Volume 7,Issue 4,2015 Table of Contents

1 Identification of Icaritin Metabolites in Rats by LC-MS/MS

Lin-hu Ye

2015, 7(4).

[Abstract](499) [HTML](0) [PDF 0.00 Byte](8)

Abstract:
Objective Icaritin is the main aglycone and also active intestinal metabolite of prenylflavonoids from the Chinese materia medica Epimedii Herba. Modern pharmacological studies have demonstrated that icaritin has a wide range of biological activities. However, its metabolites and biotransformation pathways have not yet been comprehensively investigated. The present study aims to identify icaritin metabolites in rats by using a sensitive and effective LC-MS/MS method. Methods The plasma and urine samples of rats were collected before (blank) and after oral administration of icaritin, and subjected to liquid-liquid extraction with ethyl acetate. The full-scan LC-MS chromatograms of the plasma and urine samples were compared with those of blank samples to detect the possible metabolites, which were later identified by their product ion spectra. Results A total of 23 metabolites were identified, and conjugated icaritins produced by glucuronidation, glycosylation, and sulfation were its major metabolites. Minor demethylation, hydrogenation, and oxidation metabolites were also found. Conclusion Phase II metabolism is the main metabolic pathway of icaritin.

2 HMGR, SQS, β-AS, and Cytochrome P450 Monooxygenase Genes in Glycyrrhiza uralensis

Rui Yang

2015, 7(4).

[Abstract](430) [HTML](0) [PDF 0.00 Byte](9)

Abstract:
Glycyrrhiza uralensis is frequently used in traditional Chinese medicine. This plant contains a large amount of effective constituents, including triterpenoids and flavonoids. Among them, glycyrrhizin is believed to be the marker compound to characterize the quality of G. uralensis based on Chinese Pharmacopoeia. Many studies have shown that glycyrrhizin possesses various pharmacological activities, such as antibacterial, antiviral, antitumor, anti-inflammatory, and immune-stimulating activities. In this paper, we summarized the cloning, characterization, expression, and polymorphism analysis of several functional genes involved in glycyrrhizin biosynthesis in G. uralensis.

3 Simultaneous Determination of Four Substances in Plasma and Dermal Microdialysates of Guinea Pig after Different Acupoints Administration of Fufang Baijiezi Gel

Guo-hua Wang

2015, 7(4).

[Abstract](481) [HTML](0) [PDF 0.00 Byte](9)

Abstract:
Objective To study the pharmacokinetic properties of Fufang Baijiezi Gel (FBG) after differernt acupoints administration. Methods A sensitive liquid chromatography tandem mass spectrometry method (LC-MS) was developed and validated to determine sinapine thiocyanate, tetrahydropalmatine, 6-gingerol, and asarinin in plasma of guinea pig and dermal microdialysates simultaneously. Microdialysates were separated on a Ultimate? XB-Phenyl analytical column (150 mm × 2.1 mm, 5μm) and detected by electrospray ionization (ESI) in selected ion monitoring (SIM) mode. The method was validated in terms of selectivity, linearity, sensitivity, and recovery. A signi?cant difference was observed in main pharmacokinetic parameters of Cmax, tmax, and AUC between acupoints administration and nonacupoints administration. Acupoints administration resulted in a more obvious increase in bioavailability of sinapine thiocyanate, tetrahydropalmatine, 6-gingerol, and asarinin than nonacupoints administration according to the above LC-MS assay method.

4 Investigation of Mechanism of Premature Ovarian Failure Regulation by Kidney-tonifying Herbs and Liver-clearing Herbs in Dingjing Decoction

Xiu-feng Wang

2015, 7(4).

[Abstract](562) [HTML](0) [PDF 0.00 Byte](10)

Abstract:
Objective To investigate the mechanisms through which kidney-tonifying herbs (KTHs) and liver-clearing herbs (LCHs) in Dingjing Decoction (DJD) regulate premature ovarian failure (POF). Methods One hundred and fifty Sprague-Dawley rats were randomly divided into five groups such as control, model, KTHs, LCHs, and DJD groups. POF-related biological molecules were examined. Factor analysis was performed to investigate the regulatory networks and key biomolecules involved in mediating POF after treatment with KTHs and LCHs. Results The master regulatory factors in the reproductive endocrine network associated with KTHs intervention included four molecules in the pituitary-ovarian axis, cortisol (CORT) in the target gland of pituitary-adrenal axis, and some molecules in the hypothalamus. In contrast, the master regulatory factors associated with LCHs intervention included four molecules in the pituitary-ovarian axis and some molecules in the hypothalamus; No biomolecules in the pituitary-adrenal axis were involved in the LCH-mediated mechanisms. Gonadotropin-releasing hormone (GnRH), which was identified as a common biological molecule in the hypothalamus, was involved in regulating the reproductive endocrine network in association with KTHs intervention. Conclusion KTHs directly regulates biological molecules in the pituitary-adrenal axis and indirectly regulates those in the pituitary-adrenal axis through the hypothalamus, while the LCHs only exert its effects indirectly. GnRH is the key biological molecule associated with KTHs intervention.

