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1.
J Nat Prod ; 81(11): 2371-2380, 2018 11 26.
Article in English | MEDLINE | ID: mdl-30381950

ABSTRACT

Fifteen new structurally unique monoterpenoid carbazole alkaloids, including two pairs of epimers (1/2 and 3/4), three pairs of enantiomers (6a/6b, 7a/7b, and 8a/8b), and five optically pure analogues (5, 9-12), were obtained from a 95% aqueous EtOH extract of Murraya microphylla by a combination of bioassay- and LC-MS-guided fractionation procedures. Their structures were established based on NMR and HRESIMS data interpretation. The absolute configuration of compound 1 was determined via X-ray crystallographic data analysis and for all compounds by comparison of experimental and calculated ECD data. Compounds 1-5 were assigned as five new thujane-carbazole alkaloids, and compounds 6-12 as 10 new menthene-carbazole alkaloids linked through an ether or carbon-carbon bond. Compounds 1-12 promoted insulin secretion in the HIT-T15 cell line, 1.9-3.1-fold higher than the gliclazide control at 100 µM.


Subject(s)
Alkaloids/isolation & purification , Alkaloids/pharmacology , Chromatography, Liquid/methods , Insulin/metabolism , Mass Spectrometry/methods , Murraya/chemistry , Alkaloids/chemistry , Carbazoles/chemistry , Carbazoles/isolation & purification , Carbazoles/pharmacology , Cell Line , Crystallography, X-Ray , Humans , Molecular Structure , Terpenes/chemistry , Terpenes/isolation & purification , Terpenes/pharmacology
2.
Zhongguo Zhong Yao Za Zhi ; 43(11): 2339-2344, 2018 Jun.
Article in Chinese | MEDLINE | ID: mdl-29945388

ABSTRACT

Pu-erh tea is a unique post-fermented tea processed from tender leaves of Camellia assamica. Characteristic component puerins were produced during the microbial fermentation process.This study focuses on the therapeutic effect and mechanism of puerinⅠ(P1) in Pu-erh tea on ApoE-/- mice with dyslipidemia and diabetes. It was found that P1 could significantly decreased total cholesterol (TC), triglyceride (TG) and fast blood glucose (FBG), and markedly improved impaired glucose tolerance (IPGTT) and insulin sensitivity (ITT) in hyperlipidemic and hyperglycemic ApoE-/- mice. Further experiments proved that P1 reduced FBG and plasma TG levels by inhibiting intestinal α-glycosidase enzymes activity and by activating low-density lipoprotein receptor respectively. This study confirmed the therapeutic effect and mechanism of P1 on ApoE-/- mice with diabetes and hyperlipidemia. Based on the good efficacy of this compound, P1 could be used as a new drug to treat the disorder of glycolipid metabolism.


Subject(s)
Flavonoids/pharmacology , Lipid Metabolism Disorders/drug therapy , Plant Extracts/pharmacology , Tea/chemistry , Animals , Blood Glucose/analysis , Diabetes Mellitus, Experimental , Glucose Tolerance Test , Glycolipids/metabolism , Hyperlipidemias , Insulin Resistance , Lipid Metabolism , Mice , Mice, Knockout, ApoE , Triglycerides/blood
3.
Zhongguo Zhong Yao Za Zhi ; 43(10): 2118-2122, 2018 May.
Article in Chinese | MEDLINE | ID: mdl-29933680

ABSTRACT

Focal cerebral ischemia reperfusion is an essential process during ischemic stroke. The apoptosis of vascular endothelial cells induced by ischemia/reperfusion (I/R) injury is an important cause for brain injury after focal cerebral ischemia. Longxuetongluo capsule (LTC) has been used for the treatment of ischemic stroke in clinic. However, its underlying action mechanism is still unclear. This study aimed to verify the protective effect and mechanisms of LTC on HUVEC cells against oxygen-glucose deprivation/reoxygenation (OGD/R) injury through MTT, LDH, flow cytometry, AO/EB staining and western blot assays. As a result, OGD/R significantly decreased the viability of HUVEC cells, which was significantly improved by LTC. LDH release assay showed that OGD/R significantly increased the lactate dehydrogenase (LDH) release, and LTC dramatically reduced the OGD/R-induced LDH release. Further mechanism study indicated that LTC dose-dependently inhibited the cleavage of PARP, caspase 3, and caspase 9 induced by OGD/R, suggesting that LTC could inhibit the activation of caspase 3/9 apoptosis pathway in the OGD/R-induced apoptosis of HUVEC cells. In conclusion, LTC could protect HUVEC cells against OGD/R injury by inhibiting the activation of mitochondria-related caspase 3/9 apoptosis pathway.


Subject(s)
Apoptosis/drug effects , Drugs, Chinese Herbal/pharmacology , Endothelial Cells/drug effects , Reperfusion Injury , Cell Survival , Glucose , Humans , Oxygen
4.
Zhongguo Zhong Yao Za Zhi ; 42(11): 2038-2041, 2017 Jun.
Article in Chinese | MEDLINE | ID: mdl-28822144

ABSTRACT

Pu-erh tea has gradually aroused general concern with social development and people's enhanced awareness of health. Pu-erh tea is rich in multiple active constitute such as flavonoids, catechins, phenolic acids, flavanols polymer, purine alkaloids, and hydrolysable tannin as a microbial-fermented tea.It is reported that Pu-erh tea have a variety of pharmacologically activities, such as anti-hyperlipidemic, anti-diabetic, anti-oxidative, anti-tumor, anti-bacterial, anti-inflammatory, and anti-viral effects. In this paper, the main pharmacological effects of Pu-erh tea are reviewed. We wish this work will provide some references and clues for further research of Pu-erh tea.


Subject(s)
Plant Extracts/pharmacology , Tea/chemistry , Fermentation , Humans
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