Increasing energy expenditure through activation of brown adipose tissue (BAT) is a critical approach to treating obesity and diabetes. In this study, rutin, a natural compound extracted from mulberry and a drug used as a capillary stabilizer clinically for many years without any side effects, regulated whole-body energy metabolism by enhancing BAT activity. Rutin treatment significantly reduced adiposity, increased energy expenditure, and improved glucose homeostasis in both genetically obese (Db/Db) and diet-induced obesity (DIO) mice. Rutin also induced brown-like adipocyte (beige) formation in subcutaneous adipose tissue in both obesity mouse models. Mechanistically, we found that rutin directly bound to and stabilized SIRT1, leading to hypoacetylation of peroxisome proliferator-activated receptor γ coactivator-1α protein, which stimulated Tfam transactivation and eventually augmented the number of mitochondria and UCP1 activity in BAT. These findings reveal that rutin is a novel small molecule that activates BAT and may provide a novel therapeutic approach to the treatment of metabolic disorders.-Yuan, X., Wei, G., You, Y., Huang, Y., Lee, H. J., Dong, M., Lin, J., Hu, T., Zhang, H., Zhang, C., Zhou, H., Ye, R., Qi, X., Zhai, B., Huang, W., Liu, S., Xie, W., Liu, Q., Liu, X., Cui, C., Li, D., Zhan, J., Cheng, J., Yuan, Z., Jin, W. Rutin ameliorates obesity through brown fat activation.

Extracellular matrix protein 1 (ECM1) is a glycoprotein involved in a number of biologic processes. To investigate the expression of ECM1 in hepatocellular carcinoma (HCC) and determine its correlation with tumor progression and prognosis, the expression levels of ECM1 in three HCC and one normal liver cell lines, tumor, and corresponding adjacent tissues from 18 HCC patients were analyzed by reverse transcription polymerase chain reaction (RT-PCR) and Western blotting. Immunohistochemistry assay was used to determine the expression of ECM1 in HCC and corresponding paracarcinomatous tissues from 77 patients. The results of Western blotting were consistent with the results from RT-PCR analysis of ECM1 mRNA expression. Among the four cell lines, the expression level in HCCLM3, which with the highest metastatic potential, was significantly higher than that with lower (P < 0.05); while ECM1 expression was not detected in normal liver cell line. Expression level of ECM1 was significantly increased in HCC compared with adjacent and normal liver tissues (P < 0.05). Immunohistochemically, the expression of ECM1 in HCC was judged to be positive in 57 (74.0%) cases, significantly higher than that in corresponding paracarcinomatous tissues (P < 0.01), and it was associated with tumor size (P = 0.036), number of tumor nodules (P = 0.048), TNM stage (P = 0.029), and vascular invasion (P = 0.007). In particular, the expression of ECM1 was found to be an independent factor for predicting overall and disease-free survival of HCC. The expression level of ECM1 was associated with metastatic potential of HCC, and its abnormal expression may be used as a predictive factor of unfavorable prognosis and recurrence for HCC after surgery.

2-(2-Phenylethyl) chromones are the major constituents responsible for the quality of agarwood, which is one of the most valuable non-timber products used as incenses, perfumes, traditional medicines and other products. In this study, cell suspension culture of Aquilaria sinensis (Lour) Gilg was used to monitor the eliciting effects of crude fungal extracts on cell growth and chromones production. Crude extracts of Melanotus flavolivens (B. etc) Sing. prepared with different solvents were used to elicit the production of 2-(2-phenylethyl) chromones in cell suspension cultures of A. sinensis. Four 2-(2-phenylethyl) chromones, 6,7-dimethoxy-2-(2-phenylethyl) chromone (1), 6,7-dimethoxy-2-[2-(4¢-methoxyphenyl)ethyl] chromone (2), 6-methoxy-2-[2-(4¢-methoxyphenyl)ethyl] chromone (3) and 6-methoxy-2-(2-phenylethyl) chromone (4), were detected by LC-MS in the cell suspension culture of A. sinensis elicited with crude extracts of M. flavolivens. Three hundred and seventy eight, 196 and 31 lg g )1 DW of 2-(2-phenylethyl) chromones were obtained in the cell cultures induced by water extracts, 50 and 95% ethanol extracts of M. flavolivens, respectively. The results show that water-soluble materials in the crude extracts are the main components inducing the production of 2-(2-phenylethyl) chromones in the cell cultures.

Herpes simplex virus type 1 (HSV-1) is a commonly occurring human pathogen worldwide. There is an urgent need to discover and develop new alternative agents for the management of HSV-1 infection. Tripterygium hypoglaucum (level) Hutch (Celastraceae) is a traditional Chinese medicine plant with many pharmacological activities such as anti-inflammation, anti-tumor and antifertility. The usual medicinal part is the roots which contain about a 1% yield of alkaloids. A crude total alkaloids extract was prepared from the roots of T. hypoglaucum amd its antiviral activity against HSV-1 in Vero cells was evaluated by cytopathic effect (CPE) assay, plaque reduction assay and by RT-PCR analysis. The alkaloids extract presented low cytotoxicity (CC(50) = 46.6 μg/mL) and potent CPE inhibition activity, the 50% inhibitory concentration (IC(50)) was 6.5 μg/mL, noticeably lower than that of Acyclovir (15.4 μg /mL). Plaque formation was significantly reduced by the alkaloids extract at concentrations of 6.25 μg/mL to 12.5 μg/mL, the plaque reduction ratio reached 55% to 75 which was 35% higher than that of Acyclovir at the same concentration. RT-PCR analysis showed that, the transcription of two important delayed early genes UL30 and UL39, and a late gene US6 of HSV-1 genome all were suppressed by the alkaloids extract, the expression inhibiting efficacy compared to the control was 74.6% (UL30), 70.9% (UL39) and 62.6% (US6) respectively at the working concentration of 12.5 μg/mL. The above results suggest a potent anti-HSV-1 activity of the alkaloids extract in vitro.