scholarly journals A Strategy for Screening the Lipid-Lowering Components in Alismatis Rhizoma Decoction Based on Spectrum-Effect Analysis

2022 ◽  
Vol 2022 ◽  
pp. 1-10
Author(s):  
Xiao-Yan Chang ◽  
Jia-Shuo Wu ◽  
Fang-Qing Zhang ◽  
Zhuang-Zhuang Li ◽  
Wei-Yi Jin ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Farnesoid X Receptor ◽  
Lipid Lowering ◽  
Hypolipidemic Effect ◽  
Least Squares Regression ◽  
Human Hepatoma Cells ◽  
Effect Analysis ◽  
Effective Components ◽  
Alismatis Rhizoma ◽  
Spectrum Effect

Alismatis Rhizoma decoction (ARD), comprised of Alisma plantago-aquatica subsp. orientale (Sam.) Sam and Atractylodes macrocephala Koidz. at a ratio of 5 : 2, is a classic traditional Chinese medicine (TCM) formula with successful clinical hypolipidemic effect. This paper aimed to explore the major bioactive compounds and potential mechanism of ARD in the treatment of hyperlipidemia on the basis of spectrum-effect analysis and molecular docking. Nine ARD samples with varying ratios of the constituent herbs were prepared and analyzed by UPLC-Q-TOF/MS to obtain the chemical spectra. Then, the lipid-lowering ability of the nine samples was tested in an oleic acid-induced lipid accumulation model in human hepatoma cells (HepG2). Grey relational analysis and partial least squares regression analysis were then performed to determine the correlation between the chemical spectrums and lipid-lowering efficacies of ARD. The potential mechanisms of the effective compounds were investigated by docking with the farnesoid X receptor (FXR) protein. The results indicated that alisol B 23-acetate, alisol C 23-acetate, and alisol B appeared to be the core effective components on hyperlipidemia in ARD. Molecular docking further demonstrated that all three compounds could bind to FXR and were potential FXR agonists for the treatment of hyperlipidemia. This study elucidated the effective components and potential molecular mechanism of action of ARD for treating hyperlipidemia from a perspective of different compatibility, providing a new and feasible reference for the research of TCM formulas such as ARD.

scholarly journals Molecular mechanism underlying the hypolipidemic effect of Shanmei Capsule based on network pharmacology and molecular docking

2021 ◽  
Vol 29 ◽  
pp. 239-256
Author(s):  
Qian Wang ◽  
Lijing Du ◽  
Jiana Hong ◽  
Zhenlin Chen ◽  
Huijian Liu ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Signaling Pathway ◽  
Molecular Mechanism ◽  
Kegg Pathway ◽  
Network Pharmacology ◽  
Pathway Enrichment Analysis ◽  
Signal Pathways ◽  
Hypolipidemic Effect ◽  
Active Ingredients ◽  
Pathway Enrichment

BACKGROUND: Shanmei Capsule is a famous preparation in China. However, the related mechanism of Shanmei Capsule against hyperlipidemia has yet to be revealed. OBJECTIVE: To elucidate underlying mechanism of Shanmei Capsule against hyperlipidemia through network pharmacology approach and molecular docking. METHODS: Active ingredients, targets of Shanmei Capsule as well as targets for hyperlipidemia were screened based on database. Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment were performed via Database for Annotation, Visualization, and Integrated Discovery (DAVID) 6.8 database. Ingredient-target-disease-pathway network was visualized utilizing Cytoscape software and molecular docking was performed by Autodock Vina. RESULTS: Seventeen active ingredients in Shanmei Capsule were screened out with a closely connection with 34 hyperlipidemia-related targets. GO analysis revealed 40 biological processes, 5 cellular components and 29 molecular functions. A total of 15 signal pathways were enriched by KEGG pathway enrichment analysis. The docking results indicated that the binding activities of key ingredients for PPAR-α are equivalent to that of the positive drug lifibrate. CONCLUSIONS: The possible molecular mechanism mainly involved PPAR signaling pathway, Bile secretion and TNF signaling pathway via acting on MAPK8, PPARγ, MMP9, PPARα, FABP4 and NOS2 targets.