5 Comparison on Traditional and Machinery Decoctions for Da-cheng-qi Decoction Based on Chemical Ingredients, Pharmacological Functions, and Clinical Trials

Rui-fang Xie

2015, 7(4).

[Abstract](487) [HTML](0) [PDF 0.00 Byte](8)

Abstract:
Objective Patients and doctors often have questions about the equivalence of traditional and machinery decoctions. In this article, using Da-cheng-qi Decoction (DCQD) as a model of formula, traditional decoction (TD), machinery decoction under high pressure (MDHP), and machinery decoction under normal pressure (MDNP) were compared. Methods For chemical structures, HPLC fingerprints were established and evaluated using AHP combined with CRITIC weighing method; For animals’ effects, the experiments of small intestinal propulsion were conducted; For clinical effects, a randomized clinical trial (RCT) was designed and performed. Results Although there were some differences between TD and MDNP for chemical ingredients, there was no significant difference for animal experiments and clinical trials (P > 0.05). Conclusion The traditional and machinery decoctions of DCQD are bioequivalent.

6 Antipyretic Effects of Eupatorium chinense L. and its Mechanism

Yi-ping Jiang

2015, 7(4).

[Abstract](935) [HTML](0) [PDF 0.00 Byte](6)

Abstract:
Objective To investigate the antipyretic effect of Eupatorium chinense L. and its mechanism. Methods The content of arginine vasopressin (AVP) in ventral septal area (VSA) and blood plasma, and cyclic adenosine monophosphate (cAMP) levels of hypothalamus and blood plasma were determined by enzyme linked immunosorbent assay. Results The body temperature (Tb) was decreased at 1 h after administration of E. chinense (3 and 6 g/kg) and Aspirin (0.3 g/kg) respectively, which was significantly different from the temperature of fever model group. The antipyretic effect of Aspirin and E. chinense lasted for longer time. Aspirin (0.3 g/kg) and E. chinense (3 and 6 g/kg) reduced the level of cAMP in hypothalamus of fever rats and increased AVP content in plasma. The changes in cAMP content in plasma of all drug treatment groups were not obvious. Conclusion E. chinense has strong antipyretic effect and may affect the production of AVP and cAMP in fever rats.

7 Hypoglycemic and Hypolipidemic Effects of Lycium barbarum Polysaccharide in Diabetic Rats

Rong Zhao

2015, 7(4).

[Abstract](855) [HTML](0) [PDF 0.00 Byte](11)

Abstract:
Objective To study the antidiabetic effects and the underlying molecular mechanisms of Lycium barbarum polysaccharide (LBP) and its DEAE cellulose elution fraction LBP-IV in diabetic rats induced by high fat diet (HFD) and streptozotocin (STZ). Methods After ig administration of LBP-IV [50, 100, and 200 mg/(kg·d)] and LBP [100 mg/(kg?d)] once daily for consecutive 4 weeks to diabetic rats, the glucose and lipids in blood, and mRNA expression of phosphoenolpyruvate carboxykinase (PEPCK), sterol regulatory element binding-protein-1c (SREBP-1c), and fatty acid synthase (FAS) in liver were determined. Results Ig administration of LBP and LBP-IV significantly decreased the levels of blood glucose, HbA1c, TC, TG, and LDL-C, as well as the hepatic mRNA expression of PEPCK, SREBP-1c, and FAS, whereas significantly increased the oral glucose tolerance of diabetic rats. Conclusion Our findings suggest that the antidiabetic effects of LBP and LBP-IV are associated with the decreased hepatic mRNA expression of PEPCK, SREBP-1c, and FAS in HFD-STZ induced diabetic rats.

8 Efficacy and Safety of BBR in Patients with Type 2 Diabetes Mellitus: A Meta-Analysis

Xiao-chen Wei

2015, 7(4).

