OBJECTIVETo analyze the efficacy and safety of bicyclol combined with thymosin in treatment of chronic viral hepatitis B (CHB).

METHODSA total of 135 patients with CHB were randomized into experimental group and control group. The patients in the experimental group received bicyclol orally 75 mg daily and thymosin 20 mg intramuscular injection once every 2 days for 24 weeks and those in control group received bicyclol orally 75 mg daily alone for 24 weeks. The levels of serum aminotransferase (ALT/AST), HBV-DNA, HBeAg /antiHBe were observed.

RESULTSCompared with pre-treatment levels, the serum aminotransferase levels decreased significantly in both groups, but there were no statistically significant differences between them. HBeAg negative conversion rate was significantly higher in the experimental group than in the control group (35.3 percent vs.19.4 percent, P less than 0.05). HBV DNA negative conversion rate was significantly higher in the experimental group than in the control group (36.7 percent vs. 20.9 percent, P less than 0.05). No obvious adverse events which were probably related to the drugs were observed in this study.

CONCLUSIONThe combination of bicyclol with thymosin had better effect in treatment of chronic hepatitis B ias compared with bicyvlol alone.

Adolescent ; Adult ; Biphenyl Compounds ; administration & dosage ; adverse effects ; Drug Therapy, Combination ; Female ; Hepatitis B, Chronic ; drug therapy ; Humans ; Male ; Middle Aged ; Thymosin ; administration & dosage ; adverse effects

OBJECTIVETo evaluate the efficacy and safety of bicyclol for chronic hepatitis B.

METHODThe authors searched CBMDisk, CJFD (2000-2006), CJD-CD, PubMed (1966-2006) for randomized controlled trials (RCT) comparing bicyclol versus non-antiviral interventions, interferon alpha (IFN-a) and lamivudine for treatment of chronic hepatitis B. Two reviewers performed data extraction and quality assessment independently and discussed when there was different opinion. We analyzed the data with RevMan 4.2 software supplied by Cochrane Collabration.

RESULTSFourteen RCTs involving 1782 patients were included. ALT recovery rate of bicyclol group was 69.3 percent while that of the control group was 59.0 percent, the difference was statistical significant [RR 1.24, 95 percent CI (1.01, 1.52), P=0.04]. Loss of HBeAg in the bicyclol group (22.1 percent) was higher than that of the control group (13.5 percent) [RR 1.65, 95 percent CI (1.32, 2.06), P<0.00001]. No serious adverse events were reported.

CONCLUSIONBicyclol might be beneficial to recovery of liver function and loss of serum HBV marker. However, more high quality clinical trials are needed for confirmation.

Antiviral Agents ; administration & dosage ; adverse effects ; Biphenyl Compounds ; administration & dosage ; adverse effects ; Hepatitis B virus ; drug effects ; Hepatitis B, Chronic ; drug therapy ; Humans ; Randomized Controlled Trials as Topic

OBJECTIVETo develop a UPLC method for the simultaneous determination of liquiritin, narirutin, hesperidin, ammonium glycyrrhetate, honokiol and magnolol in Huoxiang Zhengqi oral liquid.

METHODA Zorbax Eclipse C18 column was used with the mobile phase of acetonitrile and 0. 05% phosphate acid by gradient elution at the detection wavelength of 220 nm. The flow rate was 0.42 mL x min(-1) and the column temperature was 30 degrees C.

RESULTThe calibration curves were linear in the ranges of 0.001 7-0.034, 0.003 4-0.068, 0.006 4-0.128, 0.012 8-0.256, 0.003 2-0.064, 0.006 4-0.128 microg, respectively. The average recoveries were 103.3%, 98.39%, 98.29%, 102.1%, 98.45%, 102.2% with RSDs of 2.1%,1.0%, 0.50%, 2.3%, 0.9%, 2.0%, respectively.

CONCLUSIONThe UPLC method was simple, rapid and accurate, it could be used for quality control of Huoxiang Zhengqi oral liquid.

