...

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两岸三地药理学与临床药理学术会议

作者： cho chi-hin Department of Pharmacology Chinese University of Hong Kong

Objective Mucus forms the physical barrier along the gastrointestinal(GI)*** plays an im- portant role to prevent mucosal damage and *** previous finding showed that antibacterial peptide’cathelicidin’increased mucus thickness and prevented inflammation in the *** the current study,we examined the protective mechanisms by which the peptide increased mucus synthesis in vitro. Methods Human colonic cell line(HT-29)was used to assess the stimulatory action of cathelicidin on mucus synthesis which was measured by the D-[6-

关键词： cathelicidin mucus mucin mitogen-activated protein kinase

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Cathelicidin stimulates colonic mucus synthesis by up-regulating MUC1 and MUC2 expression through a mitogen-activated protein kinase pathway

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沈阳药科大学学报 2008年第S1期25卷 3-3页

作者： cho chi-hin Department of Pharmacology Chinese University of Hong Kong

Objective Mucus forms the physical barrier along the gastrointestinal(GI)*** plays an important role to prevent mucosal damage and *** previous finding showed that antibacterial peptide 'cathelicidin' increased mucus thickness and prevented inflammation in the *** the current study,we examined the protective mechanisms by which the peptide increased mucus synthesis in *** Human colonic cell line(HT-29)was used to assess the stimulatory action of cathelicidin on mucus synthesis which was measured by the D-[6-3H] glucosamine incorporation *** Human cathelicidin(LL-37)dose-dependently(10-40 μg·mL-1)and significantly stimulated mucus ***-time PCR data showed that addition of LL-37 induced more than 50% increase in MUC1 and MUC2 mRNA *** with MUC1 and MUC2 siRNAs normalized the stimulatory action of LL-37 on mucus ***-37 also activated the phosphorylation of mitogen-activated protein(MAP)kinase in the cells.A specific inhibitor of the MAP kinase pathway,U0126,completely blocked the increase of MUC1 and MUC2 expression as well as mucus synthesis by *** Taken together LL-37 stimulates mucus synthesis through the activation of MUC1 and MUC2 expression and the MAP kinase pathway in human colonic cells.

关键词： cathelicidin mucus mucin mitogen-activated protein kinase

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The role of 5-lipoxygenase in the tumorigenesis promoted by cigarette smoke

The role of 5-lipoxygenase in the tumorigenesis promoted by ...

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中国药理学会第八次全国代表大会暨全国药理学术会议

作者： Liu Edgar Shiu-Lam Shin Vivian-Yvonne cho chi-hin Department of Pharmacology The University of Hong Kong Hong Kong China

AIM: 5-lipoxygenase (5-LOX) is an enzyme that converts arachidonic acid to 5-s-HETE, andseveral studies have suggested a link between 5-s-HETE formation and carcinogenesis in variousorgans. Our previous study shows that passive cigarette smoking promotedinflammation-associated adenoma formation in colon. The purpose of the present study was toinvestigate the possible involvement of 5-LOX in the tumorigenesis enhanced by cigarette ***: In vivo study, male balb/c mice were allocated into 4 groups: control, cigarettesmoke (CS), dextran sulfate sodium (DSS) and DSS+CS. They were given water or 3% DSS indrinking water for 7 days to induce colitis, with or without 1-hour daily exposure to 2% CS. They

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表皮生长因子通过上调环氧酶2促进人食管鳞癌细胞HKESC-1的增殖

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南方医科大学学报 2011年第8期31卷 1323-1326页

作者：余乐曹之宪刘叔文南方医科大学药学院广东广州510515 香港中文大学生物医学学院

目的研究表皮生长因子(EGF)促进人食管鳞癌细胞增殖的机制。方法氚标记的脱氧胸腺嘧啶核苷掺入法检测细胞增殖。酶免疫法检测前列腺素(PGE2)的释放。免疫印迹法检测环氧酶1(COX-1),环氧酶2(COX-2),PGE2受体亚型EP1和EP2的蛋白表达。结果... 详细信息