[Abstract](597) [HTML](0) [PDF 0.00 Byte](7)

Abstract:
Objective To assess the efficacy and safety of berberine (BBR) in patients with type 2 diabetes mellitus (T2DM) by performing a systematic review. Methods PubMed, Cochrane Library, Embase, CNKI, and CBM were searched until May 2014. The randomized controlled trials (RCTs) of the effects of BBR on blood glucose in patients with T2DM were included. The quality of RCTs was assessed by the Jadad scale, and the Review Manager 5.1 software was used for data syntheses and analyses. Results Seventeen RCTs involving 1198 patients were included. The methodological quality of these RCTs was generally low. Compared with the control groups (placebo or no intervention with medicine), BBR suggested the statistically significant benefits in improving fasting blood glucose (FBG), postprandial blood glucose (PBG), glycosylated hemoglobin, and homeostasis model assessment of insulin resistance. Subgroups analysis of BBR compared with metformin (MET) showed that 1.5g/d MET was significantly better than BBR (0.9?1.5 g/d) in lowering FBG and PBG. However, there was no significant difference between 1.5g/d BBR and 0.75g/d MET groups in blood glucose profiles. In comparison with rosiglitazone, BBR suggested the statistically significant benefits in lowering FBG. And there was no significant difference between BBR and glipizide groups in blood glucose profiles. In addition, the combination therapy of BBR and oral hypoglycemic agents had the advantages over oral hypoglycemic agents alone. No serious adverse effects of BBR have been reported. Conclusion BBR may have the beneficial effects in the control of blood glucose levels, though the efficacy of BBR is not superior to MET. BBR appeares to have advantages over rosiglitazone in improving FBG levels. In addition, the combination therapy of BBR and oral hypoglycemic agents may be a new attempt. However, the efficacy of BBR in patients with T2DM should be further evaluated by more RCTs in a larger population of patients.

9 A New Sesquiterpenoid Glycoside from Rhizomes of Atractylodes lancea

Min Yin

2015, 7(4).

[Abstract](663) [HTML](0) [PDF 0.00 Byte](3)

Abstract:
Objective To study the water-soluble chemical constituents rhizomes of from Atratylodes lancea. Methods Two sesquiterpenoid glycosides were purified by column chromatography and their structures were determined by spectroscopic analysis. They were also evaluated for anti-inflammatory activity by determining the inhibitory activity on LPS-induced NO and PGE2 generation in RAW 264.7 cell lines. Results Compound 1 was a new sesquiterpenoid glycoside, named as (1S,4S,5R,7R,10S)-4,11,14-trihydroxy- guai-3-one-11-O-β-D-glucopyranoside, but exhibited no appreciable activity. Compound 2 was atractyloside A and showed weak activity. Conclusion The hydroxy methyl group at C-10 of guaiol-type glycoside could be important for anti- inflammatory activity.

10 Chemical Constituents from Hypericum beanii

Da-song Yang

2015, 7(4).

[Abstract](655) [HTML](0) [PDF 0.00 Byte](9)

Abstract:
Objective To study the chemical constituents from the aerial parts of Hypericum beanii. Methods Various chromatographic techniques were used to separate the constituents and their structures were elucidated on the basis of extensive spectroscopic interpretation. Results Fifteen compounds were isolated from the aerial parts of H. beanii. Their structures were identified as hyperbeanol E (1), (E )-linalool-1-oic acid (2), (4S,5R )-5-(4′-methyl-3′-pentenyl)-4-hydroxy-5-methyl- dihydrofuran-2-one (3), benzoic acid (4), 4-(3-O-3″)-3″-methylbutenyl-6-phenyl- pyran-2-one (5), 4-hydroxy-4a,7-dimethoxy-4,4a-dihydrodibenzo-p-dioxin-2(3H )- one (6), isoimperatorin (7), 2,3-dimethoxyxanthone (8), 3,4-dihydroxy-2- methoxyxanthone (9), osajaxanthone (10), nigrolineaxanthone F (11), hypercohone G (12), betulinic acid (13), oleanolic acid 3β-caffeate (14), and isoastilbin (15). Conclusion Compound 1 is a new menthane monoterpene derivative which owns an extra lactone ring. Compounds 2–7 and 10–15 are isolated from genus Hypericum Linn. for the first time and the other compounds are first obtained from the plants in H. beanii.

11 Effect of Chinese Medicine Naodesheng against Repeated Transient Global Cerebral Ischemia in Mice

Chun-hua Hao

2015, 7(4).

[Abstract](411) [HTML](0) [PDF 0.00 Byte](6)

Abstract:

12 Treatment of Kangxian Pills to Chronic Liver Injury in Mice Induced with Carbon Tetrachloride

Huan-tian Cui

2015, 7(4).

