Synthesis and biological evaluation of novel H6 analogues as drug resistance reversal agents

Wang, Xiao; Ren, Qian wen; Liu, Xian xuan; Yang, Yan; Wang, Bing hua; Zhai, R. Grace; Qi, Jia; Tian, Jing wei; Wang, Hong Bo; Bi, Yi

doi:10.1016/j.ejmech.2018.10.033

Cited by 19 publications

(15 citation statements)

References 25 publications

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“…e CDIO concept is the latest achievement of the international engineering education reform in recent years. It originated from an engineering education reform plan initiated in 2000 by four engineering and technical schools including the Massachusetts Institute of Technology (MIT) and the KTH Royal Institute of Technology [6]. e basic CDIO education model consists of four basic links: conceive, design, implement, and operate.…”

Section: Cdio Conceptmentioning

confidence: 99%

On English Courses and Teaching Strategies in Compound Application-Oriented Talents Training Based on the Education Ideas of CDIO in the Construction of Smart Cities

Xie

2022

Security and Communication Networks

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To improve the level of English education in China and promote the cultivation of compound application-oriented talents in colleges and universities, this research integrates the concept of conceive design implement operate (CDIO) into college English education. First, the CDIO educational concept is introduced in detail. Second, the moth-flame optimization (MFO) algorithm and the support vector machine (SVM) model by the MFO algorithm are presented, and they are applied to teaching evaluation, and then the teaching plan is proposed by the CDIO concept. The teaching evaluation model is applied to the English teaching of students in class A with ordinary learning levels in a university in Hengyang City. The implementation method of the teaching plan is explained in detail by taking “Unit 2 Charlie Chaplin” in the textbook “New Horizons College English” as an example. Finally, the accuracy of the MFO-SVM model for teaching evaluation is verified by simulation analysis, and the corresponding teaching strategies are summarized through teaching evaluation and customization of teaching plans. The experimental results reveal that the MFO-SVM model has an accuracy of 96.43% in teaching evaluation, while the extreme learning machine (ELM), SVM, and back propagation neural network (BPNN) models have an accuracy of 92.27%, 90.45%, and 86.36%, respectively in the evaluation results of the teaching quality. The summarized teaching strategies are mainly divided into four parts, namely, autonomous learning, project-based teaching, dynamic generation and information feedback, and production teaching. This research has a certain reference for the current reform of English education in China and the cultivation of compound application-oriented talents.

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Section: Cdio Conceptmentioning

confidence: 99%

On English Courses and Teaching Strategies in Compound Application-Oriented Talents Training Based on the Education Ideas of CDIO in the Construction of Smart Cities

Xie

2022

Security and Communication Networks

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“…The most active derivative 122 increased the chemosensitivity of KBV cells towards paclitaxel at larger extent than 121 and the standard P-gp modulators verapamil ( 1 ), tariquidar ( 10 ) and zosuquidar ( 11 ). In vivo assay revealed that 122 also enhanced the efficacy of paclitaxel against KBV cancer cell-derived xenograft tumors ( Table 14 ) [ 139 ].…”

Section: Terpenesmentioning

confidence: 99%

Overcoming Multidrug Resistance: Flavonoid and Terpenoid Nitrogen-Containing Derivatives as ABC Transporter Modulators

2020

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Multidrug resistance (MDR) in cancer is one of the main limitations for chemotherapy success. Numerous mechanisms are behind the MDR phenomenon wherein the overexpression of the ATP-binding cassette (ABC) transporter proteins P-glycoprotein (P-gp), breast cancer resistance protein (BCRP) and multidrug resistance protein 1 (MRP1) is highlighted as a prime factor. Natural product-derived compounds are being addressed as promising ABC transporter modulators to tackle MDR. Flavonoids and terpenoids have been extensively explored in this field as mono or dual modulators of these efflux pumps. Nitrogen-bearing moieties on these scaffolds were proved to influence the modulation of ABC transporters efflux function. This review highlights the potential of semisynthetic nitrogen-containing flavonoid and terpenoid derivatives as candidates for the design of effective MDR reversers. A brief introduction concerning the major role of efflux pumps in multidrug resistance, the potential of natural product-derived compounds in MDR reversal, namely natural flavonoid and terpenoids, and the effect of the introduction of nitrogen-containing groups are provided. The main modifications that have been performed during last few years to generate flavonoid and terpenoid derivatives, bearing nitrogen moieties, such as aliphatic, aromatic and heterocycle amine, amide, and related functional groups, as well as their P-gp, MRP1 and BCRP inhibitory activities are reviewed and discussed.

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“…1-Hydroxybenzotriazole is a widely-used coupling reagent along with carbodiimides used mostly in amide and ester synthesis [ 11 , 12 ]. While this reagent is mainly used to form intermediate active esters of various natural compounds that further react to form final amides or esters, several studies reported the biological assessment of various 1-hydroxybenzotriazole-triterpene esters, some of which exhibited higher biological effects as opposed to unmodified triterpenes [ 13 , 14 , 15 , 16 , 17 ]. Therefore, 1-hydroxybenzotriazole is a reagent that can be easily used to obtain triazole-containing triterpene esters, with potential increased biological potential.…”

Section: Introductionmentioning

confidence: 99%

Novel Triterpenic Acid—Benzotriazole Esters Act as Pro-Apoptotic Antimelanoma Agents

Mioc

Prodea

et al. 2022

IJMS

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Pentacyclic triterpenes, such as betulinic, ursolic, and oleanolic acids are efficient and selective anticancer agents whose underlying mechanisms of action have been widely investigated. The introduction of N-bearing heterocycles (e.g., triazoles) into the structures of natural compounds (particularly pentacyclic triterpenes) has yielded semisynthetic derivatives with increased antiproliferative potential as opposed to unmodified starting compounds. In this work, we report the synthesis and biological assessment of benzotriazole esters of betulinic acid (BA), oleanolic acid (OA), and ursolic acid (UA) (compounds 1–3). The esters were obtained in moderate yields (28–42%). All three compounds showed dose-dependent reductions in cell viability against A375 melanoma cells and no cytotoxic effects against healthy human keratinocytes. The morphology analysis of treated cells showed characteristic apoptotic changes consisting of nuclear shrinkage, condensation, fragmentation, and cellular membrane disruption. rtPCR analysis reinforced the proapoptotic evidence, showing a reduction in anti-apoptotic Bcl-2 expression and upregulation of the pro-apoptotic Bax. High-resolution respirometry studies showed that all three compounds were able to significantly inhibit mitochondrial function. Molecular docking showed that compounds 1–3 showed an increase in binding affinity against Bcl-2 as opposed to BA, OA, and UA and similar binding patterns compared to known Bcl-2 inhibitors.

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Synthesis and biological evaluation of novel H6 analogues as drug resistance reversal agents

Cited by 19 publications

References 25 publications

On English Courses and Teaching Strategies in Compound Application-Oriented Talents Training Based on the Education Ideas of CDIO in the Construction of Smart Cities

On English Courses and Teaching Strategies in Compound Application-Oriented Talents Training Based on the Education Ideas of CDIO in the Construction of Smart Cities

Overcoming Multidrug Resistance: Flavonoid and Terpenoid Nitrogen-Containing Derivatives as ABC Transporter Modulators

Novel Triterpenic Acid—Benzotriazole Esters Act as Pro-Apoptotic Antimelanoma Agents

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