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1.
Bioorg Chem ; 115: 105178, 2021 10.
Article in English | MEDLINE | ID: mdl-34303897

ABSTRACT

Four undescribed ent-kaurane diterpenoids, wilkaunoids A - D (1-4), and three undescribed abietane diterpenoids, wilabinoids A - C (13-15), along with thirteen known ones (5-12 and 16-20), were isolated from Tripterygium wilfordii. Their structures were elucidated by extensive spectroscopic methods, electroniccirculardichroism calculation, and X-ray diffraction analysis. Compounds 1 and 2 were a pair of C-19 epimers of ent-kaurane diterpenoids, featuring a rare 19,20-epoxy-19,20-dimethoxy-kaurane fragment. Compound 3 possessed a rare naturally occurring 1,3-dioxacyclohexane moiety. Compounds 13 and 15 represented the first example of abietane diterpenoids with an isovalerate substitution from the genus of Tripterygium. The possible biosynthetic pathways of 1-3 were postulated. The effect of 1-20 on nitric oxide production was examined in lipopolysaccharide-stimulated RAW 264.7 cells. Abietane diterpenoid quinones 7-13 (IC50: 1.9-10.2 µM) exhibited the significant activity to inhibit nitric oxide production versus positive control (NG-monomethyl-l-arginine acetate salt, IC50 = 24.9 µM). The structure activity relationship of 7-13 in inhibiting nitric oxide production was then discussed. The most potent 7 and 8 were found to significantly suppress the expression of cyclooxygenase-2 and inducible nitric oxide synthase proteins, showing a good anti-inflammatory potential. The findings provided some valuable insights for the discovery and structural modification of abietane diterpenoids towards anti-inflammatory lead compounds.


Subject(s)
Abietanes/pharmacology , Anti-Inflammatory Agents/pharmacology , Diterpenes, Kaurane/pharmacology , Tripterygium/chemistry , Abietanes/chemistry , Animals , Anti-Inflammatory Agents/chemistry , Diterpenes, Kaurane/chemistry , Macrophages/drug effects , Macrophages/metabolism , Mice , Nitric Oxide/metabolism , RAW 264.7 Cells
2.
Chem Biodivers ; 18(4): e2001066, 2021 Apr.
Article in English | MEDLINE | ID: mdl-33656782

ABSTRACT

Three new matrine-type alkaloids, 8ß-hydroxyoxysophoridine (1), 9ß-hydroxysophoridine (2), 9ß-hydroxyisosophocarpine (3), together with one known analog, 11,12-dehydromatrine (4), were isolated from the seeds of Sophora alopecuroides L. The structures of new compounds were elucidated using extensive spectroscopic techniques including the experimental and calculated ECD data. The anti-inflammatory activities of all the isolates on NO production in RAW 264.7 cells stimulated by lipopolysaccharide were evaluated. Among them, 8ß-hydroxyoxysophoridine (1) showed a significant inhibitory effect with an IC50 value of 18.26 µM.


Subject(s)
Alkaloids/pharmacology , Anti-Inflammatory Agents/pharmacology , Nitric Oxide/antagonists & inhibitors , Plant Extracts/pharmacology , Seeds/chemistry , Sophora/chemistry , Alkaloids/chemistry , Alkaloids/isolation & purification , Animals , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/isolation & purification , Dose-Response Relationship, Drug , Lipopolysaccharides/antagonists & inhibitors , Lipopolysaccharides/pharmacology , Mice , Nitric Oxide/biosynthesis , Plant Extracts/chemistry , Plant Extracts/isolation & purification , RAW 264.7 Cells
3.
Zhonghua Yi Xue Za Zhi ; 87(2): 105-8, 2007 Jan 09.
Article in Zh | MEDLINE | ID: mdl-17418017