[Abstract](541) [HTML](0) [PDF 0.00 Byte](3)

Abstract:
Objective Kangxian Pills, containing Angelicae Sinensis, Chuanxiong Rhizoma, radix paeoniae rubra, and 12 other kinds of Chinese materia medica, have the functions of softening and dispersing blood stasis. It has been used for liver injury and liver fibrosis. The current study was designed to evaluate the anti-hepatic injury activity and the mechanism of Kangxian Pills on a CCl4-induced animal model. Methods To induce chronic liver injury, mice were treated with CCl4 twice a week for four weeks. Kangxian Pills (6 or 12 g/kg) and Compound Biejia Ruangan Tablet (0.901 g/kg) were ig given to mice once daily for four weeks after CCl4 was withdrawal. The anti-hepatic injury activities and mechanisms of Kangxian Pills were assessed by hepatic histology and by measuring the levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT), albumin (ALB), and total protein (TP) of serum as well as superoxide dismutase (SOD) and glycogen (Gn) of the liver. Results Kangxian Pills significantly decreased the levels of liver index, ALT, and AST in mice liver injury models in treatment group. Moreover, Kangxian Pills and Compound Biejia Ruangan Tablet inhibited the CCl4-induced reduction of SOD and Gn levels in the liver. The histological study showed that Kangxian Pills could reduce cellular swelling and infiltration of inflammatory cells in liver injury. Conclusion Kangxian Pills possess the potent abilities to alleviate chronic liver injury, suggesting that Kangxian Pills exert this effect by enhancing the anti-oxidant ability and metabolism of the liver.

13 Metabolism Study Builds the Bridge from Research to Development

Chang-xiao Liu

2015, 7(4):289-289. DOI: 10.1016/S1674-6384(15)60053-3

[Abstract](368) [HTML](0) [PDF 132.59 K](995)

Abstract:

14 HMGR, SQS, β-AS, and Cytochrome P450 Monooxygenase Genes in Glycyrrhiza uralensis

Rui Yang , Bo-chuan Yuan , Yong-sheng Ma , Li-qiang Wang , Chun-sheng Liu , Ying Liu

2015, 7(4):290-295. DOI: 10.1016/S1674-6384(15)60054-5

[Abstract](812) [HTML](0) [PDF 364.08 K](1267)

Abstract:
Glycyrrhiza uralensis is frequently used in traditional Chinese medicine. This plant contains a large amount of effective constituents, including triterpenoids and flavonoids. Among them, glycyrrhizin is believed to be the marker compound to evaluate the quality of G. uralensis based on Chinese Pharmacopoeia. Many studies showed that glycyrrhizin possesses various pharmacological activities, such as antibacterial, antiviral, antitumor, anti-inflammatory, and immune-stimulating activities. In this paper, we summarized the cloning, characterization, expression, and polymorphism analysis of several functional genes involved in glycyrrhizin biosynthesis in G. uralensis.

15 Identification of Icaritin Metabolites in Rats by LC-MS/MS

Lin-hu Ye , Bing-xin Xiao , Fang-rui Cao , Ying Zheng , Rui-le Pan , Qi Chang

2015, 7(4):296-302. DOI: 10.1016/S1674-6384(15)60055-7

[Abstract](901) [HTML](0) [PDF 425.71 K](1445)

Abstract:
Objective Icaritin is the main aglycone and also active intestinal metabolite of prenylflavonoids from the Chinese materia medica Epimedii Herba. Modern pharmacological studies have demonstrated that icaritin has a wide range of biological activities. However, its metabolites and biotransformation pathways have not yet been comprehensively investigated. The present study aims to identify icaritin metabolites in rats by using a sensitive and effective LC-MS/MS method. Methods The plasma and urine samples of rats were collected before(blank) and after oral administration of icaritin, and subjected to liquid-liquid extraction with ethyl acetate. The full-scan LC-MS chromatograms of the plasma and urine samples were compared with those of blank samples to detect the possible metabolites, which were later detected by their product ion spectra. Results A total of 23 metabolites were identified, and conjugated icaritins produced by glucuronidation, glycosylation, and sulfation were its major metabolites. Minor demethylation, hydrogenation, and oxidation metabolites were also found. Conclusion Phase II metabolism is the main metabolic pathway of icaritin.

16 Protection of Salidroside on Primary Astrocytes from Cell Death by Attenuating Oxidative Stress

Cun-hua Zhao , Zhi-hui Zhu , Ye-ling Wang , Georg Reiser , Li Tang

2015, 7(4):303-309. DOI: 10.1016/S1674-6384(15)60056-9

[Abstract](444) [HTML](0) [PDF 327.20 K](1273)