Hypolipidemic effect of prepared Polyherbal formulations in Wistar albino rats

2021 ◽  
pp. 4314-4320
Author(s):  
Ranjan Kumar Giri ◽  
Sunil Kumar Kanungo ◽  
Saroj Kumar Patro ◽  
Minaketan Sahoo ◽  
Dibya Sundar Panda
Keyword(s):  
Elevated Serum ◽  
Density Lipoprotein ◽  
Lipid Lowering ◽  
Control Group ◽  
Albino Rats ◽  
Histopathological Study ◽  
Oral Glucose ◽  
Hypolipidemic Effect ◽  
Standard Drug ◽  
Wistar Albino Rats

Lipid lowering effect of polyherbal formulations using eight different plants was evaluated in triton and diet induced hyperlipidemic models of wistar albino rats. Formulations such as Tablet, Syrup and Suspension inhibited the elevation in serum cholesterol and triglyceride levels on Triton WR 1339 administration rats. The formulations at the same dose level significantly attenuated the elevated serum total cholesterol and triglycerides with an increase in high-density lipoprotein cholesterol in high-fat diet-induced hyperlipidemic rats. The standard drug Niacin showed slightly better effects. The treatment with herbal formulations produced 30-35 percentage improvement in oral glucose tolerance. Similarly all the formulations also reduced the elevated C-reactive protein which is a marker of Hyperlipidemia. In histopathological study it was found that treatment of polyherbal formulation significantly reduced the plaque size in aorta compared with HFD treated control group. The outcome of the study reveals the lipid lowering activity of polyherbal formulations in dyslipidaemic conditions by interfering with the biosynthesis of cholesterol and utilization of lipids.

scholarly journals Evaluation of Lipid Lowering Effect of Milk Thistle (Silybum Marianum) in Comparison with Rosuvastatin in Rats by Using Ace-alera® Analyzer

2020 ◽  
Vol 14 ◽  
Keyword(s):  
Low Density Lipoprotein ◽  
Density Lipoprotein ◽  
Hdl Cholesterol ◽  
Lipid Lowering ◽  
Control Group ◽  
Milk Thistle ◽  
High Dose ◽  
Hypolipidemic Effect ◽  
Low Density ◽  
Therapeutic Protocols

Dyslipidemia is a metabolic disorder that is characterized with an elevation in the cholesterol serum levels that can be treated with various hypolipidemic drugs like rosuvastatin. The present study was undertaken to determine and evaluate the hypolipidemic effect of milk thistle seeds extract in comparison with rosuvastatin and the combination of both for the treatment of dyslipidemia in rats. Also its effect on blood glucose levels on experimentally induced dyslipidemic rats. In vivo studies were conducted on wister albino laboratory rats, in which 49 rats were induced to be dyslipidemic by a daily intragastric administration of cholesterol (2 g/kg). The induction of dyslipidemia was evaluated by comparing these rats with a negative control group that was composed of 10 healthy rats. Then, after one month dyslipidemia was induced in 49 rats that were divided into 6 groups, as the following; positive control group (n=9) received cholesterol (2 g/kg) for another one month, and the other five groups each of 8 rats continued to receive cholesterol (2 g/kg) for one month along with therapy as; rosuvastatin low dose (RL) group received 10 mg/kg, rosuvastatin high dose (RH) group received 20 mg/kg, milk thistle (MT) group received 7.15 mg/kg, (RL+MT) group received a combination of 10 mg/kg of rosuvastatin and 7.15 mg/kg of milk thistle, and (RH+MT) group received a combination of 20 mg/kg of rosuvastatin and 7.15 mg/kg of milk thistle. The statistical results of biochemical analysis showed that all the studied therapeutic protocols whether given alone; RL, RH, and MT or in a combination; RL+MT and RH+MT led to a significant (p≤0.05) hypolipidemic effect that reduced the total cholesterol (TC), triglyceride (TG), low density lipoprotein (LDL) and very low density lipoprotein (VLDL) and increased the high density lipoprotein (HDL) cholesterol levels. In conclusion, all therapeutic protocols were effective in treating dyslipidemia, as they all reduced the TC, TG, LDL, and VLDL, and increased the HDL cholesterol significantly (p≤0.05). Furthermore, we found that milk thistle can be used in the management of dyslipidemia, as it has a hypolipidemic effect. Also, the addition of milk thistle to rosuvastatin therapy reduced the risk of developing diabetes mellitus (DM), as it has a glucose modulating activity either when it was given alone or in combination with rosuvastatin. Moreover, the combination of milk thistle and rosuvastatin was of a great benefit, as it gave an intensive goal of therapy than each one alone in altering all lipid profile parameters.