Administration, Oral ; Biphenyl Compounds ; chemistry ; Chromatography, High Pressure Liquid ; methods ; Disaccharides ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Flavanones ; chemistry ; Glucosides ; chemistry ; Hesperidin ; chemistry ; Lignans ; chemistry ; Pharmaceutical Solutions ; chemistry

OBJECTIVETo investigate the effect of prescription compatibility on the pharmacokinetics of components from Dachengqi Decoction (DCQD, ) in rats.

METHODSTwenty-four male rats were randomly and equally divided into the DCQD group, Dahuang (Radix et Rhizoma Rhei, Polygonaceae) group, Houpo (Magnolia officinalis Rehd., Magnoliaceae) group, and Zhishi (Fructus Aurantii Immaturus, Rutaceae) group. The blood samples were collected before dosing and subsequently at 10, 15, 20, 30, 45 min, 1, 2, 4, 8, and 12 h following gavage. The levels of aloe-emodin, rhein, emodin, chrysophanol, honokiol, magnolol, hesperidin, and naringin in rat serum were quantified using a liquid chromatography tandem mass spectrometry (LC-MS/MS) method for pharmacokinetic study.

RESULTSThe area under the curve (AUC), mean retention time (MRT), the peak concentration (C(max)) of aloe-emodin, rhein, emodin, and chrysophanol in the DCQD group were significantly different compared with the Dahuang group (P <0.05, respectively). The mean plasma concentration, C(max), and the absorption of Dahuang's component in the DCQD group were obviously lower at each time point than those in the Dahuang group, while the elimination process of Dahuang's component was obviously delayed (P <0.05). Half-lives of aloe-emodin, chrysophanol, and rhein were also extended in the DCQD group (P <0.05, respectively). In the DCQD group, the mean plasma concentration, AUC, C(max) and absorption of honokiol, and magnolol were significantly lower (P <0.01, respectively) at each time point than those in the Houpo group, while the drug distribution half-life time (T(1/2α)), the drug eliminated half-life time (T(1/2β)), MRT, and time of peak concentration (T(max)) were significantly delayed (P <0.05, respectively). Pharmacokinetic parameters of hesperidin and naringin in the Zhishi group were not significantly different as compared with the DCQD group (P >0.05, respectively), while the MRT of naringin was significantly longer.

CONCLUSIONSThe compatibility in Chinese medicine could affect the drug's pharmacokinetics in DCQD, which proves that the prescription compatibility principle of Chinese medicine formulations has its own pharmacokinetic basis.

Administration, Oral ; Animals ; Anthraquinones ; administration & dosage ; blood ; pharmacokinetics ; Biphenyl Compounds ; administration & dosage ; blood ; pharmacokinetics ; Drug Incompatibility ; Emodin ; administration & dosage ; blood ; pharmacokinetics ; Flavanones ; administration & dosage ; blood ; pharmacokinetics ; Hesperidin ; administration & dosage ; blood ; pharmacokinetics ; Lignans ; administration & dosage ; blood ; pharmacokinetics ; Male ; Plant Extracts ; administration & dosage ; blood ; chemistry ; pharmacokinetics ; Rats ; Rats, Sprague-Dawley

PURPOSE: Chemical lights, also called Luminous Sticks, consist of a solution of diphenyl oxalate (C14H10O4) and hydrogen peroxide (H2O2). Human tissue can be damaged when the mixed solution contacts the human body. The authors report a single case of chemical injury of keratoconjunctiva by exposure to chemical lights. CASE SUMMARY: A 47-year-old man's right eye accidentally contacted the fluorescent material when breaking a Luminous Stick 7 days before being referred to our clinic. He had pain in the right eye and experienced visual loss. The patient's best corrected visual acuity in the right eye was 20/50. An ulcerative lesion with edema at the inferior bulbar and palpebral conjunctiva and coneal epithelial defect was observed upon biomicroscopic examination. The patient was hospitalized and antibiotics, steroids, mydriatic and artificial tear eye drops were applied for treatment. After 9 days of treatment, the best corrected visual acuity of the patient recovered to 20/20, and the conjunctiva and cornea were mostly healed. No complication was observed. CONCLUSIONS: Chemical lights are commonly used in concerts and festivals. If the contents contact the eyes when breaking he chemical lights, various chemical burns can occur and cause ophthalmologic complications. Since no regulations have been passed regarding chemical lights, safety education and supervision are considered to be necessary for children.
Anti-Bacterial Agents ; Biphenyl Compounds ; Burns, Chemical ; Child ; Conjunctiva ; Cornea ; Edema ; Eye ; Holidays ; Human Body ; Humans ; Hydrogen Peroxide ; Light ; Middle Aged ; Ophthalmic Solutions ; Organization and Administration ; Social Control, Formal ; Steroids ; Tears ; Ulcer ; Visual Acuity