Abstract:
Objective To investigate whether salidroside(SAL) has protective and anti-oxidative effects on astrocytes. Methods Firstly, SAL was extracted from the roots of Rhodiola rosea with 70% ethanol and butanol to obtain crude phenylethyl alcohol glycosides which have been known as bioactive part of R. rosea; Secondly, WST-1 assay was carried out to assess the cell viability of astrocytes and cortical neurons under the treatment of the purified(>95%) SAL. Moreover, WST-1 assay was also used to evaluate the cytoprotective effects of SAL preventing astrocytes from staurosporine-induced cell death; Thirdly, we examined the spontaneous reactive oxygen species(ROS) and staurosporine-induced ROS generation in astrocytes in the absence or presence of SAL. Results SAL was observed to improve the astrocytes viability but not cortical neurons. In addition, SAL was able to ameliorate staurosporine-induced cell death. Moreover, SAL was able to attenuate the spontaneous ROS and staurosporine-induced ROS generation. Conclusion We here confirm that the anti-oxidative effect of SAL on primary astrocytes might be an important mechanism accounting for the cytoprotective effects from SAL.

17 Hypoglycemic and Hypolipidemic Effects of Lycium barbarum Polysaccharide in Diabetic Rats

Rong Zhao , Rui Jin , Yong Chen , Feng-mei Han

2015, 7(4):310-315. DOI: 10.1016/S1674-6384(15)60057-0

[Abstract](428) [HTML](0) [PDF 364.97 K](1190)

Abstract:
Objective To study the antidiabetic effects and the underlying molecular mechanisms of Lycium barbarum polysaccharide(LBP) and its DEAE cellulose elution fraction LBP-IV in diabetic rats induced by high fat diet(HFD) and streptozotocin(STZ). Methods After ig administration of LBP-IV[50, 100, and 200 mg/(kg·d)] and LBP[100 mg/(kg·d)] once daily for consecutive 4 weeks to diabetic rats, the glucose and lipids in blood, mRNA expression of phosphoenolpyruvate carboxykinase(PEPCK), sterol regulatory element binding-protein-1c(SREBP-1c), and fatty acid synthase(FAS) in liver were determined. Results Ig administration of LBP and LBP-IV significantly decreased the levels of blood glucose, HbA1c, TC, TG, and LDL-C, as well as the hepatic mRNA expression of PEPCK, SREBP-1c, and FAS, whereas significantly increased the oral glucose tolerance of diabetic rats. Conclusion The findings suggest that the antidiabetic effects of LBP and LBP-IV are associated with the decreased hepatic mRNA expression of PEPCK, SREBP-1c, and FAS in HFD-STZ induced diabetic rats.

18 Pharmacokinetics of Tetramethylpyrazine Hydrochloride in Rabbits Blood after Intranasal Administration

Jin-fan Yan , Feng Han , Li Ma , Yan-jing Cheng , Jing Gao , Jin-li Deng , Xia Feng

2015, 7(4):316-322. DOI: 10.1016/S1674-6384(15)60058-2

[Abstract](456) [HTML](0) [PDF 302.25 K](1147)

Abstract:
Objective To study the pharmacokinetic behavior of tetramethylpyrazine hydrochloride(TMPH) in plasma of rabbits after intranasal administration and the relationship between absorption and dosage, furthermore, to illustrate the effects of borneol and musk used in combination with TMPH on the plasma concentration profile of TMPH in rabbits. Methods The concentration of TMPH was determined by RP-HPLC method. Coumarin was used as an internal standard. Sample preparation was carried out by extraction and precipitation with methanol. The pharmacokinetic parameters were computed by software program DAS.3.1.4. Results Blood pharmacokinetics of TMPH fitted best to a non-compartment model. After intranasal administration with single dose at 10, 20, and 40 mg/kg of TMPH, the average values of C_max were 8.075, 16.537, and 33.115μg/mL, and the average values of AUC0-t were 228.93, 399.273, and 728.917 mg/(L·min), respectively. C_max of TMPH in plasma was increased by 31.136% and 38.786% compared with those without borneol and musk, and intranasal bioavailability were increased by 21.587% and 40.633% after intranasal administration of TMPH in combination with borneol, or with borneol and musk. Conclusion Borneol and musk could enhance the intranasal absorption of TMPH and increase the concentration of TMPH in blood of rabbits, especially in the early period. This work also shows the rational compatibility between borneol and musk.

