Dimethyl Cardamonin Exhibits Anti-inflammatory Effects via Interfering with the PI3K-PDK1-PKCalpha Signaling Pathway

Consumption of herbal tea [flower buds of Cleistocalyx operculatus (Roxb.) Merr. et Perry (Myrtaceae)] is associated with health beneficial effects against multiple diseases including diabetes, asthma, and inflammatory bowel disease. Emerging evidences have reported that High mobility group box 1 (HMGB1) is considered as a key "late" proinflammatory factor by its unique secretion pattern in aforementioned diseases. Dimethyl cardamonin (2',4'-dihydroxy-6'-methoxy-3',5'-dimethylchalcone, DMC) is a major ingredient of C. operculatus flower buds. In this study, the anti-inflammatory effects of DMC and its underlying molecular mechanisms were investigated on lipopolysaccharide (LPS)-induced macrophages. DMC notably suppressed the mRNA expressions of TNF-alpha, IL-1beta, IL-6, and HMGB1, and also markedly decreased their productions in a time- and dose-dependent manner. Intriguingly, DMC could notably reduce LPS-stimulated HMGB1 secretion and its nucleo-cytoplasmic translocation. Furthermore, DMC dose-dependently inhibited the activation of phosphatidylinositol 3-kinase (PI3K), phosphoinositide-dependent kinase 1 (PDK1), and protein kinase C alpha (PKCalpha). All these data demonstrated that DMC had anti-inflammatory effects through reducing both early (TNF-alpha, IL-1beta, and IL-6) and late (HMGB1) cytokines expressions via interfering with the PI3K-PDK1-PKCalpha signaling pathway.

Identification of metabolites of nobiletin in rats using ultra-performance liquid chromatography coupled with triple-quadrupole mass spectrometry / 药学学报

In this study, metabolism of nobiletin in rats was studied using ultra-performance liquid chromatography coupled with tandem mass spectrometry (UPLC-MS/MS). As a result, seven major metabolites were found in bile, urine and serum of rats. Three phase I products were assigned to be demethyl and di-demethyl products, and other four phase II products were assigned to be glucuronic and sulfonic conjugates. The four phase II metabolites were reported for the first time. Among the metabolites found in the present study, the glucuronic conjugates of demethyl-nobiletin played a predominant role in the metabolic pathway, indicating that its potential role for glucuronidation-related factors, such as gene polymorphism, drug-drug interaction, etc., in changing the active and toxic effect of nobiletin and that it should be paid more attention in further development.

Investigation of the level of perceived control of asthma and the factors affecting such perception in South China / 南方医科大学学报

<p><b>OBJECTIVE</b>To investigate the level of the patients perceived control of asthma (PCA) in South China and analyze the risk factors contributing to inadequate PCA.</p><p><b>METHODS</b>A total of 150 asthmatic out-patients consisting of 86 males and 64 females aged 19-65 (38.6∓11.7) years were enrolled in this investigation. The patients were asked to complete questionnaires of the demographic data, perceived control of asthma (PCAQ-6) scales, asthma control test (ACT) scales and Standard asthma-specific quality of life [AQLQ(S)] scale. The data of spirometric measurements, blood cell count and induced sputum cell count were also collected.</p><p><b>RESULTS</b>All the 150 asthmatic out-patients recruited completed the questionnaires and examinations. The PCAQ-6 scores ranged from 10 to 26 (18.75∓3.42) in these patients (18.6∓3.28 in male and 18.95∓3.6 in female patients), significantly lower than those reported in other countries (P<1). PCA was positively correlated to the level of asthma control (r(p)=0.377, P=0.000) and AQLQ(S) scores (r(p)=0.675, P=0.000). Multiple linear regression showed that PCA was positively correlated to FEV1% and blood neutrophil counts, and inversely to asthma duration.</p><p><b>CONCLUSION</b>The level of the PCA appears inadequate in South China. The PCA can affect the level of asthma control and asthma-specific quality of life. The factors contributing to inadequate PCA include primarily asthma duration, lung function and blood neutrophil counts.</p>

Study on HPLC fingerprint and quality control of Propolis / 中国中药杂志

<p><b>OBJECTIVE</b>To study on HPLC fingerprint of Propolis and to control it's quality.</p><p><b>METHOD</b>The chromatographic fingerprints of seven samples from different producing areas were determined by RP-HPLC.</p><p><b>RESULT</b>The chromatograms of Propolis from different producing areas were very similar.</p><p><b>CONCLUSION</b>The quality of Propolis can be controlled by determination the HPLC fingerprint.</p>

Protective effects of Cleistocalyx operculatus on lipid peroxidation and trauma of neuronal cells / 中国中药杂志

<p><b>OBJECTIVE</b>To observe the protective effects of Cleistocalyx operculatus on lipid peroxidation in rat liver microsomes and on the trauma of PC12 cells induced by H2O2.</p><p><b>METHOD</b>The mouse liver homogenate lipid peroxidation assay and PC12 Cell culture and Cell viability (MTT assay) were applied.</p><p><b>RESULT</b>Cleistocalyx operculatus showed strong protective effects on lipid peroxidation in rat liver microsomes in a dose-dependent manner and exhibited potent protective effects on the trauma of PC12 cells induced by H2O2 (200 micromol x L(-1)) when the concentration reached 1.00 g x L(-1).</p><p><b>CONCLUSION</b>Cleistocalyx operculatus may be used as antioxidant to prevent or delay the pathogenesis of neural cell diseases.</p>