Twelve novel hybrids of slowly releasing hydrogen sulfide donor ADT-OH combined with nicotinic acid were synthesized. All of their structures had been confirmed by ¹H NMR, ¹³C NMR and MS spectra. The target compounds were evaluated for their neuroprotective effects on hippocampal neuron HT22 cells against glutamate-induced injury at the concentrations of 1-100μM with MTT assay, and their toxicity on HT22 cells untreated by glutamine at the concentration of 100μM. The active compound was further investigated for its effect on ischemic infarct volume by intraperitoneal injection at 3h after ischemia in mice models of permanent middle cerebral artery occlusion (pMCAO). The results showed that all the compounds significantly protected HT22 cells from glutamate-induced damage at most of the experimental concentrations, and had no or little neurotoxicity on normal HT22 cells at the high concentration. More importantly, compound A6 significantly reduced infarct volume in the pMCAO model. These results suggested that compound A6 may be promising for further evaluation for the intervention of cerebral ischemic injury.

01 Dec 2014·Chemical Research in Chinese Universities

Syntheses and anti-cancer activities of derivatives of tetrandrine and fangchinoline

Author: Liu Yazhou ; Zhang Maosheng ; Liang Guangyi ; Sun Qianyun ; LI Tianlei ; Pan Weidong ; Huang Lan

A series of derivatives of tetrandrine and fangchinoline was designed and synthesized to find more active anti-cancer compoundsTheir anti-cancer activities were tested against human hepatocellular carcinoma BEL-7402 and PLC/PRF/5 cells, human lung adenocarcinoma A549 cells as well as human leukemia K562 cells, and the structure-activity relationship(SAR) was also studied.All the compounds except B1 exhibited superior inhibitory activities against PLC/PRF/5 cells with half maximal inhibitory concentration(IC₅₀) values of less than 15 μmol/L, and compounds A2, A4, B2 and B4 showed IC₅₀ values of less than 9 μmol/L.Compounds A2, A6, B2 and B4 showed potent anti-cancer activities against all the tested cells with IC₅₀ values of less than 10 μmol/L.The results show that terandrine and fangchinoline derivatives are potential suppressors to human cancer.

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Indication	Highest Phase	Country/Location	Organization	Date
Neoplasms	Preclinical	China	Chinese Academy of Sciences	07 Nov 2014
Neoplasms	Preclinical	China	Guizhou University	07 Nov 2014

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