ABSTRACT

OBJECTIVE: To investigate the relations of platelet phospholipid fatty acids to thrombotic risk factors in the middle-aged and geriatric patients with hyperlipidemia in the metropolitan area of Hangzhou, Zhejiang province. METHODS: A questionnaire survey was conducted among 81 patients with hyperlipidemia, 50 males and 31 females, aged (57 +/- 8), and 65 healthy controls, 43 males and 22 females, aged (58 +/- 9) to collect the data about height, weight, and diet. Peripheral venous blood samples were collected to examine the total cholesterol, triglyceride, high-density lipoprotein cholesterol (HDL-C), low-density lipoprotein cholesterol (LDL-C), homocysteine (Hcy), 6-keto-prostaglandin F(1alpha) (6-keto-PGF(1alpha)), and thromboxane B(2) (TXB(2)) were examined by standard methods. Serum thrombotic risk factors including homocysteine and Thromboxane B(2) were determined by standard methods. Platelet phospholipid fatty acids were examined by gas chromatography. The correlation between the serum thrombotic risk factors (Hcy, TXB(2), and 6-keto-PG F1a) was analyzed by multivariate linear regression. RESULTS: There were no significant differences in platelet phospholipid fatty acids between the patients with hyperlipidemia and the healthy controls. Serum Hcy was significantly negatively correlated with docosahexaenoic acid (DHA) and the ratio of n-3 PUFA (polyunsaturated fatty acids)/n-6 PUFA (r = -0.277 and -0.231, both P < 0.01). The level of serum TXB(2) was significantly positively correlated with arachidonic acid (r = 0.176, P < 0.05), and significantly negatively correlated with DHA (r = -0.209, P < 0.01), eicosapentaenoic acid (EPA) (r = -0.194, P < 0.05), and n-3 PUFA/n-6 PUFA (r = -0.238, P < 0.01). CONCLUSION: Increasing the ratio of n-3 PUFA/n-6 PUFA in platelet phospholipid may potentially decrease the thrombotic risks such as Hcy and TXB(2) and provide a reference for diet selection.


Subject(s)
Fatty Acids/blood , Hyperlipidemias/blood , Phospholipids/blood , Thrombosis/blood , 6-Ketoprostaglandin F1 alpha/blood , Aged , Arachidonic Acid/blood , Blood Platelets/chemistry , Cholesterol/blood , Dietary Fats/blood , Female , Homocysteine/blood , Humans , Linear Models , Male , Middle Aged , Multivariate Analysis , Risk Factors , Surveys and Questionnaires , Thromboxane B2/blood
4.
Asian Pac J Cancer Prev ; 14(8): 4913-8, 2013.
Article in English | MEDLINE | ID: mdl-24083767

ABSTRACT

OBJECTIVE: To assess the level of an inpatient population's awareness about hepatitis and primary liver cancer (PLC), the most common type of which is hepatocellular carcinoma (HCC), and then to initiate education of this group. METHODS: A survey was conducted with 1300 participants within the inpatient unit in representative tertiary hospitals in the Chaoshan area of China. Structured questionnaires contained demographic data and statements about different aspects of liver cancer and hepatitis. The questionnaires were completed by trained medical practitioners after they had conducted the interviews. RESULTS: One way ANOVA showed that the sample population lacked adequate knowledge about HCC and hepatitis. Stepwise multiple regression analysis demonstrated that the participant's level of education had the greatest impact on their total knowledge score when other variables remained constant. CONCLUSIONS: The study demonstrated: a general lack of awareness amongst the participants about the preventative strategies, and the management options available for people with primary liver cancer and hepatitis; education level was an important factor affecting knowledge levels. The demonstrated deficiencies in people's knowledge about hepatitis and HCC, and their lack of subsequent protective behaviours are likely to play an important role in HCC and hepatitis transmission or prevention.


Subject(s)
Carcinoma, Hepatocellular/etiology , Health Knowledge, Attitudes, Practice , Hepatitis B/complications , Liver Neoplasms/etiology , Adult , Awareness , Carcinoma, Hepatocellular/epidemiology , Carcinoma, Hepatocellular/prevention & control , China/epidemiology , Female , Follow-Up Studies , Hepatitis B/epidemiology , Hepatitis B virus/pathogenicity , Humans , Inpatients/statistics & numerical data , Liver Neoplasms/epidemiology , Liver Neoplasms/prevention & control , Male , Middle Aged , Patient Education as Topic , Prevalence , Prognosis , Risk Factors , Surveys and Questionnaires , Tertiary Care Centers , Young Adult
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