Analysis of active patents to investigate the frequency and patterns of Chinese herbal extract combinations claiming to treat heart disease

Objective:Using Chinese patents in force to investigate the frequency and patterns of Chinese herbal extract combinations claiming to treat heart disease.Methods:Patent documents were retrieved from the official website of the State Intellectual Property Office of the People’s Republic China.Cluster,frequency,and fuzzy cluster analyses were applied.Results:A high number of patents in force included high-frequency herbs such as Salvia miltiorrhiza,Panax ginseng,and Panax notoginseng,as well as high-frequency herbal families such as Araliaceae,Leguminosae,Labiatae,and Umbelliferae.Herb pairs such as P.ginsengþOphiopogon japonicus,S.miltiorrhizaþDalbergia odorifera,and P.ginsengþSchisandra chinensis are also commonly used,as well as herbal family pairs such as AraliaceaeþLiliaceae,LauraceaeþLeguminosae,and AraliaceaeþSchisandraceae.Traditional treatment principles for preventing and treating heart diseases was most-commonly based on simultaneously treating the liver and heart and treating the lung and spleen secondarily for choosing herbal combinations.Conclusion:Most of the high-frequency Chinese herbs in the patents investigated belong to the high-frequency herbal families,and herb pairs were commonly selected to coincide with the commonly-used herbal family pairs.Low-frequency Chinese herbs were also used,but generally belonged to the high-frequency herbal families,and were therefore similar to the highfrequency herbs in terms of traditional categories of taste and channel entered.The results reflect the use of traditional principles of formula composition,and suggest that these principles may indeed be an effective guide for further research and development of Chinese herbal extract combinations to prevent and treat heart diseases.

ERβ modulation and non-modulation of ERα by administration of geniposide and panax notoginseng saponins in SH-SY5Y cells

Objective:To illustrate the effect of geniposide (GP) and panax notoginseng saponins (PNS) on estrogen receptors (ER) including ERα and ERβ within the cytoplasm and nucleus of SH-SY5Y cells.Methods:Immunofluorescence was used to observe the distribution of ERα and ERβ in cytoplasm and nucleus,but Western blot was only for ERβ detection.q-PCR was applied to detect NR3C1,S100A6 and LGALS1downstream mRNA gene expression levels of ER.Results:Through analyzing fluorescence intensity under the administration of GP and PNS in SHSY5Y cells,we found that the distribution of ERα has not been affected.We also discovered that GP and/or PNS significantly stimulated the transportation of ERβ into the nucleus in a timedependent manner (all P <.001).When SH-SY5Y cells were treated with supplements of GP,PNS,GP + PNS at 15 minutes,30 minutes and 45 minutes,the distribution of ERβ in the nucleus significantly increased compared with that in control group (all P <.001).Evidently,treatment with GP,PNS,GP + PNS was able to significantly increase the levels of ERβ protein within the nucleus compared with control group at both 30 minutes and 45 minutes intervals (all P <.001).Furthermore,GP and PNS showed signs of activating to NR3C1 and LGALS1,two genes downstream of ER.It is possible that the 5100A6 gene mainly encoded the downstream gene in ERα's signaling pathway,which was not affected after the treatment of GP and/or PNS.Conclusion:The distribution and expression of ERβ has been modulated under the administration of GP + PNS within the SH-SY5Y cells,whereas ERα has not.GP and PNS in combination may play an estrogenic-like effect with selectivity on ERβ modulation.

Effect of Tangnaikang on TGF-β_1-induced transdifferentiation of human renal tubular epithelial HK-2 cells

