ABSTRACT
OBJECTIVE: To investigate the nutritional content of edible medicinal materials in mountainous areas of Guizhou Province and compare the comprehensive nutritional value of different varieties. METHODS: A total of 15 kinds of edible herbs were collected from Guizhou Province. According to the national standard, direct drying method, Kjeldahl nitrogen determination method, Soxhlet extraction method, high performance liquid chromatography, inductively coupled plasma mass spectrometry and other detection method were used to determine the content of general nutrients, fat soluble vitamins, minerals and ash. According to the weight ranking of nutritional indexes in principal component analysis and membership function analysis, the quality of 9 kinds of food and drug substances and 6 kinds of Chinese medicinal materials were evaluated and ranked. RESULTS: The eigenvalues of the first 4 principal components were greater than 1, and the cumulative contribution rate was 82.32%. Compared with membership function analysis, the top 5 in comprehensive evaluation were Eucommia, Epimedium and honeysuckle, all of which were food and drug substances. The contents of calcium(851.69 mg/100 g), phosphorus(270.22 mg/100 g) and potassium(1446.48 mg/100 g) were the highest. The contents of carotene(21 963.87 µg/100 g) and vitamin E(57.82 mg/100 g) were the highest in the fat-soluble vitamins of Herbimedium. The contents of various indexes of honeysuckle were relatively high. CONCLUSION: Food and pharmaceutical substances have both medicinal value and nutritional value, and the overall nutritional benefit is higher than that of Chinese medicinal materials.
Subject(s)
Nutritive Value , China , Plants, Medicinal/chemistry , Plants, Edible/chemistry , Food Analysis , Phosphorus/analysis , Altitude , Drugs, Chinese Herbal/analysis , Minerals/analysisABSTRACT
Raptor, a regulatory-associated protein of mTOR, has been genetically proved to be an important regulator in lipogenesis. However, its druggable potential is rarely investigated, largely due to the lack of an inhibitor. In this study, the antiadipogenic screening of a daphnane diterpenoid library followed by target fishing led to the identification of a Raptor inhibitor, 1c (5/7/6 carbon ring with orthoester and chlorine functionalities). Pharmacodynamic studies verified that 1c is a potent and tolerable antiadipogenic agent in vitro and in vivo. Mechanistic studies revealed that the targeting of Raptor by 1c could block the formation of mTORC1 and then downregulate the downstream S6K1- and 4E-BP1-mediated C/EBPs/PPARγ signaling, eventually retarding adipocyte cell differentiation at the early stage. These findings suggest that Raptor can be explored as a novel therapeutic target for obesity and its related complications, and 1c as the first Raptor inhibitor may provide a new therapeutic option for these conditions.
Subject(s)
Multiprotein Complexes , Phosphoproteins , Regulatory-Associated Protein of mTOR/metabolism , Phosphoproteins/metabolism , Phosphorylation , Multiprotein Complexes/metabolism , Mechanistic Target of Rapamycin Complex 1/metabolism , Transcription Factors/metabolismABSTRACT
Euphohyrisnoids A (1) and B (2), two highly rearranged lathyrane diterpenoids featuring a unique tetracyclo[10.2.2.01,10.03,7]cetane and tricyclo[8.4.1.03,7]pentadecane skeleton, respectively, were isolated from the seeds of Euphorbia lathyris. Their structures were determined by detailed spectroscopic analysis and were further confirmed by single-crystal X-ray diffraction. 1 significantly inhibited adipogenesis in 3T3-L1 adipocytes by retarding cell differentiation at the early stage.
Subject(s)
EuphorbiaABSTRACT
Phytochemical investigation of the leaves and twigs of Croton yanhuii led to the isolation of seven highly modified nor-clerodane diterpenoids (1-7), including three new ones, croyanoids A-C (1-3), along with four known analogues (4-7). Compound 1 incorporates a 5,12-epoxy ring, forming a unique cage-like, 6/6/6/5-fused tetracyclic ring system. Their structures were established by extensive spectroscopic analysis, and the absolute configurations of 1-4 were determined by a combination of circular dichroism (CD) analysis and single-crystal X-ray diffraction. All compounds were tested in an array of bioassays, but were inactive. Crotoeurin A (7), a nor-clerodane dimer with a high yield of 0.2 isolated in current study, was considered as a chemotaxonomic marker for this species.
Subject(s)
Croton/chemistry , Diterpenes, Clerodane/chemistry , 3T3-L1 Cells , A549 Cells , Animals , China , Diterpenes, Clerodane/isolation & purification , Humans , Mice , Molecular Structure , Nitric Oxide , Phytochemicals/chemistry , Phytochemicals/isolation & purification , Plant Leaves/chemistry , RAW 264.7 CellsABSTRACT
Crotonpenoids A (1) and B (2), two highly modified clerodane diterpenoids featuring a new 10-(butan-2-yl)-1,6,12-trimethyltricyclo[7.2.1.02,7]dodecane skeleton, were isolated from the leaves and twigs of Croton yanhuii. Their structures including the absolute configurations were determined by spectroscopic analysis, single-crystal X-ray diffraction, and biomimetic semisynthesis. Compounds 1 and 2 exhibited an agonistic effect on pregnane X receptor at 10 µM.