目的研究表皮生长因子(EGF)促进人食管鳞癌细胞增殖的机制。方法氚标记的脱氧胸腺嘧啶核苷掺入法检测细胞增殖。酶免疫法检测前列腺素(PGE2)的释放。免疫印迹法检测环氧酶1(COX-1),环氧酶2(COX-2),PGE2受体亚型EP1和EP2的蛋白表达。结果 EGF上调人食管鳞癌HKESC-1细胞COX-2蛋白表达,而不影响COX-1蛋白表达。EGF还能刺激HKESC-1细胞释放PGE2,并上调PGE2受体亚型EP2的蛋白表达。非选择性COX抑制剂吲哚美辛和COX-2选择性抑制剂SC-236均可完全阻断EGF刺激的PGE2释放。这两种COX抑制剂也都能够抑制EGF的促细胞增殖作用。结论 EGF对HKESC-1细胞的促增殖作用,一方面是通过诱导COX-2蛋白的表达从而促进PGE2的释放;另一方面通过上调EP2受体的蛋白表达。

关键词：食管鳞癌 EGF 环氧酶前列腺素环氧酶抑制剂

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Involvement of polyamine in the delay of wound healing induced by cigarette smoke

Involvement of polyamine in the delay of wound healing induc...

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中国药理学会第八次全国代表大会

作者： Shin Vivian - Yvonne LIU Edgar Shiu - Lam KOO Marcel Wing - Leung cho chi - hin Department of Pharmacology The University of Hong Kong Hong Kong China

AIM: Strong association of cigarette smoking and peptic ulcer diseases has been well established. However, the mechanistic adverse action of cigarette smoke on wound healing is still unclear. Cell proliferation and cell migration are important factors for maintaining the gastrointestinal integrity during wound repair. Ornithine decarboxylase (ODC), a rate-limiting enzyme for polyamine biosynthesis, is crucial for cell growth and differentiation. This study was designed to delineate the involvement of polyamines on the delay of wound healing induced by cigarette smoke. METHODS: Cigarette smoke extracts (CSE) were prepared from the burning cigarettes, and differentiated into chloroform extract (CE) and

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The role of 5 -lipoxygenase in the tumorigenesis promoted by cigarette smoke

The role of 5 -lipoxygenase in the tumorigenesis promoted by...

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第六届全国药理学教学学术会议

作者： YE Yi - Ni, Liu Edgar Shiu - Lam, Shin Vivian - Yvonne, cho chi - hin Department of Pharmacology, The University of Hong Kong, Hong Kong, china

AIM: 5-lipoxygenase (5-LOX) is an enzyme that converts arachidonic acid to 5-s-HETE, and several studies have suggested a link between 5 - s - HETE formation and carcinogenesis in various organ. Our previous study shows that passive cigarettesmoking promoted inflammation - associated adenoma formation in colon. The purpose of the present study was to investigate the possible involvement of 5 - LOX in the tumorigenesis enhanced by cigarette smoke. METHODS: In vivo study, male balb/c mice were allocated into 4 groups: control, cigarette smoke (CS), dextran sulfate sodium (DSS)

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A New Encryption Mechanism Supporting the Update of Encrypted Data for Secure and Efficient Collaboration in the Cloud Environment

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Computer Modeling in Engineering & Sciences 2025年第1期142卷 813-834页

作者： Chanhyeong cho Byeori Kim Haehyun cho Taek-Young Youn Department of Cyber Security Dankook UniversityYongin16890Republic of Korea Department of Software Soongsil UniversitySeoul07027Republic of Korea

With the rise of remote collaboration,the demand for advanced storage and collaboration tools has rapidly ***,traditional collaboration tools primarily rely on access control,leaving data stored on cloud servers vulnerable due to insufficient *** paper introduces a novel mechanism that encrypts data in‘bundle’units,designed to meet the dual requirements of efficiency and security for frequently updated collaborative *** bundle includes updated information,allowing only the updated portions to be reencrypted when changes *** encryption method proposed in this paper addresses the inefficiencies of traditional encryption modes,such as Cipher Block Chaining(CBC)and Counter(CTR),which require decrypting and re-encrypting the entire dataset whenever updates *** proposed method leverages update-specific information embedded within data bundles and metadata that maps the relationship between these bundles and the plaintext *** utilizing this information,the method accurately identifies the modified portions and applies algorithms to selectively re-encrypt only those *** approach significantly enhances the efficiency of data updates while maintaining high performance,particularly in large-scale data *** validate this approach,we conducted experiments measuring execution time as both the size of the modified data and the total dataset size *** show that the proposed method significantly outperforms CBC and CTR modes in execution speed,with greater performance gains as data size ***,our security evaluation confirms that this method provides robust protection against both passive and active attacks.