BACKGROUNDCongestive heart failure (CHF) is a major cause of morbidity and mortality worldwide and angiotensin converting-enzyme inhibitor (ACEI) is the cornerstone in its treatment. However, CHF continues to progress despite this therapy, perhaps because of production of angiotensin II (Ang II) by alternative pathways. The present study was conducted to examine the combined effects of a chronic ACEI, ramipril, and a chronic Ang II type 1 receptor blocker, TCV116, on rat CHF after myocardial infarction (MI).

METHODSCongestive heart failure was caused by MI in rats, which was induced by ligating the left anterior descending coronary artery. The experiment protocol included sham-operated rats (Sham), MI-control rats (MI-control), MI rats treated with ramipril 3 mg/kg (MI-ramipril) or TCV116 2 mg/kg (MI-TCV116) per day, half dosage (MI-1/2R&T) or full dosage (MI-R&T) combination of the two. At 22 weeks, cardiac hemodynamic parameters such as mean arterial pressure (MAP), left ventricular systolic pressure (LVSP), maximal rate of left ventricule pressure development and decline (LV dP/dtmax) and left ventricular end diastolic pressure (LVEDP), and cardiac morphometric parameters such as heart weight (HW), left ventricular weight (LVW) and left ventricular cavity area (LVCA) were measured, mRNA expressions of cardiac molecule genes such as beta myosin heavy chain (betaMHC), B-type natriuretic peptide (BNP), transforming growth factor-beta1 (TGF-beta1), collagen I and III were quantified with reverse transcription polymerase chain reaction (RT-PCR) in the surviving septum myocardium, and survival rates were calculated.

RESULTSThere were no significant differences in MI sizes (%) among each MI related experimental groups (33 +/- 13, 34 +/- 14, 33 +/- 13, 35 +/- 13 and 33 +/- 14 for MI-control, MI-ramipril, MI-TCV116, MI-1/2R&T and MI-R&T, respectively, no statistical significance for all). Compared with sham-operated rats, MI rats without therapy showed significant increases in morphometric parameters as well as in mRNA expressions of cardiac molecule genes (P < 0.01); while their hemodynamic parameters were significantly impaired (P < 0.01), and in terms of spontaneous deaths survival rate shortened (P < 0.05). Compared with MI rats without therapy, MI rats treated with each single drug showed significant attenuation of mRNA expressions of cardiac molecule genes (P < 0.01); while their hemodynamic parameters were significantly improved (P < 0.05 or P < 0.01), and in terms of spontaneous deaths survival rate prolonged (P < 0.05). Both half and full dosage combined treatments exerted more powerful effects on improvement of cardiac phenotypic changes and on attenuation of betaMHC, BNP mRNA expressions (P < 0.05 vs monotherapy); while LVEDP was further lowered (P < 0.05 vs monotherapy). However, the total death in MI rats with full dosage combined treatment was more though there were no significant differences when compared with other treatments.

CONCLUSIONSThe results suggest that treatment with appropriate dosage combination of a chronic ACEI and a chronic ARB may further improve cardiac remodeling and cardiac function after MI.