scholarly journals Secondary Metabolite Mapping Identifies Peony Episperm Inhibitors of Human Hepatoma Cells

2019 ◽  
Vol 14 (7) ◽  
pp. 1934578X1986031
Author(s):  
Xiao Yang ◽  
Ruixue Deng ◽  
Pu Liu ◽  
Jiangxia Hu ◽  
Wentian Niu ◽  
...  
Keyword(s):  
Liver Cancer ◽  
Secondary Metabolite ◽  
Principal Components ◽  
Human Liver ◽  
Cancer Cell Line ◽  
Least Squares Regression ◽  
Human Hepatoma Cells ◽  
Liquid Chromatograph ◽  
Medicinal Uses ◽  
Human Liver Cancer

As the main by-product during the oil production of peony seeds, the episperm is traditionally used as a lead component in folk herbal formulas for the cancer treatment in China. However, the investigation of its phytochemical foundation underlying anticancer effects remains an ongoing challenge. The work therefore determined growth inhibition activities of 8 solvent extracts of peony episperms in the human liver cancer cell line. This activity was then mapped onto the secondary metabolite profile of extracts by principal components analysis (PCA). The top 3 principal components of High Performance Liquid Chromatograph (HPLC)-PCA map discriminated extract activities mainly based on the differential content of 5 stilbene compounds, which were then tested individually. The trans-ε-viniferin, gnetin-H, suffruticosol A, suffruticosol B, and suffruticosol C were thus determined as growth inhibitors and apoptosis inducers of human liver cancer cells with activities comparable to that of the antineoplastic cisplatin. A partial least squares regression-HPLC model was also constructed for the prediction of inhibitory effects of peony episperm extracts. These results expand the fundamental understanding of the peony episperms and support its current medicinal uses in China. Moreover, PCA-mediated secondary metabolite mapping was proved to be an efficient approach to qualify biomedical products required for pharmaceutical and medicinal uses.

WO5-OR-6 COMMON VARIANT OF FARNESOID-X-RECEPTOR GENE ENHANCES THE RESPONSE TO LIPID-LOWERING THERAPY

2007 ◽  
Vol 8 (1) ◽  
pp. 6
Author(s):  
A. Nohara ◽  
H. Tada ◽  
S. Katsuda ◽  
M. Kawashiri ◽  
A. Inazu ◽  
...  
Keyword(s):  
Receptor Gene ◽  
Farnesoid X Receptor ◽  
Common Variant ◽  
Lipid Lowering ◽  
Lipid Lowering Therapy ◽  
Lowering Therapy

scholarly journals Screening and Characterizing Tyrosinase Inhibitors from Salvia miltiorrhiza and Carthamus tinctorius by Spectrum-Effect Relationship Analysis and Molecular Docking

2018 ◽  
Vol 2018 ◽  
pp. 1-10 ◽  
Author(s):  
Ya-Li Wang ◽  
Guang Hu ◽  
Qian Zhang ◽  
Yu-Xiu Yang ◽  
Qiao-Qiao Li ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Amino Acid ◽  
Salvia Miltiorrhiza ◽  
Carthamus Tinctorius ◽  
Amino Acid Residues ◽  
Analysis Method ◽  
Effect Relationship ◽  
Relationship Analysis ◽  
Ms Analysis ◽  
Spectrum Effect

