Various column chromatography, such as silica gel, Sephadex LH-20, ODS, and semi-preparative HPLC was used to isolate and purify the chemical constituents from Cinnamomum cassia. The structures were determined on the basis of NMR and MS spectral data analysis, together with the comparison with literature data. Fifteen compounds were isolated from the 85% aqueous ethanol extract of C. cassia, and their structures were identified as (2R, 3R)-5,7,3',4'-tetramethoxyflavan-3-ol( 1), (2R, 3R)-5,7-dimethoxy-3',4'-methylenedioxyflavan-3-ol (2), coumarin (3), cinnamic acid (4), (E)-2-hydroxy-phenylpropionic acid cinnamoyl ester (5), 3, 3', 4, 4'-tetrahydroxy biphenyl (6), methylstictic acid (7), epi-boscialin (8), (1R,2S,3S,4S)-2,3-epoxy-1, 4-dihydroxy-5-methyl-5-cyelohexene (9), 4,5-dihydroxy-3-methyl cyclohex-2-enone (10), cis-4-hydroxymellein (11), and 2-hydroxy-4-methoxyl-cinnamaldehyde (12). Compounds 5-11 were obtained from this genus plants for the first time.
Cinnamomum aromaticum ; chemistry ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Mass Spectrometry ; Molecular Structure

This study is to develop a sensitive method by using reversed-phase high performance liquid chromatography coupled with UV detector (HPLC-UV) to simultaneously determine four bioactive compounds, iriflophenone 3-C-beta-D-glucoside, iriflophenone 3,5-C-beta-D-diglucoside, mangiferin, and iriflophenone 2-O-alpha-L-rhamnoside in the leaves of Aquilaria sinensis. An Agilent Zorbax SB-C, column (4, 6 mm x 250 mm, 5 microm) was used, and the gradient elution was performed with mobile phase of 0.1% aqueous phosphoric acid and acetonitrile at a flow rate of 1 mL x min(-1). The detection wavelength was 280 nm, and the column temperature was 25 degrees C. The four marker compounds were well separated with good linearity (R2 > 0.9990), precision, stability and repeatabili y. The-recovery rates were in the range of 98.80%-101.39%. For 15 branch of the leaves, the contents of iriflophenone 3-C-beta-D-gluoside, iriflophenone 3,5-C-beta-D-diglucoside, mangiferin, and iriflophenone 2-O-alpha-L-rhamnoside were between 0.41-14.48, 0.72-3.85, 4.30-29.07, 0.24-5.06 mg, respectivley. This method is precise, accurate and reliable, which provides an efficient way for the quality control of the leaves of A. sinensis. This will promote the comprehensive usage of this plant.
Benzophenones ; analysis ; Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; analysis ; Plant Leaves ; chemistry ; Spectrophotometry, Ultraviolet ; methods ; Thymelaeaceae ; chemistry ; Xanthones ; analysis

Referring to the rapid developed life science and the higher requirements for the approval of innovative Chinese drugs in recent years, this paper described systematically the discovery, research and development (R&D) approaches for the innovative Chinese drugs under the new situation from the following five aspects, i. e., active components discovered from TCMs, the discovery of effective fractions of TCMs and their formulae, the R&D of TCM innovative drugs based on famous classic prescriptions and famous Chinese patent drugs, and the transformation of clinical effective prescriptions, on the basis of analysing the advantages of innovative drugs derived from natural products based on TCM theories and the problems existed in current R&D of new TCM drugs. Moreover, five suggestions are also given for the rapid development of TCM innovative drugs in China. All these will provide reference for the R&D of TCM innovative drugs.
China ; Drug Discovery ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; pharmacology ; Humans ; Medicine, Chinese Traditional ; trends ; Research

Acute Coronary Syndrome ; etiology ; Aortic Valve Insufficiency ; Female ; Heart Valve Prosthesis ; adverse effects ; Humans ; Middle Aged ; Prosthesis Failure

In this study, the flow injection (FI) technology combined with the unique step wise multiple ions monitoring scanning (step-wise MIM) mode of Qtrap-MS was first established for the identification and discrimination of eight Murraya species. It only takes 5 min for each sample to detect approximate 600 compounds. The characteristic MS chromatograms of eight Murraya plants were analyzed by Analyst and SIMCA-P. The results of PCA showed that sect. Murraya and sect. Bergera were clearly divided into two categories, suggesting that there is difference in the chemical compositions between these two groups. Further detail analysis of the MS data could realize the preliminary structure elucidation of the component types contained in different plants. The main components in M. exotica and M. alata are coumarins, and polymethoxyflavones are rich in M. paniculata, while carbazole alkaloids are the major ones in sect. Bergera plants. The results are consistent with our previous comprehensive analysis of the chemical components of Murraya species. In conclusion, our research confirmed that FI-Qtrap-MS technology can be used for rapid identification and differentiation of similar plant species, providing reference for chemical taxonomy and a new method for the quality evaluation of medicinal materials.

