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Hao Jia Xu Re Qing Granules (HJ), is an effective clinically used antipyretic based on traditional Chinese medicine. Although its antipyretic therapeutic effectiveness is obvious, its therapeutic mechanism has not been comprehensively explored yet. In this research, we first identified potential biomarkers which may be relevant for the antipyretic effect of HJ based on urine metabolomics using ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS). A rat model of fever was established using the yeast-induced febrile response. Total-ion-current metabolic profiles of different groups were acquired and the data were processed by multivariate statistical analysis-partial least-squares discriminant analysis. As envisioned, the results revealed changes of urine metabolites related to the antipyretic effect. Fourteen potential biomarkers were selected from the urine samples based on the results of Student's t-test, "shrinkage t", variable importance in projection and partial least-squares discriminant analysis. N-Acetylleucine, kynurenic acid, indole-3-ethanol, nicotinuric acid, pantothenic acid and tryptophan were the most significant biomarkers found in the urine samples, and may be crucially related to the antipyretic effect of HJ. Consequently, we propose the hypothesis that the significant antipyretic effect the HJ may be related to the inhibition of tryptophan metabolism. This research thus provides strong theoretical support and further direction to explain the antipyretic mechanism of HJ, laying the foundation for future studies., (© 2018 John Wiley & Sons, Ltd.)

To against the emergence of drug-resistent candidiasis, the studys of synergism of natural compounds combine with antifungal agents in vitro showed a continuous growth in recent years. The paper reviewed recent progresses to compare the synergetic effect by FICI method, and to conclude the synergetic mechanisms which have been confirmed as a reference for futher study.

Objective: To study the effect of HGD on diabetic cardiomyopathy and its mechanism., Methods: The T2-DM rats model was established by combining high fat diet with STZ. The blood glucose, insulin, myocardial fibrosis and TGF-beta1/Smad3 signaling pathway were observed; TGF-beta1 and Smad3 mRNA expression were detected by RT-PCR method, protein expression detected by immunohistochemical method., Results: HGD obviously reduced fasting blood glucose, insulin, improved insulin resistance, reduced myocardial hydroxyproline contents, lowered cardiac index, significantly inhibited over-expression of TGF-beta1/SMAD3 mRNA and protein in diabetic rats cardiac., Conclusion: HGD can obviously prevent experimental diabetic myocardial fibrosis through the regulation effect on TGFbeta1/Smad3 signaling pathway.

Fifteen limonoids, meliatoosenins E-S (1-15), and 10 known compounds were isolated from the fruits of Melia toosendan. Their structures were elucidated on the basis of extensive spectroscopic methods including DEPT, HSQC, HMBC, (1)H-(1)H COSY, and ROESY experiments. All the compounds were evaluated for antiproliferative activity using A-549 and HL-60 cell lines., (Copyright © 2011 Elsevier Ltd. All rights reserved.)

Objective: To observe the anti-atherosclerotic effect and its possible mechanisms of Modified Zhenzhu Tiaozhi Capsule (MZTC) in rabbits., Methods: 50 rabbits were divided into five groups, i.e., the normal group, the model group, the simvastatin group (3 mg/kg), the high dose MZTC group (1.6 g crude drug/kg), and the low dose MZTC group (1.6 g crude drug/kg), respectively, ten in each group. The atherosclerosis (AS) model was established by feeding rabbits with high fat diet. Corresponding medicines were administrated on the basis of high fat diet for twelve successive weeks. Levels of blood lipids, serum superoxide dismutase (SOD), malondialdehyde (MDA), and nitric oxide (NO) were detected. The area of the aortic tunica intima plaque was determined. The pathological changes of the aorta were observed., Results: Compared with the model group, serum levels of total cholesterol (TC), triglyceride (TG), low-density lipoprotein cholesterol (LDL-C), MDA, and atherosclerotic index (AI) were significantly lowered in the MZTC groups (P<0.05, P<0.01), while serum levels of high-density lipoprotein cholesterol (HDL-C), SOD, and NO obviously increased (P<0.05, P<0.01). Serum levels of TC, TG, LDL-C, and in the MZTC groups were obviously higher than those of the simvastatin group (P<0.01), and there was insignificant difference in other indices. The ratio of the aortic tunica intima plaque percentage to the total tunica intima area was also markedly lower than that of the model group (P<0.05, P<0.01). Results under light microscope indicated the pathological changes of the aorta was obviously attenuated., Conclusions: MZTC could inhibit the formation and development of AS plaque. Its mechanism might be associated with regulating lipids metabolism, antioxidation, and improving endothelial functions.