19 Antipyretic Effects of Eupatorium chinense and Its Mechanism

Yi-ping Jiang , Jiang-ping Xu

2015, 7(4):323-327. DOI: 10.1016/S1674-6384(15)60059-4

[Abstract](399) [HTML](0) [PDF 270.27 K](1873)

Abstract:
Objective To investigate the antipyretic effect of Eupatorium chinense and its mechanism. Methods The content of arginine vasopressin(AVP) in ventral septal area(VSA) and blood plasma, and cyclic adenosine monophosphate(cAMP) levels of hypothalamus and blood plasma were determined by enzyme linked immunosorbent assay. Results The body temperature(Tb) was decreased at 1 h after administration of E. chinense(3 and 6 g/kg) and Aspirin(0.3 g/kg) respectively, which was significantly different from the temperature of fever model group. The antipyretic effect of Aspirin and E. chinense lasted for longer time. Aspirin(0.3 g/kg) and E. chinense(3 and 6 g/kg) reduced the level of cAMP in hypothalamus of fever rats and increased AVP content in plasma. The changes in cAMP content in plasma of all drug treatment groups were not obvious. Conclusion E. chinense has strong antipyretic effect and may affect the production of AVP and cAMP in fever rats.

20 Investigation of Mechanism of Premature Ovarian Failure Regulation by Kidney-tonifying Herbs and Liver-clearing Herbs in Dingjing Decoction

Xiu-feng Wang , Lei Zhang , Qing-hua Wu , Jian-xin Min , Na Ma , Lai-cheng Luo

2015, 7(4):328-333. DOI: 10.1016/S1674-6384(15)60060-0

[Abstract](507) [HTML](0) [PDF 286.32 K](1279)

Abstract:
Objective To investigate the mechanisms through which kidney-tonifying herbs(KTHs) and liver-clearing herbs(LCHs) in Dingjing Decoction(DJD) regulate premature ovarian failure(POF). Methods One hundred and fifty Sprague-Dawley rats were randomly divided into five groups such as control, model, KTHs, LCHs, and DJD groups. POF-related biological molecules were examined. Factor analysis was performed to investigate the regulatory networks and key biomolecules involved in mediating POF after treatment with KTHs and LCHs. Results The master regulatory factors in the reproductive endocrine network associated with KTHs intervention included four molecules in the pituitary-ovarian axis, cortisol(CORT) in the target gland of pituitary-adrenal axis, and some molecules in the hypothalamus. In contrast, the master regulatory factors associated with LCHs intervention included four molecules in the pituitary-ovarian axis and some molecules in the hypothalamus; No biomolecules in the pituitary-adrenal axis were involved in the LCH-mediated mechanisms. Gonadotropin-releasing hormone(GnRH), which was identified as a common biological molecule in the hypothalamus, was involved in regulating the reproductive endocrine network in association with KTHs intervention. Conclusion KTHs directly regulates biological molecules in the pituitary-adrenal axis and indirectly regulates those in the pituitary-adrenal axis through the hypothalamus, while the LCHs only exert its effects indirectly. GnRH is the key biological molecule associated with KTHs intervention.

21 Treatment of Kangxian Pills to Chronic Liver Injury in Mice Induced with Carbon Tetrachloride

Huan-tian Cui , Li Wang , Yu-hong Bian , Pei-dong Liu , Hui-fang Zhou , Zan-hong Pan

2015, 7(4):334-338. DOI: 10.1016/S1674-6384(15)60061-2

[Abstract](462) [HTML](0) [PDF 322.61 K](1161)

Abstract:
Objective Kangxian Pills, containing Angelicae Sinensis, Chuanxiong Rhizoma, radix paeoniae rubra, and 12 other kinds of Chinese materia medica, have the functions of softening and dispersing blood stasis. It has been used for liver injury and liver fibrosis. The current study was designed to evaluate the anti-hepatic injury activity and the mechanism of Kangxian Pills on a CCl₄-induced animal model. Methods To induce chronic liver injury, mice were treated with CCl₄ twice a week for four weeks. Kangxian Pills(6 or 12 g/kg) and Compound Biejia Ruangan Tablet(0.901 g/kg) were ig given to mice once daily for four weeks after CCl₄ was withdrawal. The anti-hepatic injury activities and mechanisms of Kangxian Pills were assessed by hepatic histology and by measuring the levels of aspartate aminotransferase(AST), alanine aminotransferase(ALT), albumin(ALB), and total protein(TP) of serum as well as superoxide dismutase(SOD) and glycogen(Gn) of the liver. Results Kangxian Pills significantly decreased the levels of liver index, ALT, and AST in mice liver injury models in treatment group. Moreover, Kangxian Pills and Compound Biejia Ruangan Tablet inhibited the CCl₄-induced reduction of SOD and Gn levels in the liver. The histological study showed that Kangxian Pills could reduce cellular swelling and infiltration of inflammatory cells in liver injury. Conclusion Kangxian Pills possess the potent abilities to alleviate chronic liver injury, suggesting that Kangxian Pills exert this effect by enhancing the anti-oxidant ability and metabolism of the liver.

