1.Advances in research on hypolipidemic mechanism of phytosterols.
Jing-Xia LU ; Zu-Guo ZHENG ; Zhi-Meng XU ; Hua YANG ; Ping LI
China Journal of Chinese Materia Medica 2019;44(21):4552-4559
Hyperlipidemia,as one of the severe risk factors of cardiovascular disease,could easily trigger atherosclerosis,coronary heart disease,peripheral vascular disease,pancreatitis,etc.,and could also increase the incidence of type 2 diabetes and fatty liver disease. Improving dyslipidemia could slow down the progression of atherosclerosis and reduce the risk of coronary heart disease. This is of great importance for prevention and treatment of cardiovascular disease. Phytosterols are natural active ingredients in plants. Many researches have shown that phytosterols have significant lipid-lowering activity,which could effectively lower blood cholesterol and triglyceride levels. Foods containing phytosterols have been widely used as therapeutic diets for improving dyslipidemia. In the early years,it was believed that the lipid-lowering effect of phytosterols was achieved by competitively inhibiting the absorption of dietary cholesterol in the intestine since phytosterols had similar chemical structures with cholesterol. In further researches in recent years,more progress has been made in the lipid-lowering mechanisms of phytosterols. In this paper,PubMed and Web of Science were used to review the cholesterol-lowering and triglyceride-lowering mechanisms of phytosterols according to the available data published,so as to use phytosterols more rationally in clinical application to improve hyperlipidemia and other induced diseases.
Cholesterol
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Diabetes Mellitus, Type 2
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Humans
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Hyperlipidemias
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Hypolipidemic Agents/pharmacology*
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Phytosterols/pharmacology*
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Triglycerides
2.Cycloartenol triterpenoid saponins from Cimicifuga simplex (Ranunculaceae) and their biological effects.
Lun WU ; Zhi-Li CHEN ; Yang SU ; Qiu-Hong WANG ; Hai-Xue KUANG
Chinese Journal of Natural Medicines (English Ed.) 2015;13(2):81-89
The constituents of Cimicifuga plants have been extensively investigated, and the principal metabolites are 9,19-cyclolanostane triterpenoid glycosides, which are distributed widely in Cimicifuga plants, but not in other members of the Ranunculaceae family, and are considered to be characteristics of the Cimicifuga genus. This type of triterpenoid glycoside possesses several important biological activities. More than 120 cycloartane triterpene glycosides have been isolated from Cimicifuga simplex Wormsk. The aim of this review article is to summarize all the major findings based on the available scientific literatures on C. simplex, with a focus on the identified 9,19-cyclolanostane triterpenoid glycosides. Biological studies of cycloartane triterpene glycosides from Cimicifuga spp. are also discussed.
Animals
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Cimicifuga
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chemistry
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Humans
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Phytosterols
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chemistry
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isolation & purification
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pharmacology
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Plant Extracts
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chemistry
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isolation & purification
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pharmacology
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Saponins
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chemistry
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isolation & purification
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pharmacology
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Triterpenes
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chemistry
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isolation & purification
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pharmacology
3.Low fat milk powder containing esterified plant sterols improves the blood lipid profile of adults with hypercholesterolemia.
Jianqin SUN ; Danfeng XU ; Hua XIE ; Yan WANG ; Min CHEN ; Xifeng CHANG ; Yiru PAN ; Yuan LIU ; Huijun XUE ; Hu ZHAO ; Yanqiu CHEN ; Fei XIAO
Chinese Journal of Cardiology 2014;42(7):588-592
OBJECTIVETo observe the impact of plant sterol esters (PSE) mixed in low fat milk powder (2.5 g of PSE/day) on plasma cholesterol levels in hypercholesterolemic subjects during a 6-week intervention period.
METHODSIn this double-blind, randomized, placebo-controlled study, 59 subjects (19 males, mean age (60.28 ± 6.98) years) with primary hypercholesterolemia (fasting LDL cholesterol between 3.4-6.0 mmol/L) were randomly divided into two groups (treatment group, 2.5 g of plant sterol esters a day, n = 30) and placebo group (n = 29). Blood samples were collected at week 0, 3 and 6. The primary outcome was change in plasma LDL-cholesterol (LDL-C). Secondary outcomes were changes in total cholesterol (TC), HDL cholesterol (HDL-C), triglycerides (TG), anthropometry and blood biochemistry.