Tyrosinase (TYR) is a rate-limiting enzyme in the synthesis of melanin, while direct TYR inhibitors are a class of important clinical antimelanoma drugs. This study established a spectrum-effect relationship analysis method and high-performance liquid chromatography-mass spectrometry (LC-MS) analysis method to screen and identify the active ingredients that inhibited TYR in Salvia miltiorrhiza–Carthamus tinctorius (Danshen–Honghua, DH) herbal pair. Seventeen potential active compounds (peaks) in the extract of DH herbal pair were predicted, and thirteen of them were tentatively identified by LC-MS analysis. Furthermore, TYR inhibitory activities of five pure compounds obtained from the DH herbal pair were validated in the test in which kojic acid served as a positive control drug. Among them, three compounds including protocatechuic aldehyde, hydroxysafflor yellow A, and tanshinone IIA were verified to have high TYR inhibitory activity (IC50 value of 455, 498, and 1214 μM, resp.) and bind to the same amino acid residues in TYR catalytic pocket according to the results of the molecular docking test. However, the other two compounds lithospermic acid and salvianolic acid A had a weak effect on TYR, as they do not combine with the active amino acid residues or act on the active center of TYR. Therefore, the developed methods (spectrum-effect relationship analysis and molecular docking) could be used to effectively screen TYR inhibitors in complex mixtures such as natural products.

scholarly journals Anti-Obesity and Lipid Lowering Activity of Bauhiniastatin-1 is Mediated Through PPAR-γ/AMPK Expressions in Diet-Induced Obese Rat Model

2021 ◽  
Vol 12 ◽  
Author(s):  
Reddy Sankaran Karunakaran ◽  
Oruganti Lokanatha ◽  
Ganjayi Muni Swamy ◽  
Chintha Venkataramaiah ◽  
Muppuru Muni Kesavulu ◽  
...  
Keyword(s):  
Molecular Docking ◽  
High Fat Diet ◽  
Docking Studies ◽  
Lipid Lowering ◽  
High Fat ◽  
Down Regulation ◽  
Binding Interactions ◽  
Molecular Docking Studies ◽  
Ppar Γ ◽  
Group I

Objective: To evaluate the therapeutic efficacy and underlying molecular mechanisms of Bauhiniastatin-1 (BSTN1) to alleviate adiposity in diet-induced obese rodent model and in 3T3-L1 cells.Methods: BSTN1 was purified and confirmed through HPLC. In-vitro experiments such as MTT assay, Oil Red-O (ORO) stain, cellular lipid content, glycerol release and RT-PCR analysis were performed in 3T3-L1 cells in the presence and absence of BSTN1. In animal experiments, rats were divided into Group-I: normal pellet diet-fed, Group-II: HFD-fed, Groups-III, IV and V: HFD-fed BSTN1 (1.25, 2.5, and 5 mg/kg.b.wt./day/rat)-treated and Group-VI: HFD-fed Orlistat-treated. The rats were fed either normal diet or high fat diet (HFD) for 18 weeks and water ad-libitum. BSTN1 was orally administered from 13th week onwards to the selected HFD-fed groups. Body composition parameters, biochemical assays, histopathology examination and western blot analysis were performed to identify the predicted targets related to obesity. Molecular docking studies threw light on the binding interactions of BSTN1 against PPAR-γ, FAS and AMPK.Results: BSTN1 at 20 μM significantly (p < 0.001) inhibited adipocyte differentiation and lipid accumulation in 3T3-L1 cells. A conspicuous down-regulation in the mRNA expression levels of PPAR-γ, FAS and SREBP1 was observed but AMPK expression remained unchanged in BSTN1 treated 3T3-L1 cells. A substantial decrease in body weight gain, fat percent, total body fat, serum and liver lipid profile (except high-density lipoprotein), glucose, insulin and insulin resistance in BSTN1 treated rats was noticed in a dose dependent manner. In BSTN1 (5 mg/kg.b.wt.)-treated groups significantly (p < 0.01) elevated plasma adiponectin level but reduced leptin level as well as fall in serum AST and ALT were noticed. Further, the disturbed structural integrity and architecture of adipose and hepatic tissues due to high fat diet feeding were considerably recovered with BSTN1 treatment. Down-regulation in the protein expression level of PPAR-γ and activation of AMPK through phosphorylation was observed in BSTN1 treated rats than the untreated. Molecular docking studies revealed strong binding interactions of BSTN1 against PPAR-γ and AMPK and thus supported the experimental results.Conclusion: Taken together, the results suggest that BSTN1 could be a promising pharmacological molecule in the treatment of obesity and dyslipidemia.

