Synthesis of novel ring-contracted artemisinin dimers with potent anticancer activities

Zhang, Ning; Yu, Zhimei; Yang, Xiaohong; Hu, Ping; He, Yun

doi:10.1016/j.ejmech.2018.03.010

Cited by 26 publications

(6 citation statements)

References 47 publications

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“…Several anticancer drugs usually result in the course of cell cycle arrest at a particular checkpoint, which results in the induction of the apoptotic process. [46][47][48][49] To evaluate the cell cycle profile of HT-1080 cells after treatment with the selected compounds, we performed cell cycle analysis by flow cytometry. For this study, HT-1080 cells were incubated with 10 μM of the compounds 2 b and 7 b for 24 hours (Figure 5).…”

Section: Investigation Of Cell Cyclementioning

confidence: 99%

Synthesis and Biological Evaluation of Novel Thiazole Analogs with Both Anti‐Proliferative and Mechanistic Analyses and Molecular Docking Studies

et al. 2022

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Herein, we report the synthesis of a novel series of βhimachalene derivatives, including semicarbazones, thiosemicarbazones, and thiazoles. The structures of these compounds were elucidated by NMR, IR, and HRMS analysis methods. The in vitro antitumor activity of these compounds was evaluated by the MTT assay against four human cancer cell lines, such as fibrosarcoma (HT-1080), breast adenocarcinoma (MCF-7 and MDA-MB-231), and lung carcinoma (A-549), and the results indicated that all compounds showed moderate to significant cytotoxic activities against all cancer cell lines with IC 50 values ranging from 7.19 � 0.30 to 50 μM. The mechanism of action of the most cytotoxic compounds 2 b and 7 b suggested that they induced apoptosis through caspase-3/7 activation, and elicited G2/M-phase arrest with the loss of mitochondrial membrane potential in HT-1080 cells. The molecular docking showed that compounds 2 b and 7 b activated the caspase-3 by forming a stable protein-ligand complex.

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Section: Investigation Of Cell Cyclementioning

confidence: 99%

Synthesis and Biological Evaluation of Novel Thiazole Analogs with Both Anti‐Proliferative and Mechanistic Analyses and Molecular Docking Studies

et al. 2022

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“…Malaria is a serious parasitic disease that has been spreading all over the world but mainly in Africa [ 1 ]. Artemisinin (ART), a peroxide-containing sesquiterpene lactone [ 2 , 3 ], is currently the most widely used and most effective anti-malarial drug [ 4 , 5 ].…”

Section: Introductionmentioning

confidence: 99%

Electrospun Nanofibers of Polycaprolactone/Collagen as a Sustained-Release Drug Delivery System for Artemisinin

et al. 2021

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The application of artemisinin (ART) in the treatment of malaria has been restricted to a certain degree due to its inherent limitations, such as short half-life, poor solubility, limited bioavailability, and re-crystallization. Electrospun nanofibers loaded with ART provide an excellent solution to these limitations and yield sustained drug release as well as inhibition of drug re-crystallization. In this study, ART-loaded polycaprolactone (PCL)/collagen (Col) nanofibers with different proportions of polymers were prepared. ART-loaded PCL/Col nanofibers were characterized, and further ART anti-crystallization and release behaviors were studied. SEM was used to observe the morphology of PCL/Col nanofibers. X-ray diffraction (XRD) was used to characterize the physical state of ART in ART-loaded PCL/Col nanofibers. Fourier transform infrared spectroscopy (FTIR), water contact angle measurement, weight loss, degree of swelling, and drug release experiments can verify the differences in performance of ART-loaded PCL/Col nanofibers due to different polymer ratios. The release curve was analyzed by kinetics, showing sustained release for up to 48 h, and followed the Fickian release mechanism, which was shown by the diffusion index value obtained from the Korsmeyer-Peppas equation.

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“…The ring‐contracted ART dimer 48 (IC 50 : 1.56–6.61 µM, MTT assay) demonstrated decent activity against A375, A549, SH‐SY5Y, HCT116, and PC12 cancer cell lines, and the SAR illustrated that the phosphate linker was critical for the activity. [ 81 ] Mechanistically, dimer 48 arrested cell cycle at G1 phase and induced cell apoptosis via upregulation of Bad, Bax, caspase‐3, and caspase‐9 protein expressions while inhibiting the expression of Bcl‐xL. Moreover, dimer 48 exhibited moderate metabolic stability compared to clozapine and testosterone.…”

Section: Art Dimersmentioning

confidence: 99%

The current scenario on anticancer activity of artemisinin metal complexes, hybrids, and dimers

Zhang

et al. 2022

Archiv der Pharmazie

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Cancer, the most significant cause of morbidity and mortality, has already posed a heavy burden on health care systems globally. In recent years, cancer treatment has made a significant breakthrough, but cancer cells inevitably acquire resistance, and the efficacy of the treatment is greatly reduced as the tumor progresses. To overcome the above issues, novel chemotherapeutics are needed urgently.Artemisinin and its derivatives-sesquiterpene lactone compounds possessing a unique peroxy bridge moiety-exhibit excellent safety and tolerability profiles. Mechanistically, artemisinin derivatives can promote cancer cell apoptosis, induce cell cycle arrest and autophagy, and inhibit cancer cell invasion and migration. Accordingly, artemisinin derivatives demonstrate promising anticancer efficacy both in vitro and in vivo, and even in clinical Phase I/II trials. The purpose of the present review article is to provide an emphasis on the current scenario (January 2017-January 2022) of artemisinin derivatives with potential anticancer activity, inclusive of artemisinin metal complexes, hybrids, and dimers. The structure-activity relationships and mechanisms of action are also discussed to facilitate the further rational design of more effective candidates.

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Synthesis of novel ring-contracted artemisinin dimers with potent anticancer activities

Cited by 26 publications

References 47 publications

Synthesis and Biological Evaluation of Novel Thiazole Analogs with Both Anti‐Proliferative and Mechanistic Analyses and Molecular Docking Studies

Synthesis and Biological Evaluation of Novel Thiazole Analogs with Both Anti‐Proliferative and Mechanistic Analyses and Molecular Docking Studies

Electrospun Nanofibers of Polycaprolactone/Collagen as a Sustained-Release Drug Delivery System for Artemisinin

The current scenario on anticancer activity of artemisinin metal complexes, hybrids, and dimers

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