Gentianopsis barbata (G. barbata) represents a significant plant species with considerable ornamental and medicinal value in China. This investigation sought to elucidate the primary constituents within the plant and investigate their pharmacological properties. Fifty triterpenoids (1-50), including nine previously undescribed compounds (1, 2, 7, 10, 20, 28, 29, 37, and 41) were isolated and characterized from the whole plants of G. barbata. Notably, compounds 1 and 2 exhibited the novel 3,4;9,10-diseco-24-homo-cycloartane triterpenoid skeleton. The isolated triterpenoids demonstrated substantial anti-inflammatory activity through inhibition of tumor necrosis factor α (TNF-α) and interleukin-6 (IL-6) cytokine secretion in LPS-induced RAW264.7 macrophages, and hepatoprotective effects by preventing tert-butyl hydroperoxide (t-BHP)-induced oxidative injury in HepG2 cells. These results demonstrate both the presence of diverse triterpenoids in G. barbata and their therapeutic potential for inflammatory and hepatic conditions, providing scientific evidence supporting the clinical application of this traditional Mongolian medicinal plant.
Triterpenes/isolation & purification* ; Mice ; Anti-Inflammatory Agents/isolation & purification* ; Animals ; Humans ; RAW 264.7 Cells ; Hep G2 Cells ; Interleukin-6/genetics* ; Tumor Necrosis Factor-alpha/genetics* ; Medicine, Mongolian Traditional ; Macrophages/immunology* ; Protective Agents/isolation & purification* ; Liver/drug effects* ; Gentianaceae/chemistry* ; Plant Extracts/chemistry* ; Molecular Structure

To analyze and compare the protective effects of active components in different ethyl acetate extracts (EAEEPs) from Eclipta prostrate, in order to study the comparison of materials bases protecting normal human bronchial epithelial (NHBE) cells. The MTT assay was taken to compare the protective effect of different EAEEPs on cigarette smoke extracts (CSE) -induced NHBE cells. The ultra-performance liquid chromatography (UPLC) was applied to analyze the content of phenolic acid, coumaric grass ether and flavonoid in EAEEPs. According to the results, all of the eight EAEEPs (0-200 mg x L(-1)) showed certain protective effect on NHBE cells, with statistical difference. Specifically, the total mass of EAEEP VII (89.15 mg x L(-1)) and EAEEP VIII (57.44 mg x L(-1)), which showed the strongest activity, was not the highest, while EAEEP III (132.25 mg x L(-1)) displayed the highest total mass. In the combination with the "component structure" theory, the analysis showed a significant difference in the mass structure among phenolic acid, coumaric grass ether and flavonoid in EAEEP VIII and EAEEP VIII, which were 1.0: 1. 0: 0.5 and 1.0: 1.9: 0.8, respectively. The results suggested a specific optimal "component structure" relationship may exist in EAEEP, which could provide reference for the material base study and quality control.
Bronchi ; cytology ; drug effects ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; pharmacology ; Eclipta ; chemistry ; Epithelial Cells ; cytology ; drug effects ; Humans ; Protective Agents ; chemistry ; isolation & purification ; pharmacology ; Tobacco Smoke Pollution ; adverse effects

The effects of magnolol (Mag) on hyperglycemia and hyperlipemia, hepatic oxidative stress and cytochrome P4502E1 (CYP2E1) activity of diabetic rats induced by high-fat diet (HFD) and streptozotocin (STZ) were studied. After oral administration of Mag (25, 50 and 100 mg x kg(-1) x d(-1)) for continuous 10 weeks, the blood glucose and lipids (TC, TG and LDL-C) levels, as well as the hepatic CYP2E1 activity and MDA content of diabetic rats, decreased significantly (P < 0.05 or P < 0.01), whereas the oral glucose tolerance and hepatic antioxidant enzymatic activities (CAT and GSH-Px) of diabetic rats, increased significantly (P < 0.05 or P < 0.01). The results indicated that Mag was effective against the hepatic oxidative damage, hyperglycemia and hyperlipemia of diabetic rats induced by HFD and STZ, and the inhibition of Mag on hepatic CYP2E1 activity could be an important mechanism of Mag against hepatic insulin resistance and oxidative damage.
Animals ; Biphenyl Compounds ; isolation & purification ; pharmacology ; Blood Glucose ; metabolism ; Cholesterol ; blood ; Cholesterol, LDL ; blood ; Cytochrome P-450 CYP2E1 ; metabolism ; Diabetes Mellitus, Experimental ; blood ; drug therapy ; metabolism ; Diet, High-Fat ; Glucose Tolerance Test ; Hypoglycemic Agents ; isolation & purification ; pharmacology ; Lignans ; isolation & purification ; pharmacology ; Liver ; metabolism ; Magnolia ; chemistry ; Male ; Oxidative Stress ; drug effects ; Plants, Medicinal ; chemistry ; Protective Agents ; pharmacology ; Rats ; Rats, Wistar ; Streptozocin ; Triglycerides ; blood