scholarly journals Comparative Hypolipidemic Evaluation of Aframomum Melegueta Seeds and Moringa Oleifera Leaves

2021 ◽  
pp. 166-182
Author(s):  
L. U. Nwankwo ◽  
F. A. Onyegbule ◽  
C. C. Abba ◽  
E. Agbamu
Keyword(s):  
Liver Function ◽  
Moringa Oleifera ◽  
Soxhlet Extraction ◽  
Ethanol Extract ◽  
Negative Control ◽  
Lipid Lowering ◽  
Hypolipidemic Effect ◽  
Crude Extracts ◽  
Moringa Oleifera Leaves ◽  
Crude Drugs

Aims: The study was carried out to compare the lipid lowering effects of both crude drugs as well as deducing the extracts with the best lipid lowering property; and the fractions. Study Design: The research was conducted with an experimental design solely based on laboratory trials which involved the use of ninety-six (96) male albino wistar rats to compare the hypolipidemic effects of both crude drugs and respective fractions. Place and Duration of Study: Department of Pharmacognosy Laboratory, Faculty of Pharmacy, Delta State University, Abraka, Nigeria and Department of Pharmacology and Toxicology Laboratory, Faculty of Pharmaceutical Sciences, Nnamdi Azikiwe University, Agulu, Anambra State, Nigeria. The research was carried out from March to August, 2021. Methodology: Ethanol extracts of both plants were prepared using soxhlet extraction. Each extract was then subjected to VLC fractionation using four solvents: n-hexane, chloroform, ethyl acetate and methanol. The fractions were bulked together after conducting thin layer chromatographic procedures and each extract was bulked into four fractions. The acute toxicity studies (LD50) of both extracts were determined in the rats using Lorke’s method. The crude extracts were screened for the presence and quantity of phytoconstituents using standard methods. The antilipidemic study was carried out using sixty-eight (68) rats randomized into seventeen (17) groups of four (4) animals each. Lipid profile was determined using spectrophotometer. Liver function tests and histology was also carried out using standard procedures. Results: Administration of various treatments (both crude extracts and fractions) evoked a significant (p<0.05) reduction of TC, TG, and LDL-C as well as significant (p<0.05) elevation of HDL-C when compared with the negative control. With a percentage serum lipid reduction of 45.11%TC, 48.23%TG, 63.39% LDL-C and 174.69% elevation of HDL-C, the group treated with the combination of 500 mg/kg Aframomum melegueta and 500 mg/kg Moringa oleifera produced the best hypolipidemic effect. This is closely followed by fraction MO4. Comparatively, Moringa oleifera extracts exerts a better antilipidemic effect than Aframomum melegueta seed extract. The liver function test showed that both plants has no toxic effect on the liver cells at doses of 250 mg/kg and 500 mg/kg, hence confirming the hepatoprotective effect of both crude drugs at the doses administered. Conclusion: In conclusion, results from this study suggests that ethanol extract of Moringa oleifera leaves is more effective than ethanol extract of Aframomum melegueta seeds as a                   hypolipidemic agent, however, combination of both crude drugs as a lipid lowering agent has proved to be more effective and reliable when compared to each crude drug administered independently.

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