关键词： Cloud collaboration mode of operation data update efficiency

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顺铂下调铜离子转运蛋白1诱导人食管鳞癌细胞EC109耐药

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南方医科大学学报 2011年第5期31卷 801-804页

作者：余乐陈明辉古春萍李亦蕾文静傅剑华曹之宪刘叔文南方医科大学药学院广东广州510515 南方医科大学南方医院药学部广东广州510515 中山大学肿瘤防治中心广东广州510060 香港中文大学生物医学学院

目的研究人食管鳞癌细胞顺铂耐药性产生的机制。方法 MTT法检测顺铂对耐药细胞EC109/CDDP及其亲代细胞EC109的细胞毒作用。电感耦合等离子体质谱检测细胞内顺铂的蓄积和Pt-DNA加合物的形成。Western blotting检测人多聚腺苷二磷酸核糖... 详细信息

目的研究人食管鳞癌细胞顺铂耐药性产生的机制。方法 MTT法检测顺铂对耐药细胞EC109/CDDP及其亲代细胞EC109的细胞毒作用。电感耦合等离子体质谱检测细胞内顺铂的蓄积和Pt-DNA加合物的形成。Western blotting检测人多聚腺苷二磷酸核糖聚合酶(poly-ADP-ribose polymerase,PARP)的剪切和铜离子转运蛋白1(copper transporter1,CTR1)的蛋白表达。结果顺铂耐药细胞株EC109/CDDP较其亲代细胞EC109对顺铂引起的细胞毒作用和凋亡敏感性下降,细胞内顺铂蓄积和Pt-DNA加合物的形成减少,并且CTR1蛋白表达水平降低。结论顺铂通过降低细胞CTR1蛋白表达抑制顺铂进入细胞,导致细胞耐药性的产生。

关键词：食管鳞癌 EC109 顺铂耐药性铜转运蛋白1

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Three-Stage Transfer Learning with AlexNet50 for MRI Image Multi-Class Classification with Optimal Learning Rate

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Computer Modeling in Engineering & Sciences 2025年第1期142卷 155-183页

作者： Suganya Athisayamani A.Robert Singh Gyanendra Prasad Joshi Woong cho School of Computing Sastra Deemed to be UniversityThanjavur613401India Department of Computational Intelligence SRM Institute of Science and TechnologyKattankulathur603203India Department of AI and Software Engineering Kangwon National UniversitySamcheok25913Republic of Korea Department of Electronics Information and Communication EngineeringKangwon National UniversitySamcheok25913Republic of Korea

In radiology,magnetic resonance imaging(MRI)is an essential diagnostic tool that provides detailed images of a patient’s anatomical and physiological *** is particularly effective for detecting soft tissue ***,radiologists manually interpret these images,which can be labor-intensive and time-consuming due to the vast amount of *** address this challenge,machine learning,and deep learning approaches can be utilized to improve the accuracy and efficiency of anomaly detection in MRI *** manuscript presents the use of the Deep AlexNet50 model for MRI classification with discriminative learning *** are three stages for learning;in the first stage,the whole dataset is used to learn the *** the second stage,some layers of AlexNet50 are frozen with an augmented dataset,and in the third stage,AlexNet50 with an augmented dataset with the augmented *** method used three publicly available MRI classification datasets:Harvard whole brain atlas(HWBA-dataset),the School of Biomedical Engineering of Southern Medical University(SMU-dataset),and The National Institute of Neuroscience and Hospitals brain MRI dataset(NINS-dataset)for *** hyperparameter optimizers like Adam,stochastic gradient descent(SGD),Root mean square propagation(RMS prop),Adamax,and AdamW have been used to compare the performance of the learning ***-dataset registers maximum classification *** evaluated the performance of the proposed classification model using several quantitative metrics,achieving an average accuracy of 98%.

关键词： MRI tumors classification AlexNet50 transfer learning hyperparameter tuning optimizer

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