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Acta Pharmaceutica Sinica B ; (6): 1686-1695, 2021.
Article in English | WPRIM | ID: wpr-888829


As a serine hydrolase, monoacylglycerol lipase (MAGL) is principally responsible for the metabolism of 2-arachidonoylglycerol (2-AG) in the central nervous system (CNS), leading to the formation of arachidonic acid (AA). Dysfunction of MAGL has been associated with multiple CNS disorders and symptoms, including neuroinflammation, cognitive impairment, epileptogenesis, nociception and neurodegenerative diseases. Inhibition of MAGL provides a promising therapeutic direction for the treatment of these conditions, and a MAGL positron emission tomography (PET) probe would greatly facilitate preclinical and clinical development of MAGL inhibitors. Herein, we design and synthesize a small library of fluoropyridyl-containing MAGL inhibitor candidates. Pharmacological evaluation of these candidates by activity-based protein profiling identified

Article in English | WPRIM | ID: wpr-629047


Introduction: Both kenaf (Hibiscus cannabinus) and roselle (Hibiscus sabdariffa) belong to the Malvaceae family. Method: In this study, the phytochemical analysis and anti-inflammatory activity of kenaf seed oil (KSO), kenaf seed extract (KSE), roselle seed oil (RSO) and roselle seed extract (RSE) were investigated. Results:The flavonoids content present in the roselle seed oil (RSO), roselle seed extract (RSE), kenaf seed oil (KSO) and kenaf seed extract (KSE) ranged from 52.94±7.31 mg catechin/100g of sample (KSE) to 290.05±12.04 mg catechin/100 g of (RSE); phenolic content ranged from 108.46±6.40mg GAE/ 100g of sample (RSO) to 229.65±7.91 mg GAE/ 100g of sample (RSE); saponin content ranged from 68.14±3.46 mg saponin/ 100 g of sample (KSO) to 98.50±2.44 mg saponin/ 100g of sample (RSE); terpenoid content ranged from 148.76±9.69 mg linaloo1/100g of sample (KSO) to 294.74±16.14 mg linaloo1/100g of sample (RSE); and alkaloid content ranged from 17.40±1.346%/g (KSO) to 46.95±1.792%/g (RSE). The results showed that KSE, RSO and RSE significantly inhibited (p<0.05) inflammation compared to the control. Conclusion: The present study demonstrates that KSE, RSO and RSE exhibit potent anti-inflammatory property and offer potential for use as a therapeutic regiment in managing inflammatory conditions.

Article in Chinese | WPRIM | ID: wpr-409845


To study effects of arachidonic acid (AA) on the growth and differentiation of rat adipocytes, a cells culture system of rat primary preadipocytes was established. The cells treated by different concentration of AA supplemented based on DMEM medium containing 10% fetal bovine serum. Cell proliferation was measured by trypan blue exclusion and methyl thiazolyl tetrazolium (MTT) assay method. Hoechst33342 fluorescence staining observed AA induced morphological changes. Oil Red O staining extraction assay assess the degree of adipogenesis and differentiation, and cyclooxygenases-2(COX-2) mRNA were detected by reverse transcriptase-polymerase chain reaction (RT-PCR). The results showed that rat preadipocytes treated with 120 μmol/L AA for 24-72 hours remarkably promoted the cells proliferation compared with control, 160 μmol/L AA treated for 48 hours could induce apoptosis of preadipocytes. 40, 80 μmol/L AA decreased the fat content in cells at 72 hours, and 40 μmol/L AA significantly up-regulated the expression of COX-2 mRNA at 24 hours. This results indicate that AA regulate adipocytes proliferation and differentiation depended on treatment time and concentration. 40-80 μmol/L AA maybe useful to control body fat, which may be associated with the increase of COX-2 mRNA.