Modern pharmacological studies have shown that Cistanche deserticola (C. deserticola) has a protective effect on the liver, but its active fraction and mechanism are not clear. In order to identify the effective fraction of C. deserticola Y. C. Ma, an acute alcoholic liver injury model in mice was established with 56-proof Erguotou and different fractional extracts of C. deserticola Y. C. Ma (total glycosides, polysaccharides, and oligosaccharides) were administered. After 14 days of oral administration, liver pathology and lipid deposition were measured and the expression of nuclear factor E2-related factor (Nrf-2), kelch-like ECH-associated protein-1 (Keap-1), and plasmalemma vesicle-associated protein-1 (PV1) were measured by immunofluorescence. The levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), endotoxin (ET), diamine oxidase (DAO), and D-lactic acid (D-LA) in serum, and superoxide dismutase (SOD), glutathione peroxidase (GSH-Px), catalase (CAT), and malondialdehyde (MDA) in liver were measured by ELISA. All animal experiments were carried out with approval of the Experimental Animal Welfare Ethics Committee of the Peking University Health Science Center. The results show that the total glycosides of C. deserticola Y. C. Ma (400 mg·kg^-1) could decrease liver pathology, decrease serum endotoxin, diamine oxidase, and D-lactic acid, and reduce hepatic lipid deposition. Total glycosides also promoted Nrf-2 transfer into the nucleus and decreased the expression of Keap-1 and PV1. In summary, the total glycosides of C. deserticola Y. C. Ma had a protective effect in acute alcoholic liver injury and the mechanism may be related to the activation of the Nrf-2/Keap-1 pathway, improvement of intestinal wall integrity, and inhibition of the transport of harmful substances into the liver.

Multi-target drugs attract increasing attentions for the therapy of complicated neurodegenerative diseases. In this study, a computer-assisted strategy was applied to search for multi-target compounds by the pharmacophore matching. This strategy has been successfully used to design dual-target inhibitor models against both the acetylcholinesterase (AChE) and poly (ADP-ribose) polymerase-1 (PARP-1). Based on two pharmacophore models matching and physicochemical properties filtering, one hit was identified which could inhibit AChE with IC50 value of (0.337 +/- 0.052) micromol x L(-1) and PARP-1 by 24.6% at 1 micromol x L(-1).
Acetylcholinesterase ; metabolism ; Cholinesterase Inhibitors ; pharmacology ; Computer-Aided Design ; Drug Discovery ; methods ; Poly(ADP-ribose) Polymerase Inhibitors

Objective To study the distribution of Oncomelania hupensis snails in mountainous regions and the dynamic charaeteristics of the distribution.Methods An environment calledLanbaoclosed to Puge County.Sichuan Provinee WaS selected as the study field.Random sampling was designed to determine the investigation sites.The snails were collected and the hying snaila were identified by the method of dissection in the laboratory.The distribution of snails was analyzed by some statistical indices,such as mean,variance and so on.Then the negative binomial distribution.log-normal distribution and exponential distribution were fitted to the snail data by the method of maximum likelihood estimation to explore the snail distribution in different time.Results The negative binomial distribution was fitted well to the snail data in April,May,July,August,September,November in 2008,and no distribution was fined to the snail data in June,October.December in 2008 and February in 2009.Conclusions The distribution of Oncomelania hupensis in mountainous regions is not simple negative binomial distribution,but pwbably a dynamic process and an uncertain distribution.

AlM:To explore treatment efficacy of the lower eyelid twitch muscle transposition surgery in senile entropion.METHODS:Fifty cases (86 eyes) of senile lower eyelid entropion patients underwent lower eyelid twitch muscle transposition correction surgery as the experimental group, and the other 42 cases (68 eyes) of senile lower eyelid entropion patients received orbicularis muscle shortening correction as controls group. The correction rate, double eyelid symmetry and overcorrection rate of patients were observed one week after surgery. The patients were followed up for 6~12mo to be observed the long-term recurrence rate, double eyelid symmetry and overcorrection rate.RESULTS: One week after operation, eyelid symmetry, overcorrection rate of experimental group and control group had significant difference (P<0. 05); After followed up for 6 ~12mo, eyelid symmetry, overcorrection rate of experimental group and control group had significant difference (P<0. 05). CONCLUSlON: Folding and orbicularis muscle shortening treatment of senile entropion was compared with the lower eyelid twitch muscle transposition surgery treatment of senile entropion, We can find that clinical results in double eyelid surgery symmetry and overcorrection rate are of obvious advantage.

Objective To compare the durability and cost-effectiveness of slightly acidic electrolyzed oxidizing water(SAEOW),ortho-phthalaldehyde (OPA) and glutaraldehyde (GA) in two conditions,i.e.,continuous machine cleaning and continuous manual cleaning.Methods The maximal numbers of endoscopes which were disinfected by the three disinfectants at its minimal effective concentration,as well as the corresponding costs were compared.The cost-effectiveness of three disinfectants were evaluated with revenue-incremental cost analysis.Results The number of endoscopes disinfected by ortho-phthalaldehyde was larger than that by two other disinfectants,140 ± 2 by machine wash and 226 ± 1 by hand washing;followed by glutaral disinfectant,88 ± 2 and 108 ± 2 by machine wash and hand wash,respectively;slightly acidic electrolyzed oxidizing water disinfected the least endoscopes,34 ± 2 and 39 ± 1 by machine wash and hand wash.There were significant differences among these three disinfectants (all P ＜ 0.05).Compared with GA,one more Yuan invested to OPA yielded 2.24 yuan more under the condition of machine wash and 3.14 yuan more under the condition of hand wash.Compared with GA,one Yuan invested in SAEOW produced 47.14 yuan by machine wash and 45.6 Yuan by hand wash.Conclusion Under full workload,orthophthalaldehyde shows the best durability among the three disinfectants,while slightly acidic electrolyzed oxidizing water shows the highest economic benefit.