Design, Synthesis, Characterization, and Antiproliferative Activity of Organoplatinum Compounds Bearing a 1,2,3-Triazole Ring

Singh, Khushwant; Gangrade, Ankit; Jana, Achintya; Mandal, Biman B.; Das, Neeladri

doi:10.1021/acsomega.8b02849

Cited by 64 publications

(60 citation statements)

References 34 publications

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“… a Concentration that inhibits cell viability by 50%. b Selectivity index = IC 50 of normal cells/IC 50 of cancer cells [ 28 ] …”

Section: Resultsmentioning

confidence: 99%

“…In addition, AA exhibits greater cytotoxicity in cancer cells than normal bronchial epithelial cells, with an approximately 2-fold selectivity index. The greater number is considered a higher selectivity for cancer cells [ 28 ]. Since Bcl-2 family proteins play important roles in the regulation of apoptosis, a type of programmed cell death, the balance of anti- and pro-apoptotic proteins determine the fate of the cells [ 35 ].…”

Section: Discussionmentioning

confidence: 99%

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Antitumor activities of Aspiletrein A, a steroidal saponin from Aspidistra letreae, on non-small cell lung cancer cells

Nguyen

Seephan

et al. 2021

BMC Complement Med Ther

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Background Lung cancer is one of the leading causes of death worldwide due to its strong proliferative and metastatic capabilities. The suppression of these aggressive behaviors is of interest in anticancer drug research and discovery. In recent years, many plants have been explored in order to discover new bioactive secondary metabolites to treat cancers or enhance treatment efficiency. Aspiletrein A (AA) is a steroidal saponin isolated from the whole endemic species Aspidistra letreae in Vietnam. Previously, elucidation of the structure of AA and screening of its cytotoxic activity against several cancer cell lines were reported. However, the antitumor activities and mechanisms of action have not yet been elucidated. In this study, we demonstrated the anti-proliferative, anti-migrative and anti-invasive effects of AA on H460, H23 and A549 human lung cancer cells. Methods MTT, wound healing and Transwell invasion assays were used to evaluate the anti-proliferation, anti-migration and anti-invasion effects of AA, respectively. Moreover, the inhibitory effect of AA on the activity of protein kinase B (Akt), a central mediator of cancer properties, and apoptotic regulators in the Bcl-2 family proteins were investigated by Western blotting. Results AA exhibits antimetastatic effects in human lung cancer cells through the inhibition of the pAkt/Akt signaling pathway, which in turn resulted in a significant inhibitory effect of AA on the migration and invasion of the examined lung cancer cells. Conclusions Aspiletrein A may be a potent inhibitor of protein kinase B (Akt). Hence, AA could be further explored as a potential antimetastatic lead compound.

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“… a Concentration that inhibits cell viability by 50%. b Selectivity index = IC 50 of normal cells/IC 50 of cancer cells [ 28 ] …”

Section: Resultsmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Antitumor activities of Aspiletrein A, a steroidal saponin from Aspidistra letreae, on non-small cell lung cancer cells

Nguyen

Seephan

et al. 2021

BMC Complement Med Ther

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“…The stats indicate that all the synthesised compounds were at least thrice times more toxic than cisplatin against MG-63, MDA-MB-231, and HDF cell lines, and the compound with highest toxicity was 51. 90 Notably, the additional potentially active compound 52 possessing 3-(tert-butoxycarbonylamino)phenyl-substituted triazole moiety not only exhibited obviously improved IC 50 values ranging from 0.7 to 1.2 mM against a panel of tested cancer cells but also showed very weak cytotoxicity on normal cells. Preliminary mechanistic studies indicated that compound 52 could induce apoptosis in MDA-MB-231 cells and was worth developing into a novel natural product-like anticancer agent by proper structural modication.…”

Section: Introductionmentioning

confidence: 97%

CuAAC-ensembled 1,2,3-triazole-linked isosteres as pharmacophores in drug discovery: review

et al. 2020

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“…The SI value reflects selectivity, where a higher SI indicates more selective cytotoxicity. An SI value lower than 2 indicates either low selectivity [ 48 ] or general toxicity [ 49 ]. Values higher than 2 indicate selectivity.…”

Section: Discussionmentioning

confidence: 99%

Comparison of Chemical Composition and Biological Activities of Eight Selaginella Species

et al. 2020

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Selaginella P. Beauv. is a group of vascular plants in the family Selaginellaceae Willk., found worldwide and numbering more than 700 species, with some used as foods and medicines. The aim of this paper was to compare methanolic (MeOH) and dichloromethane (DCM) extracts of eight Selaginella species on the basis of their composition and biological activities. Six of these Selaginella species are underinvestigated. Using ultra-high performance liquid chromatography–high-resolution mass spectrometry (UHPLC–HRMS) analysis, we identified a total of 193 compounds among the tested Selaginella species, with flavonoids predominating. MeOH extracts recovered more constituents that were detected, including selaginellins, the occurrence of which is only typical for this plant genus. Of all the tested species, Selaginellaapoda contained the highest number of identified selaginellins. The majority of the compounds were identified in S. apoda, the fewest compounds in Selaginellacupressina. All the tested species demonstrated antioxidant activity using oxygen radical absorption capacity (ORAC) assay, which showed that MeOH extracts had higher antioxidant capacity, with the half maximal effective concentration (EC50) ranging from 12 ± 1 (Selaginellamyosuroides) to 124 ± 2 (Selaginellacupressina) mg/L. The antioxidant capacity was presumed to be correlated with the content of flavonoids, (neo)lignans, and selaginellins. Inhibition of acetylcholinesterase (AChE) was mostly discerned in DCM extracts and was only exhibited in S. myosuroides, S. cupressina, Selaginellabiformis, and S. apoda extracts with the half maximal inhibitory concentration (IC50) in the range of 19 ± 3 to 62 ± 1 mg/L. Substantial cytotoxicity against cancer cell lines was demonstrated by the MeOH extract of S. apoda, where the ratio of the IC50 HEK (human embryonic kidney) to IC50 HepG2 (hepatocellular carcinoma) was 7.9 ± 0.2. MeOH extracts inhibited the production of nitrate oxide and cytokines in a dose-dependent manner. Notably, S. biformis halved the production of NO, tumor necrosis factor (TNF)-α, and interleukin (IL)-6 at the following concentrations: 105 ± 9, 11 ± 1, and 10 ± 1 mg/L, respectively. Our data confirmed that extracts from Selaginella species exhibited cytotoxicity against cancer cell lines and AChE inhibition. The activity observed in S. apoda was the most promising and is worth further exploration.

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Design, Synthesis, Characterization, and Antiproliferative Activity of Organoplatinum Compounds Bearing a 1,2,3-Triazole Ring

Cited by 64 publications

References 34 publications

Antitumor activities of Aspiletrein A, a steroidal saponin from Aspidistra letreae, on non-small cell lung cancer cells

Antitumor activities of Aspiletrein A, a steroidal saponin from Aspidistra letreae, on non-small cell lung cancer cells

CuAAC-ensembled 1,2,3-triazole-linked isosteres as pharmacophores in drug discovery: review

Comparison of Chemical Composition and Biological Activities of Eight Selaginella Species

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