Objective: To observe the effect of fufang zhenzhu tiaozhi capsule (FTZ) on lipid metabolism in atherosclerotic rabbits., Methods: 50 rabbits were divided into five groups: normal control group, model group, simvastatin group, the high-dose group and low-dose group of FTZ. The atherosclerotic model was established by feeding the rabbits with high fat diet. The medicine interfered groups were administrated with homologous medicine on the base of high fat diet. All the rabbits were fed for 12 weeks. The blood lipids levels were determined just before the experiment and at the forth, the eighth and the twelfth weekend of the experiment. At the end of the experiment, serum apolipoprotein levels, liver lipid contents and the area of atherosclerotic plaque were determined respectively., Results: Compared with model group, TC, TG, LDL-C and ApoB levels were significantly decreased in FTZ groups (P < 0.05 or P < 0.01). The level of HDL-C and the ratio of ApoA I /ApoB were raised significantly (P < 0.05). The contents of TC,TG in liver tissue and the area percentage of atherosclerotic plaque were also markedly reduced (P < 0.05 or P < 0.01) in the FTZ groups., Conclusion: FTZ could efficiently regulate the abnormality of lipid metabolism in experimental atherosclerotic rabbits, and this maybe one mamechanisms of its antiatherogenic effect.

Four new limonoids (1, 3, 4, 6), named meliatoosenins A-D, eight new euphane- and tirucallane-type triterpenoids (8-15), named meliasenins A-H, and 13 known compounds have been isolated from the stem bark of Melia toosendan. The structures of new compounds were established on the basis of 1D and 2D NMR experiments ((1)H-(1)H COSY, HSQC, HMBC, and ROESY).

Ethnopharmacological Relevance: The herbal formula Xiangdan injection and its modifications have been used in traditional Chinese medicine for about hundreds years to alleviate pain and promoting blood., Aim: To investigate the anti-hypoxia active fraction of Xiangdan injection., Materials and Methods: Xiangdan injection was extracted by ligarine, chloroform, acetic ether, n-butanol and water, represented respectively by A, B, C, D and E. Five extractions were group on the L12(2(5)) orthogonal designed table. NIH mices anti-hypoxia experiment under normal pressure with rats was adopted on the basis of orthogonal design, prediction pharmacodynamics model of TCM prescriptions was established, and the simulation bias was evaluated by combining two scatterplots. The anti-hypoxia active fraction of Xiangdan injection was determined by experiments., Results: The prediction model of TCM prescriptions established in this study can predict the drug actions for different formulas, and PE%

Phytochemical investigation on the stem bark and wood of Trigonostemon chinensis led to the isolation of four new dinorditerpenoids, trigonostemons A-D (1, 3, 5, 6), a new phenanthrenone, trigonostemon E (7), and a new bisindole alkaloid, trigonostemon F (8). The structures were established by extensive spectroscopic methods. The absolute configurations of 1-6 were determined by X-ray crystallography, circular dichroism, quantum chemical TDDFT calculations, and chemical transformations. The relative configuration of 8 was confirmed by X-ray diffraction analysis.

Objective: To investigate the anti-hypoxia active fraction of Xiangdan injection., Methods: The anti-hypoxia experiment under normal pressure with mice was adopted on the basis of orthogonal design, and a support vector machine model was established for pharmacodynamics prediction of TCM prescriptions. Moreover, the anti-hypoxia active fraction of Xiangdan injection was determined by experimental confirmation., Results: The prediction model established in this study could predict the drug actions of different formulas., Conclusion: As indicated in model prediction and experimental confirmation, the pharmacodynamic actions of several formulas are superior to that of the original formula, and ADE has the best effect.

