| Animal Research: |
| Phytomedicine. 2013 May 15;20(7):571-6. | | Antihyperglycemic and sub-chronic antidiabetic actions of morolic and moronic acids, in vitro and in silico inhibition of 11β-HSD 1.[Pubmed: 23453304 ] | Morolic acid(1) and moronic acid(2) are the main constituents of acetonic extract from Phoradendron reichenbachianum (Loranthaceae), a medicinal plant used in Mexico for the treatment of diabetes.
METHODS AND RESULTS:
The aim of the current study was to establish the sub-acute antidiabetic and antihyperlipidemic effects of compounds 1 and 2 over non insulin-dependent diabetic rat model. Also, to determine the antihyperglycemic action on normoglycemic rats by oral glucose tolerance test. Daily-administered Morolic acid(1) and moronic acid (2)(50 mg/kg) significantly lowered the blood glucose levels at 60% since first day until tenth day after treatment than untreated group (p<0.05). Moreover, analyzed blood samples obtained from diabetic rats indicated that both compounds diminished plasmatic concentration of cholesterol (CHO) and triglycerides (TG), returning them to normal levels (p<0.05). Also, pretreatment with 50 mg/kg of each compound induced significant antihyperglycemic effect after glucose and sucrose loading (2 g/kg) compared with control group (p<0.05). In vitro studies showed that compounds 1 and 2 induced inhibition of 11β-HSD 1 activity at 10 μM. However, in silico analysis of the pentaclyclic triterpenic acids on 11β-HSD 1 revealed that all compounds had high docking scores and important interactions with the catalytic site allowing them to inhibit 11β-HSD 1 enzyme.
CONCLUSIONS:
In conclusion, Morolic acid and moronic acid have shown sustained antidiabetic and antihyperglycemic action possibly mediated by an insulin sensitization with consequent changes of glucose, cholesterol and triglycerides, in part mediated by inhibition of 11β-HSD 1 as indicated by in vitro and in silico studies. |
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| Structure Identification: |
| Zhong Yao Cai. 2015 Jun;38(6):1209-11. | | Chemical Constituents From Rhus chinensis Fruit Dregs.[Pubmed: 26762062] | To isolate and elucidate the constituents from the fruit dregs of Rhus chinensis.
METHODS AND RESULTS:
The constituents were isolated and purified by chromatography on silica gel,Sephadex LH-20, RP-C18 gel and recrystallization. The structures were elucidated on the basis of the chemical evidence and spectroscopic data.
Ten compounds were obtained: β-sitosterol (1), Morolic acid (2), (2S) -1-O-heptatriacontanoyl glycerol (3), α-monpalmitin (4), palmitic acid (5), gallic acid (6), methyl gallate (7), ethyl gallate (8), propyl gallate (9), and protocatechuic acid (10).
CONCLUSIONS:
Compounds 3, 4 and 9 are isolated from the plants of Rhus genus for the first time. | | Tetrahedron, 2009, 65(22):4304-4309. | | Efficient synthesis of morolic acid and related triterpenes starting from betulin.[Reference: WebLink] |
METHODS AND RESULTS:
Morolic acid (1) is a naturally occurring pentacyclic triterpene whose derivatives exhibit promising anti-HIV and other biological activities. An efficient synthesis of 1 has been accomplished in 11 steps with a total yield of 24% starting from betulin. Some related natural triterpenes including moradiol (4), acridocarpusic acid D (5), acridocarpusic acid E (6), and moronic aldehyde (7) have also been synthesized.
CONCLUSIONS:
Biological assay results showed that 1, 5, and 6 exhibited moderate inhibitory activity against glycogen phosphorylase. |
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