OBJECTIVE: To explore the function of Tangnaikang (TNK) in the prevention and treatment of renal interstitial fibrosis through transdifferentiation of the human renal tubular epithelial cell line HK-2 induced by transforming growth factor-β1(TGF-β1).METHODS: HK-2 cells cultured in dulbecco's modified eagle medium/F12 (1∶1) with 10% fetal calf serum were divided into six groups: blank control group, TGF-β1 group (TGF-β1 10 ng/mL), serum control group (TGF-β1 10 ng/mL+10% serum), treatment group 1 (TGF-β1 10 ng/mL+ 5% TNK serum),treatment group 2 (TGF-β1 10 ng/mL+10% TNK serum), and treatment group 3 (TGF-β1 10 ng/mL+20% TNK serum). Cell proliferation was detected by 4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Expression of α-smooth muscle actin (α-SMA) and E-cadherin were observed by immunohistochemical assay. The contents of collagen Ⅰ (Col Ⅰ), collagen Ⅲ (Col Ⅲ), and fibronectin (FN) in the culture medium supernatant were detected by ELISA.RESULTS: E-cadherin was expressed and α-SMA was not expressed in normal HK-2 cells. In HK-2 cells cultured with TGF-β1,α-SMA expression significantly increased, HK-2 cells significantly proliferated, and secretion of Col Ⅰ, Col Ⅲ, and FN significantly increased compared with the blank control group (all P<0.05). In the HK-2 cells cultured with TGF-β1 and TNK serum, the expression of α-SMA significantly decreased, the expression of E-cadherin significantly increased, and the cell proliferation and the secretion of Col Ⅰ, Col Ⅲ and FN were significantly inhibited compared with the TGF-β1 group (all P<0.05).CONCLUSION: TNK can inhibit cell proliferation and reduce secretion of Col Ⅰ, Col Ⅲ, and FN.This indicates that TNK can inhibit transdifferentiation of human renal tubular epithelial cells induced by TGF-β1, with the effect of preventing and treating renal interstitial fibrosis.

Antihyperglycemic and antihyperlipidemic action of cinnamaldehyde in C57blks/j Db/db mice

OBJECTIVE:To investigate the effects of cinnamaldehyde(CA),an active and major compound in cinnamon,on glucose metabolism and insulin resistance in C57BLKS/J db/db mice.METHODS:Sixteen male C57BLKS db/db mice were randomly divided into control and CA treatment groups.CA was given(20 mg.kg-1.day-1,p.o.) for 4 weeks.Pure water was given to control and db/+ mice.Subsequently,the levels of fasting blood glucose(FBG),fasting serum insulin,triglyeride,cholesterol,low-density lipoprotein-cholesterol(LDL-C),high-density lipoprotein-cholesterol(HDL-C),and free fatty acids(FFA),as well as the mRNA content of adiponectin and tumor necrosis factor(TNF)-α in adipose tissue,glucose transporter type 4(GLUT-4) in skeletal muscle,and protein expressions of Akt,phospho-Akt(Thr308),AMPKα,phospho-AMPKα(Thr172) in skeletal muscle were measured.RESULTS:1) CA decreased serum levels of FBG and insulin as well as body weight in db/db mice;2) CA increased serum HDL-C levels;3) CA significantly decreased the mRNA expression of TNF-α in adipose tissue and upregulated mRNA expression of GLUT-4 in skeletal muscle;4) protein expression of p-Akt was increased in CA-treated mice,but Akt,AMPKα and p-AMPKα showed no change.CONCLUSION:CA has antihyperglycemic and antihyperlipidemic actions in db/db mice and could be useful in the treatment of type-2 diabetes.

Multiple measurements of quasars acting as standard probes: Model independent calibration and exploring the dark energy equation of states

Recently, two classes of quasar samples were identified, which are promising as new cosmological probes extending to higher redshifts. The first sample uses the nonlinear relation between the ultraviolet and X-ray luminosities of quasars to derive luminosity distances, whereas the linear sizes of compact radio quasars in the second sample can serve as standardized rulers, providing angular-diameter distances. In this study, under the assumption of a flat universe, we refreshed the calibration of multiple measurements of high-redshift quasars(in the framework of a cosmological-model-independent method with the newest Hubble parameters data). Furthermore, we placed constraints on four models that characterize the cosmic equation of state(w). The obtained results show that:(1) the two quasar samples could provide promising complementary probes at much higher redshifts,whereas compact radio quasars perform better than ultraviolet and X-ray quasars at the current observational level;(2) strong degeneracy between the cosmic equation of state(w) and Hubble constant(H0) is revealed, which highlights the importance of independent determination of H0 from time-delay measurements of strongly lensed quasars;(3) together with other standard ruler probes, such as baryon acoustic oscillation distance measurements, the combined QSO+BAO measurements are consistent with the standard ΛCDM model at a constant equation of state w =-1;(4) ranking the cosmological models, the polynomial parametrization gives a rather good fit among the four cosmic-equation-of-state models, whereas the Jassal-Bagla-Padmanabhan(JBP) parametrization is substantially penalized by the Akaike Information Criterion and Bayesian Information Criterion.