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Benzimidazole and its derivatives as cancer therapeutics:The potential role from traditional to precision medicine

Acta Pharmaceutica Sinica B 2023年第2期13卷 478-497页

作者： Yeuan Ting Lee Yi Jer Tan chern ein oon Institute for Research in Molecular Medicine(INFORMM) Universiti Sains Malaysia11800 MindenPenangMalaysia

Cancer is the second leading cause of mortality globally which remains a continuing threat to human health *** insensitivity and resistance are critical hurdles in cancer treatment;therefore,the development of new entities targeting malignant cells is considered a high *** therapy is the cornerstone of precision *** synthesis of benzimidazole has garnered the attention of medicinal chemists and biologists due to its remarkable medicinal and pharmacological *** has a heterocyclic pharmacophore,which is an essential scaffold in drug and pharmaceutical *** studies have demonstrated the bioactivities of benzimidazole and its derivatives as potential anticancer therapeutics,either through targeting specific molecules or non-gene-specific *** review provides an update on the mechanism of actions of various benzimidazole derivatives and the structure-activity relationship from conventional anticancer to precision healthcare and from bench to clinics.

关键词： Benzimidazole derivatives Targeted therapy Anticancer Precision medicine

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Anti-tumour activity and toxicological studies of combination treatment of Orthosiphon stamineus and gemcitabine on pancreatic xenograft model

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World Journal of Gastroenterology 2022年第32期28卷 4620-4634页

作者： Ashwaq Hamid Salem Yehya Ayappa V Subramaniam Muhammad Asif Gurjeet Kaur Amin M S Abdul Majid chern ein oon Institute for Research in Molecular Medicine Universiti Sains MalaysiaPenang 11800Malaysia Cancer Research Eman BiodiscoveriesKedah 08000Malaysia Department of Pharmacology Faculty of PharmacyThe Islamia University of BahawalpurPunjab 63100Pakistan Department of Cancer Biology and Therapeutics The John Curtin School of Medical ResearchAustralia 2601Australia

BACKGROUND Pancreatic cancer is the most aggressive cancer *** is the first line chemo-drug used for pancreatic cancer but exerts a broad spectrum of organ toxicities and adverse effects in *** To evaluate the anti-tumour activity and toxicological effects of Orthosiphon stamineus extract formulation(ID:C5EOSEW5050ESA trademarked as Nuvastatic^(TM)),and gemcitabine combination on pancreatic xenograft *** Mice were randomly divided into six groups of 6 mice each(n=6)and given different treatments for 28 *** study design consisted of a 2 x 3 factorial treatment structure,with gemcitabine(yes/no)by oral(at 1200 and 400 mg/kg per day).Human pancreatic cancer cells were injected subcutaneously into the flanks of athymic nude mice.C5EOSEW5050ESA(200 or 400 mg/kg per day)was administered orally,while gemcitabine(10 mg/kg per 3 d)was given intraperitoneally either alone or in combination *** analyses of vital organs,tumour tissues,and incidence of lethality were *** of tumour necrosis and proliferation were determined by haematoxylin-eosin staining and immunohistochemistry for Ki-67,*** No signs of toxicity or damage to vital organs were observed in all treatment groups compared to the untreated group.C5EOSEW5050ESA at 200 mg/kg and gemcitabine combination had no additive antitumor effects compared to a single ***,a comparably greater response in a reduction in tumour growth,Ki-67 protein expression,and necrosis was demonstrated by 400 mg/kg of C5EOSEW5050ESA and gemcitabine combination than that of the individual *** These results highlighted the synergistic activity of C5EOSEW5050ESA with gemcitabine to reduce pancreatic tumour growth in mice compared to a single ***,this study provides valuable insights into using C5EOSEW5050ESA as a complementary treatment with gemcitabine for pancreatic cancer.

关键词： Pancreatic cancer Orthosiphon stamineus C5EOSEW5050ESA Gemcitabine Complementary medicine

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BZD9L1 benzimidazole analogue hampers colorectal tumor progression by impeding angiogenesis

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World Journal of Gastrointestinal Oncology 2023年第5期15卷 810-827页

作者： chern ein oon Ayappa V Subramaniam Lik Yang Ooi Ashwaq Hamid Salem Yehya Yeuan Ting Lee Gurjeet Kaur Sreenivasan Sasidharan Beiying Qiu Xiaomeng Wang Institute for Research in Molecular Medicine Universiti Sains MalaysiaPenang 11800Malaysia Cancer Research Eman BiodiscoveriesKedah 08000Malaysia Vatche and Tamar Division of Digestive Diseases Department of MedicineDavid Geffen School of Medicine at University of California Los AngelesLos AngelesCA 90095United States Academic Clinical Program Duke-NUS Medical SchoolNational University of SingaporeSingapore 169857Singapore Singapore National Eye Centre Singapore Eye Research InstituteSingapore 168751Singapore