RESULTSLDL-C significantly reduction from baseline (4.18 ± 0.54) mmol/L to (3.44 ± 0.61) mmol/L (-17.7%, P < 0.05) at week 3 and (3.35 ± 0.39) mmol/L (-19.9%, P < 0.05) at week 6 in the treatment group, whereas in placebo group from (4.11 ± 0.54) mmol/L at baseline to (3.47 ± 0.60) mmol/L (-15.57%, P < 0.05) and (3.61 ± 0.39) mmol/L (-12.17%, P < 0.05) at week 3 and week 6, respectively. TC was reduced from (6.30 ± 0.86) mmol/L at baseline to (5.92 ± 0.75) mmol/L (-6.03%, P > 0.05) at week 3 and (5.43 ± 0.77) mmol/L (-13.8%, P < 0.05) at week 6 in treatment group, from (6.20 ± 0.76) mmol/L at week 0 to (5.70 ± 0.76) mmol/L (-8.06%, P < 0.05) at week 3 and (5.84 ± 0.75) mmol/L (-5.81%, P < 0.05) at week 6 in placebo group. PSE-enriched milk did not affect plasma HDL-C level and TG level at both week 3 and week 6. After normalization to the placebo group, the treatment group showed significant reduction in LDL-C and total cholesteron after 6 weeks. The observed difference of reduction was 7.69% (-0.33 mmol/L, P < 0.05) for LDL-C and 8.00% (-0.51 mmol/L, P < 0.05) for TC between the two groups. There were no significant changes in safety parameters, including blood biochemistry tests during the study period.
CONCLUSIONPlant sterol ester enriched milk powder is effective in reducing LDL-C among Chinese hypercholesterolemic subjects at a dosage recommended by EFSA.
Animals ; Cholesterol ; Cholesterol, HDL ; Cholesterol, LDL ; Double-Blind Method ; Female ; History, 18th Century ; Humans ; Hypercholesterolemia ; diet therapy ; Lipids ; Male ; Middle Aged ; Milk ; Phytosterols ; pharmacology ; therapeutic use ; Triglycerides
4.Study on chemical constituents in rhizome of Pinellia ternata.
Ping HE ; Shuai LI ; Su-juan WANG ; Yong-chun YANG ; Jian-gong SHI
China Journal of Chinese Materia Medica 2005;30(9):671-674
OBJECTIVETo study the chemical constituents in rhizome of Pinellia ternata.
METHODThe constituents were isolated by silica-gel and Sephadex LH-20 chromatography. The structures were identified by spectroscopic analysis including 2D NMR techniques.
RESULTSix compounds were obtained and identified as stigmast-4-en-3-one(I), cycloartenol(II), 5alpha,8alpha-epidioxyergosta-6,22-dien-3-ol(III), beta-sitosterol-3-O-beta-D-glucoside-6'-eicosanate(IV), alpha-monpalmitin(V), beta-sitosterol(VI). The bioactive assay indicated that: compound III was active against the human tumor cell lines HCT-8, Bel-7402, BGC-823, A549, A2780.
CONCLUSIONCompounds I-IV were isolated from Pinellia ternata for the first time, compound II was the first triterpene isolated from this genus. Compound III may be one of the antitumor constituents of P. ternata.
Antineoplastic Agents, Phytogenic ; chemistry ; isolation & purification ; pharmacology ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Ergosterol ; analogs & derivatives ; chemistry ; isolation & purification ; pharmacology ; Humans ; Phytosterols ; chemistry ; isolation & purification ; Pinellia ; chemistry ; Plants, Medicinal ; chemistry ; Rhizome ; chemistry ; Stigmasterol ; analogs & derivatives ; chemistry ; isolation & purification ; Triterpenes
5.Development of the devices for synthetic biology of triterpene saponins at an early stage: cloning and expression profiling of squalene epoxidase genes in panax notoginseng.