22 Effect of Chinese Patent Medicine Naodesheng against Repeated Transient Global Cerebral Ischemia in Mice

Chun-hua Hao , Wen-gong Xi , Hai-juan Zheng , Wei-ting Wang , Zhuan-you Zhao

2015, 7(4):339-343. DOI: 10.1016/S1674-6384(15)60062-4

[Abstract](449) [HTML](0) [PDF 312.77 K](1369)

Abstract:
Objective To investigate the therapeutic effect and possible mechanisms of Chinese ptent medicine Naodesheng(NDS) on repeated transient global cerebral ischemia(GCI) in mice. Methods The repeated transient GCI mice were induced by bilateral carotid arteries ligation, and were randomly divided into model group, Sham group without arteries ligation, NDS groups(1.25 and 2.5 g/kg) and positive control(vinpocetine 3.1 mg/kg, VP) group. After oral administration once daily for successive 7 d, the transient GCI was induced. The degree of neurological deficit, histological changes, and neurons loss in the hippocampus were evaluated. In order to investigate the possible mechanisms, the oxidative stress and inflammatory factor were measured after 24 h of GCI. Comparison among multiple groups was performed with one-way analysis of variance(ANOVA). Results NDS could significantly alleviate the neurological function impairment, histological injury, and neurons loss, increase the superoxide dismutase(SOD) activity, decrease the content of malondialdehyde(MDA), and reduce inflammatory factor in the ischemic brain tissue. Conclusion NDS could significantly reduce brain injury induced by global ischemia, and its mechanism is closely associated with anti-oxidation and anti-inflammation.

23 Efficacy and Safety of Berberine in Patients with Type 2 Diabetes Mellitus:A Meta-Analysis

Xiao-chen Wei , Li-qin Zhu , Chun-ge Wang

2015, 7(4):344-353. DOI: 10.1016/S1674-6384(15)60063-6

[Abstract](431) [HTML](0) [PDF 671.74 K](1265)

Abstract:
Objective To assess the efficacy and safety of berberine(BBR) in patients with type 2 diabetes mellitus(T2DM) by performing a systematic review. Methods PubMed, Cochrane Library, Embase, CNKI, and CBM were searched until May 2014. The randomized controlled trials(RCTs) of the effects of BBR on blood glucose in patients with T2DM were included. The quality of RCTs was assessed by the Jadad scale, and the Review Manager 5.1 software was used for data syntheses and analyses. Results Seventeen RCTs involving 1198 patients were included. The methodological quality of these RCTs was generally low. Compared with the control groups(placebo or no intervention with medicine), BBR suggested the statistically significant benefits in improving fasting blood glucose(FBG), postprandial blood glucose(PBG), glycosylated hemoglobin, and homeostasis model assessment of insulin resistance. Subgroups analysis of BBR compared with metformin(MET) showed that 1.5g/d MET was significantly better than BBR(0.9-1.5 g/d) in lowering FBG and PBG. However, there was no significant difference between 1.5g/d BBR and 0.75g/d MET groups in blood glucose profiles. In comparison with rosiglitazone, BBR suggested the statistically significant benefits in lowering FBG. And there was no significant difference between BBR and glipizide groups in blood glucose profiles. In addition, the combination therapy of BBR and oral hypoglycemic agents had the advantages over oral hypoglycemic agents alone. No serious adverse effects of BBR have been reported. Conclusion BBR may have the beneficial effects in the control of blood glucose levels, though the efficacy of BBR is not superior to MET. BBR appeares to have advantages over rosiglitazone in improving FBG levels. In addition, the combination therapy of BBR and oral hypoglycemic agents may be a new attempt. However, the efficacy of BBR in patients with T2DM should be further evaluated by more RCTs in a larger population of patients.

24 Comparison on Traditional and Machinery Decoctions for Da-cheng-qi Decoction Based on Chemical Ingredients, Pharmacological Functions, and Clinical Trials

Rui-fang Xie , Yi-min Li , Zhi-cheng Li , Zhi-na Shi , Pei-pei Chen , Song-hua He , Hua-feng Wei , Yan-hong Wang , Ying-hao Zhou , You-hua Wang , Xin Zhou

2015, 7(4):354-364. DOI: 10.1016/S1674-6384(15)60064-8

[Abstract](387) [HTML](0) [PDF 381.37 K](1257)

Abstract:
Objective Patients and doctors often have questions about the equivalence of traditional and machinery decoctions. In this article, using Da-cheng-qi Decoction(DCQD) as a model of formula, traditional decoction(TD), machinery decoction under high pressure(MDHP), and machinery decoction under normal pressure(MDNP) were compared. Methods For chemical components, HPLC fingerprints were established and evaluated using AHP combined with CRITIC weighing method; For animals' effects, the experiments of small intestinal propulsion were conducted; For clinical effects, a randomized clinical trial(RCT) was designed and performed. Results Although there were some differences between TD and MDNP in chemical ingredients, there was no significant difference in animal experiments and clinical trials(P>0.05). Conclusion The traditional and machinery decoctions of DCQD could be used bioequivalently.