This study is to observe the protection effect of amentoflavone (AMT) in Selaginella tamariscina against TNF-alpha-induced vascular inflammation injury of endothelial cells. On the basis of TNF-alpha induced human umbilical vein endothelial cell, observe the influence of AMT on endothelial active factor, the contents of SOD and MDA, the protein expression of vascular endothelial adhesion molecules and inflammatory factor; study the effect of its common related signal pathways such as NF-kappaB; research the effect of AMT against TNF-a induced human umbilical vein endothelial cell injury by means of MTT, ELISA, Western blotting and the cell immunofluorescence. The results showed that AMT could increase the content of NO and decrease the levels of VCAM-1, E-selectin, IL-6, IL-8 and ET-1; enhance the activity of SOD, reduce the content of MDA; downregulate the protein expressions of VCAM-1, E-selectin, NF-kappaBp65 and up-regulate IkappaBalpha, attenuate the NF-kappaBp65 transfer to cell nucleus. AMT has the effect of protect vascular endothelial and maybe via the signal pathway of NF-kappaB to down-regulate the inflammation factor and oxidative damage factor of downstream.
Biflavonoids ; isolation & purification ; pharmacology ; Cell Cycle ; drug effects ; Cell Survival ; drug effects ; E-Selectin ; metabolism ; Endothelin-1 ; metabolism ; Human Umbilical Vein Endothelial Cells ; Humans ; I-kappa B Proteins ; metabolism ; Interleukin-6 ; metabolism ; Interleukin-8 ; metabolism ; Malondialdehyde ; metabolism ; NF-KappaB Inhibitor alpha ; Nitric Oxide ; metabolism ; Plants, Medicinal ; chemistry ; Protective Agents ; isolation & purification ; pharmacology ; Selaginellaceae ; chemistry ; Superoxide Dismutase ; metabolism ; Transcription Factor RelA ; metabolism ; Tumor Necrosis Factor-alpha ; adverse effects ; Vascular Cell Adhesion Molecule-1 ; metabolism

The protective effects of Da Chai Hu Granules (DCHKL) on islet cells which were incubated with 4 mmol x L(-1) alloxan (AXN) were studied. The viability of islet cells were measured with MTT. Insulin released into medium and in islets was detected by radioimmunoassay. Cell apoptosis rate was determined by flow cytometry. The expression of anti-apoptotic gene Bcl-2 and pro-apoptotic gene Bax in islet cells were measured with RT-PCR (reverse transcription polymerase chain reaction). Serum containing DCHKL can promote the activity of islet cells significantly (P < 0.01). Basal insulin secretion and high glucose-stimulated insulin secretion increased significantly (P < 0.01). Serum containing DCHKL can inhibit apoptosis of islet cells, the ratio of apoptosis was decreased. Serum containing DCHKL increased expression of Bcl-2 mRNA and decreased expression of Bax mRNA. DCHKL can significantly promote proliferation of islet cells and increase the amount of basal secretion of pancreatic islet cells and high glucose-stimulated insulin secretion. The expression of Bcl-2 increased significantly. The expression of Bax decreased significantly. DCHKL have a protective effect on the islet cells.
Alloxan ; toxicity ; Animals ; Apoptosis ; drug effects ; Cell Proliferation ; drug effects ; Cells, Cultured ; Drug Combinations ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Insulin ; metabolism ; secretion ; Islets of Langerhans ; cytology ; drug effects ; metabolism ; Plants, Medicinal ; chemistry ; Protective Agents ; pharmacology ; Proto-Oncogene Proteins c-bcl-2 ; genetics ; metabolism ; RNA, Messenger ; metabolism ; Rats ; Rats, Sprague-Dawley ; bcl-2-Associated X Protein ; genetics ; metabolism