Yun-Yun NIU ; Xiao-Xuan ZHU ; Hong-Mei LUO ; Chao SUN ; Lin-Fang HUANG ; Shi-Lin CHEN
Acta Pharmaceutica Sinica 2013;48(2):211-218
Synthetic biology of traditional Chinese medicine (TCM) is a new and developing subject based on the research of secondary metabolite biosynthesis for nature products. The early development of synthetic biology focused on the screening and modification of parts or devices, and establishment of standardized device libraries. Panax notoginseng (Burk.) F.H.Chen is one of the most famous medicinal plants in Panax species. Triterpene saponins have important pharmacological activities in P. notoginseng. Squalene epoxidase (SE) has been considered as a key rate-limiting enzyme in biosynthetic pathways of triterpene saponins and phytosterols. SE acts as one of necessary devices for biosynthesis of triterpene saponins and phytosterols in vitro via synthetic biology approach. Here we cloned two genes encoding squalene epoxidase (PnSE1 and PnSE2) and analyzed the predict amino acid sequences by bioinformatic analysis. Further, we detected the gene expression profiling in different organs and the expression level of SEs in leaves elicited by methyl jasmonate (MeJA) treatment in 4-year-old P notoginseng using real-time quantitative PCR (real-time PCR). The study will provide a foundation for discovery and modification of devices in previous research by TCM synthetic biology. PnSE1 and PnSE2 encoded predicted proteins of 537 and 545 amino acids, respectively. Two amino acid sequences predicted from PnSEs shared strong similarity (79%), but were highly divergent in N-terminal regions (the first 70 amino acids). The genes expression profiling detected by real-time PCR, PnSE1 mRNA abundantly accumulated in all organs, especially in flower. PnSE2 was only weakly expressed and preferentially in flower. MeJA treatment enhanced the accumulation of PnSEI mRNA expression level in leaves, while there is no obvious enhancement of PnSE2 in same condition. Results indicated that the gene expressions of PnSE1 and PnSE2 were differently transcribed in four organs, and two PnSEs differently responded to MeJA stimuli. It was strongly suggested that PnSEs play different roles in secondary metabolite biosynthesis in P. notoginseng. PnSE1 might be involved in triterpenoid biosynthesis and PnSE2 might be involved in phytosterol biosynthesis.
Acetates
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pharmacology
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Amino Acid Sequence
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Cloning, Molecular
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Cyclopentanes
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pharmacology
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Flowers
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metabolism
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Gene Expression Regulation, Enzymologic
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Gene Expression Regulation, Plant
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Oxylipins
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pharmacology
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Panax notoginseng
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genetics
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metabolism
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Phylogeny
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Phytosterols
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biosynthesis
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Plant Growth Regulators
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pharmacology
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Plant Leaves
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metabolism
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Plant Roots
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metabolism
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Plant Stems
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metabolism
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Plants, Medicinal
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genetics
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metabolism
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Saponins
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biosynthesis
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Squalene Monooxygenase
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biosynthesis
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chemistry
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genetics
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Synthetic Biology
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Triterpenes
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metabolism
6.New steroidal alkaloid and furostanol glycosides isolated from Solanum lyratum with cytotoxicity.
Yun-Ling XU ; Jia LV ; Wei-Fang WANG ; Yue LIU ; Ya-Juan XU ; Tun-Hai XU
Chinese Journal of Natural Medicines (English Ed.) 2018;16(7):499-504
Two previously undescribed steroidal compounds, 16, 23-epoxy-22, 26-epimino-cholest-22(N), 23, 25(26)-trien-3β-ol-3-O-β-D-glucopyranosyl-(1→2)-β-D-glucopyranosyl-(1→4)-β-D-galactopyranoside (1) and 26-O-β-D-glucopyranosyl-(25R)-5α-furost-20(22)-en-3β, 26-diol (2), together with 7 known ones including 26-O-β-D-glucopyranosyl-(25R)-5, 20(22)-dien-furost-3β, 26-diol (3), (25R)-5-en-spirost-3β-ol-O-β-D-glucopyranosyl-(1→4)-[α-L-rhmanopyranosyl-(1→2)]-β-D-galactopyranoside (4), funkioside D (5), aspidistrin (6), tigogenin-3-O-β-D-lucotrioside (7), desglucolanatigonin II (8), and degalactotigonin (9), were isolated from Solanum lyratum Thunb. Their cytotoxic activities were tested in two cancer cell lines by MTT method. One of the steroidal glycosides (6) showed significant cytotoxic activity against gastric cancer SGC7901 and liver cancer BEL-7402 cells.
Alkaloids
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chemistry
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isolation & purification
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toxicity
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Antineoplastic Agents
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chemistry
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isolation & purification
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toxicity
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Cell Line, Tumor
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Cell Survival
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drug effects
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Glycosides
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chemistry
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pharmacology
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toxicity
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Humans
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Inhibitory Concentration 50
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Molecular Structure
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Phytosterols
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chemistry
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isolation & purification
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toxicity
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Plant Extracts
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chemistry
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toxicity
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Plants, Medicinal
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chemistry
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Solanum
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chemistry
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Sterols
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chemistry
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pharmacology
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toxicity