Four new 9,10-dihydrophenanthrenes, juncuenins A-D (1-4), three new phenanthrenes, dehydrojuncuenins A-C (5-7), and three known compounds were isolated from the whole plants of Juncus setchuensis. The structures of the new compounds were established on the basis of detailed 1D and 2D NMR studies.

Four new merrillianin-type sesquiterpenes, oligandrumins A-D (1-4), two new seco-prezizaane-type sesquiterpenes, veranisatins D and E (5 and 6), and a new phenylpropane glycoside, oligandrumin E (7), were isolated from the ethanol extract of pericarps of Illicium oligandrum, together with six known sesquiterpenoids and two phenylpropanoids. Their structures were established on the basis of extensive spectroscopic analyses. The structures of 1 and 2 were further confirmed by single-crystal X-ray diffraction experiments. Anislactone B (13) and the erythro form of anethole glycol (14) were shown to attenuate the damage induced by H(2)O(2) in SH-SY5Y cells.

Four new abietane diterpenoids, fortunins A-D (1-4), and six new 18-hydroxymethylene abietane diterpenoids, fortunins E-J (5-10), along with 12 known diterpenoids, were isolated from the bark of Cryptomeria fortunei. The structures of new compounds were established on the basis of 1D and 2D NMR and other spectroscopic analyses.

Investigation of the roots of Stemona tuberosa afforded five minor constituents, stemoenonine (1), 9a- O-methylstemoenonine (2), oxystemoenonine (3), 1,9a- seco-stemoenonine (4), and oxystemoninine (5), along with the known compound stemoninoamide (6). Their structures were elucidated by 1D and 2D NMR spectra and other spectroscopic studies. Alkaloids 1, 2, and 6, as well as the representative stemoninine-type alkaloid, stemoninine (7), were screened for antitussive activity in the citric acid-induced guinea pig cough model. Compounds 6 and 7 exhibited strong antitussive activity after oral and intraperitoneal administrations.

In our systematical investigation on Chinese Meliaceae plants, the stems of Cipadessa baccifera collected in Yunnan province were studied. Two new tetranortriterpenoids, cipadessalide ( 1) and rubralin D ( 2), one new pregnane, 3beta,4beta-dihydroxy-2beta-acetoxypregnan-16-one ( 3), and two new sesquiterpenoids, bacciferins A ( 4) and B ( 5), along with 10 known compounds were isolated. Their structures were elucidated by 1D and 2D NMR spectra and other spectroscopic studies, as well as chemical conversion.

Five new alkaloids, 6beta-hydroxystemofoline (1), 16-hydroxystemofoline (2), neostemofoline (3), protostemodiol (4), and 13-demethoxy-11(S*),12(R*)-dihydroprotostemonine (5), along with 10 known alkaloids, were isolated from stems and leaves of Stemona japonica. Their structures were elucidated by 1D and 2D NMR and other spectroscopic studies. The insecticidal activity of the agonist 16-hydroxystemofoline (2) and antagonist 13-demethoxy-11(S*),12(R*)-dihydroprotostemonine (5) was demonstrated by electrophysiological in vitro tests on the insect nicotinic acetylcholine receptor and by in vivo screenings against relevant agricultural insect pests.

Three new dimeric sesquiterpenoids, chloramultilides B-D ( 1- 3), along with 10 known sesquiterpenoids, were isolated from the whole plant of Chloranthus spicatus. Their structures were established by physical data (1D and 2D NMR, MS). The structure and absolute configuration of 1 was confirmed by X-ray crystallography. Compound 1 exhibited moderate in vitro antifungal activity.

Five new stemoninine-type alkaloids, bisdehydrostemoninine (1), isobisdehydrostemoninine (2), bisdehydroneostemoninine (3), and bisdehydrostemoninines A (4) and B (5), were isolated from the crude-alkaloid extract of the roots of Stemona tuberosa. Their structures were elucidated on the basis of one- and two-dimensional NMR and other spectroscopic studies. The relative configuration of 4 was determined by X-ray diffraction. Alkaloid 1 displayed significant antitussive activity in the citric acid-induced guinea pig cough model.