OBJECTIVETo study the protective effect of different solvent extracts from Platycladi Cacumen Carbonisatum (PCC) on LPS-induced human umbilical vein endothelial cell damage, and discuss the effective extracts from PCC for protecting vascular endothelial cells and their possible active substances.

METHODHUVECs were cultured in vitro; And LPS was adopted to establish the human umbilical vein endothelial cell damage model. MTT colorimetric method was used to determine cell activity; Xanthine oxidase method was adopted to detect the activity of superoxide dismutases (SOD) in the cell culture fluid; The TBA method was adopted to determine the content of malondialdehyde (MDA); The nitrate reductase method was used to detect the content of nitric oxide (NO); And UPLC/Q-TOF-MS was used to analyze the difference in flavonoids components among different solvent extracts from PCC.

RESULTCompared with the model group, N-butanol extract (100 mg x L(-1)) and ethylacetate extract (100, 50 mg x L(-1)) could significantly enhance the cell activity (P < 0.05), significantly reduce MDA and NO content, and increase SOD activity (P < 0.05). Among the four solvent extracts, the content of total flavonids were the highest in ethyl acetate extract, the lowest in water extract and equivalent in N-butanol and petroleum benzene extract. In terms of the contents of quercitrin and myricitrin, N-butanol extract were second only to ethyl acetate extract.

CONCLUSIONEthylacetate extract from PCC has a notable antagonistic effect in the damage induced by LPS to HUVECs, and thus is the most effective extract from PCC in protecting vascular endothelial cells. Quercitrin, myricitrin or multiple flavonoids that it contains may be their active substances for protecting vascular endothelial cells. Its mechanism may be related to the decrease in the production of NO and the inhibition of lipid peroxidation in cells.

Cupressus ; chemistry ; Endothelial Cells ; drug effects ; metabolism ; Humans ; Lipopolysaccharides ; adverse effects ; Malondialdehyde ; metabolism ; Nitric Oxide ; metabolism ; Plant Extracts ; isolation & purification ; pharmacology ; Protective Agents ; isolation & purification ; pharmacology ; Superoxide Dismutase ; metabolism ; Umbilical Veins ; cytology

Fascioliasis is one of the public health problems in the world. Cysteine proteinases (CP) released by Fasciola gigantica play a key role in parasite feeding, migration through host tissues, and in immune evasion. There has been some evidence from several parasite systems that proteinases might have potential as protective antigens against parasitic infections. Cysteine proteinases were purified and tested in vaccine trials of sheep infected with the liver fluke. Multiple doses (2 mg of CP in Freund's adjuvant followed by 3 booster doses 1 mg each at 4 week intervals) were injected intramuscularly into sheep 1 week prior to infect orally with 300 F. gigantica metacercariae. All the sheep were humanely slaughtered 12 weeks after the first immunization. Changes in the worm burden, ova count, and humoral and cellular responses were evaluated. Significant reduction was observed in the worm burden (56.9%), bile egg count (70.7%), and fecel egg count (75.2%). Immunization with CP was also found to be associated with increases of total IgG, IgG1, and IgG2 (P<0.05). Data showed that the serum cytokine levels of pro-inflammatory cytokines, IL-12, IFN-gamma, and TNF-alpha, revealed significant decreases (P<0.05). However, the anti-inflammatory cytokine levels, IL-10, TGF-beta, and IL-6, showed significant increases (P<0.05). In conclusion, it has been found that CP released by F. gigantica are highly important candidates for a vaccine antigen because of their role in the fluke biology and host-parasite relationships.
Animals ; Antibodies, Helminth/immunology ; Cysteine Proteases/administration & dosage/*immunology/isolation & purification ; Cytokines/immunology ; Fasciola/chemistry/*enzymology/immunology ; Fasciola hepatica/immunology/physiology ; Fascioliasis/immunology/parasitology/*prevention & control ; Female ; Helminth Proteins/administration & dosage/*immunology/isolation & purification ; Humans ; Male ; Protective Agents/*administration & dosage/isolation & purification ; Sheep ; Vaccines/immunology