25 Simultaneous Determination of Four Substances in Plasma and Dermal Microdialysates of Guinea Pig after Different Acupoints Administration of Fufang Baijiezi Gel

Guo-hua Wang , Bao-xian Zhang , Qi-xia Nie , Chen Zang , Qiong Zhu

2015, 7(4):365-370. DOI: 10.1016/S1674-6384(15)60065-X

[Abstract](367) [HTML](0) [PDF 545.42 K](1038)

Abstract:
Objective To study the pharmacokinetic properties of Fufang Baijiezi Gel(FBG) after different acupoints administration. Methods Sinapine thiocyanate, tetrahydro-palmatine, 6-gingerol, and asarinin, which were four substances of FBG, were determined by a sensitive liquid chromatography tandem mass spectrometry method(LC-MS) both in plasma and dermal microdialysates of guinea pig simultaneously. Microdialysates were separated on an Ultimate® XB-Phenyl analytical column(150 mm×2.1 mm, 5μm) and detected by electrospray ionization(ESI) in selected ion monitoring(SIM) mode. The method was validated in terms of selectivity, linearity, sensitivity, and recovery. Result A significant difference was observed in main pharmacokinetic parameters of C_max, t_max, and AUC between acupoints administration and nonacupoints administration. Conclusion Acupoints administration resulted in a more obvious increase in bioavailability of sinapine thiocyanate, tetrahydropalmatine, 6-gingerol, and asarinin than nonacupoints administration.

26 A New Sesquiterpenoid Glycoside from Rhizomes of Atractylodes lancea

Min Yin , Chao-cheng Xiao , Yu Chen , Ming Wang , Fu-qin Guan , Qi-zhi Wang , Yu Shan , Xu Feng

2015, 7(4):371-374. DOI: 10.1016/S1674-6384(15)60066-1

[Abstract](406) [HTML](0) [PDF 388.97 K](1100)

Abstract:
Objective To study the water-soluble chemical constituents from the rhizomes of Atractylodes lancea. Methods Two sesquiterpenoid glycosides were purified by column chromatography and their structures were determined by spectroscopic analysis. They were also evaluated for anti-inflammatory activity by determining the inhibitory activity on LPS-induced NO and PGE₂ generation in RAW 264.7 cell lines. Results Compound 1 was a new sesquiterpenoid glycoside, named as(1S,4S,5R,7R,10S)-4,11,14-trihydroxy-guai-3-one-11-O-β-D-glucopyranoside, but exhibited no appreciable activity. Compound 2 was atractyloside A and showed weak activity. Conclusion The hydroxyl group at C-10 of guaiol-type glycoside could be important for anti-inflammatory activity.

27 Chemical Constituents from Hypericum beanii

Da-song Yang , Zi-lei Li , Yong-ping Yang , Xiao-li Li , Wei-lie Xiao

2015, 7(4):375-379. DOI: 10.1016/S1674-6384(15)60067-3

[Abstract](484) [HTML](0) [PDF 399.39 K](1304)

Abstract:
Objective To study the chemical constituents from the aerial parts of Hypericum beanii. Methods Various chromatographic techniques were used to separate the constituents and their structures were elucidated on the basis of extensive spectroscopic interpretation. Results Fifteen compounds were isolated from the aerial parts of H. beanii. Their structures were identified as hyperbeanol E(1),(E)-linalool-1-oic acid(2),(4S,5R)-5-(4'-methyl-3'-pentenyl)-4-hydroxy-5-methyl-dihydrofuran-2-one(3), benzoic acid(4), 4-(3-O-3")-3"-methylbutenyl-6-phenyl-pyran-2-one(5), 4-hydroxy-4a,7-dimethoxy-4,4a-dihydrodibenzo-p-dioxin-2(3H)-one(6), isoimperatorin(7), 2,3-dimethoxyxanthone(8), 3,4-dihydroxy-2-methoxyxanthone(9), osajaxanthone(10), nigrolineaxanthone F(11), hypercohone G(12), betulinic acid(13), oleanolic acid 3β-caffeate(14), and isoastilbin(15). Conclusion Compound 1 is a new menthane monoterpene derivative which owns an extra lactone ring. Compounds 2-7 and 10-15 are isolated from genus Hypericum Linn. for the first time and the other compounds are first obtained from the plants in H. beanii.

Volume 7,Issue 4,2015 Table of Contents

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