BACKGROUND The development of new vasculatures(angiogenesis)is indispensable in supplying oxygen and nutrients to fuel tumor *** dysregulation in the tumor vasculature is critical to colorectal cancer(CRC)***(SIRT)enzymes are highly expressed in blood ***9L1 benzimidazole analogue is a SIRT 1 and 2 inhibitor with reported anticancer activities in ***,its role has yet to be explored in CRC tumor *** To investigate the anti-angiogenic potential of BZD9L1 on endothelial cells(EC)in vitro,ex vivo and in HCT116 CRC xenograft in vivo *** ***926 EC were treated with half inhibitory concentration(IC50)(2.5μM),IC50(5.0μM),and double IC50(10.0μM)of BZD9L1 and assessed for cell proliferation,adhesion and SIRT 1 and 2 protein ***,2.5μM and 5.0μM of BZD9L1 were employed in downstream in vitro assays,including cell cycle,cell death and sprouting in *** effect of BZD9L1 on cell adhesion molecules and SIRT 1 and 2 were assessed via real-time quantitative polymerase chain reaction(qPCR).The growth factors secreted by EC post-treatment were evaluated using the Quantibody Human Angiogenesis *** co-culture with HCT116 CRC cells was performed to investigate the impact of growth factors modulated by BZD9L1-treated EC on *** effect of BZD9L1 on sprouting impediment and vessel regression was determined using mouse ***116 cells were also injected subcutaneously into nude mice and analyzed for the outcome of BZD9L1 on tumor necrosis,Ki67 protein expression indicative of proliferation,cluster of differentiation 31(CD31)and CD34 EC markers,and SIRT 1 and 2 genes via hematoxylin and eosin,immunohistochemistry and qPCR,*** BZD9L1 impeded EC proliferation,adhesion,and spheroid sprouting through the downregulation of intercellular adhesion molecule 1,vascular endothelial cadherin,integrin-alpha V,SIRT1 and SIRT2 *** compound also arrested the cells at G1 phase and i

关键词： Colorectal cancer BZD9L1 Sirtuin Benzimidazole Angiogenesis

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Mesuaferrea stem bark extract induces apoptosis and inhibits metastasis in human colorectal carcinoma HCT 116 cells, through modulation of multiple cell signalling pathways

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Chinese Journal of Natural Medicines 2017年第7期15卷 505-514页

作者： Muhammad Asif Armaghan Shafaei Aman Shah Abdul Majid Mohammed Oday Ezzat Saad S Dahham Mohamed B.Khadeer Ahamed chern ein oon Amin Malik Shah Abdul Majid EMAN Testing and Research Laboratory Department of Pharmacology School of Pharmaceutical Sciences Universiti Sains Malaysia Penang 11800 Malaysia Department of Pharmaceutical Chemistry School of Pharmaceutical Sciences Universiti Sains Malaysia Penang 11800 Malaysia Department of Pharmacology School of Medical Sciences Quest International University Perak Malaysia Centre for Drug Research Universiti Sains Malaysia Penang 11800 Malaysia Institute for Research in Molecular Medicine (INFORMM) Universiti Sains Malaysia Penang 11800 Malaysia

Considering the great potential of natural products as anticancer agents, the present study was designed to explore the molecular mechanisms responsible for anticancer activities of Mesua ferrea stem bark extract against human colorectal carcinoma. Based on MTT assay results, bioactive sub-fraction(SF-3) was selected for further studies using HCT 116 cells. Repeated column chromatography resulted in isolation of less active α-amyrin from SF-3, which was identified and characterized by GC-MS and HPLC methods. α-amyrin and betulinic acid contents of SF-3 were measured by HPLC methods. Fluorescent assays revealed characteristic apoptotic features, including cell shrinkage, nuclear condensation, and marked decrease in mitochondrial membrane potential in SF-3 treated cells. In addition, increased levels of caspases-9 and-3/7 levels were also observed in SF-3 treated cells. SF-3 showed promising antimetastatic properties in multiple in vitro assays. Multi-pathway analysis revealed significant down-regulation of WNT, HIF-1α, and EGFR with simultaneous up-regulation of p53, Myc/Max, and TGF-β signalling pathways in SF-3 treated cells. In addition, promising growth inhibitory effects were observed in SF-3 treated HCT 116 tumour spheroids, which give a hint about in vivo antitumor efficacy of SF-3 phytoconstituents. In conclusion, these results demonstrated that anticancer effects of SF-3 towards colon cancer are through modulation of multiple molecular pathways.

关键词： Mesua ferrea a-Amyrin Apoptotic Antimetastatic Molecular pathways

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