OBJECTIVETo establish a new rapid method to screen potential hepatoprotective compounds from traditional Chinese medicine, and identify the hepatoprotective compounds in Paeoniae Radix Rubra.

METHODFluorescein diacetate labelled and MTT assay were applied for screening the hepatoprotective fractions on HepG2 cells exposed to galactosamine. The active fractions were analyzed by chromatography coupled with mass spectrometry. Finally, the hepatoprotective effects of the identified compounds were validated by hepatoprotective assay.

RESULTThree hepatoprotective fractions were founded, in which three compounds were identified as paeoniflorin, ethyl palmitate and ethyl linoleate. Validation results indicated that all the three compounds can attenuate the galactosamine induced injury on HepG2 cells.

CONCLUSIONPaeoniflorin, ethyl palmitate and ethyl linoleate from paeoniae radix rubra showed potential hepatoprotective activity.

Benzoates ; isolation & purification ; pharmacology ; Bridged-Ring Compounds ; isolation & purification ; pharmacology ; Glucosides ; isolation & purification ; pharmacology ; Hep G2 Cells ; Humans ; Linoleic Acids ; isolation & purification ; pharmacology ; Liver ; drug effects ; Monoterpenes ; Paeonia ; chemistry ; Palmitic Acids ; isolation & purification ; pharmacology ; Protective Agents ; isolation & purification

To investigate the effects of lanosterol (1), inotodiol (2) and trametenolic acid (3) from Inonotus obliquus against oxidative damage induced by CCl4 in mice, 1, 2 and 3 (20, 10 and 5 mg x kg(-1)) were respectively administered to mice, once a day for 3 days. Then the mice were induced to oxidative damage by CCl4 on the third day 30 min after the administration. The activities of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-PX) and the content of malondialdehyde (MDA) and reductive glutathione (GSH) in serum and liver homogenate were determined. And the levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) and interleukin-6 (IL-6) concentration in serum were detected. The results showed that treatment with compound 1, 2 and 3 could significantly increase the activities of SOD, CAT and GSH-PX in serum and liver homogenate. Furthermore, the content of GSH in serum and liver homogenate increased and MDA content decreased markedly. In addition, compound 1, 2 and 3 could significantly inhibit the activities of ALT and AST in serum, and decrease the IL-6 concentration in serum remarkably. So, compound 1, 2 and 3 can protect mice against oxidative stress injury induced by CCl4. Furthermore, compound 1, 2 and 3 can protect cells from damage through inhibition on ALT, AST and the expression of IL-6.
Alanine Transaminase ; blood ; Animals ; Aspartate Aminotransferases ; blood ; Carbon Tetrachloride ; Catalase ; blood ; metabolism ; Female ; Glutathione ; blood ; metabolism ; Glutathione Peroxidase ; blood ; metabolism ; Interleukin-6 ; blood ; Lanosterol ; analogs & derivatives ; isolation & purification ; pharmacology ; Liver ; metabolism ; Male ; Malondialdehyde ; blood ; metabolism ; Mice ; Oxidative Stress ; drug effects ; Polyporaceae ; chemistry ; Protective Agents ; isolation & purification ; pharmacology ; Random Allocation ; Superoxide Dismutase ; blood ; metabolism ; Triterpenes ; isolation & purification ; pharmacology

Cells, Cultured ; Epinephrine ; adverse effects ; Human Umbilical Vein Endothelial Cells ; drug effects ; ultrastructure ; Humans ; Laminaria ; chemistry ; Polysaccharides ; isolation & purification ; pharmacology ; Protective Agents ; pharmacology