Angiotensin-Converting Enzyme Inhibitors ; administration & dosage ; Animals ; Benzimidazoles ; administration & dosage ; Biphenyl Compounds ; administration & dosage ; Blood Pressure ; drug effects ; Drug Therapy, Combination ; Heart Failure ; drug therapy ; pathology ; physiopathology ; Male ; Myocardial Infarction ; complications ; Myocardium ; pathology ; Ramipril ; administration & dosage ; Rats ; Rats, Sprague-Dawley ; Receptor, Angiotensin, Type 1 ; drug effects ; Tetrazoles ; administration & dosage ; Ventricular Function, Left ; drug effects

OBJECTIVETo investigate the long-term effects of TCV116 (candesartan cilexetil) on cardiac function changes after myocardial infarction.

METHODSMyocardial infarction (MI) was induced by ligation of the left anterior descending coronary artery in rats. One week after the surgical performance,the surviving rats were randomly assigned to the following treatment groups: (1) MI rats with no therapy; (2) MI rats treated with TCV116 2 mg/kg per day; (3) Sham-operated control and (4) Sham-operated rats treated with TCV116 2 mg/kg per day. At 22 weeks, left ventricular function and cardiac histomorphometric parameters were measured, mRNA expression of cardiac genes such as beta myosin heavy chain, B-type natriuretic peptide, transforming growth factor beta1, collagen I and III quantified, and survival rates calculated.

RESULTSTreatment with TCV116 significantly improved LV function, suppressed mRNA expression of cardiac genes,and extended the survival period compared with MI rats with no therapy (P<0.05).

CONCLUSIONTreatment with long-term angiotensin II type 1 receptor blocker may improve LV function and prolong the survival of rats after MI.

Angiotensin II Type 2 Receptor Blockers ; Animals ; Benzimidazoles ; administration & dosage ; pharmacology ; Biphenyl Compounds ; administration & dosage ; pharmacology ; Heart Failure ; drug therapy ; etiology ; physiopathology ; Male ; Myocardial Infarction ; complications ; Myocardium ; metabolism ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Receptor, Angiotensin, Type 2 ; administration & dosage ; Tetrazoles ; administration & dosage ; pharmacology ; Ventricular Function, Left ; drug effects ; Ventricular Myosins ; metabolism ; Ventricular Remodeling ; drug effects

AIMTo observe effects of angiotensin (Ang) II receptor antagonist (AT1) irbesartan and angiotensin-converting enzyme (ACE) inhibitor perindopril on rat myocardium calcineurin expression and sarcoplasmic reticulum Ca(2+)-ATPase activity in the model of pressure-overload cardiac hypertrophy.

METHODSForty male adult Sprague Dawley rats were divided into 5 groups. One group was treated by sham operation; four groups were myocardium hypertrophy cases caused by banding aortic above renal artery. Drugs were given one week after operation. Group 1: sham group, rats (n=8) were gavaged with normal saline 2 ml/(kg.d) (ig); Group 2: control group, rats (n=8) were treated with normal saline 2 ml/(kg.d) (ig); Group 3: rats (n=8) were given perindopril 2 mg/(kg.d) (ig); Group 4: rats (n=8) were treated with irbesartan 20 mg/(kg.d) (ig); Group 5: rats (n=8) were given irbesartan 20 mg/(kg.d) plus perindopril 2 mg/(kg.d) (ig). Morphometric determination, calcineurin expression and sarcoplasmic reticulum Ca(2+)-ATPase activity were done at the end of 6 week of drug intervention. Expression of calcineurin in myocardium was detected by immunohistochemistry.

RESULTSLeft ventricular mass index (LVMI), transverse diameter of myocardial cell (TDM), calcineurin activity were remarkably decreased after drug intervention and this decrease was most remarkable in the combination drug therapy group. Sarcoplasmic reticulum Ca(2+)-ATPase activity was increased after drug intervention, especially in the combined drug therapy group. Calcineurin expression in myocardium was remarkably decreased after drug intervention. LVMI was positively correlated with TDM and calcineurin, negatively correlated with sarcoplasmic reticulum Ca(2+)-ATPase.

CONCLUSIONThese data suggest that irbesartan and perindopril inhibit cardiac hypertrophy through the increased activity of sarcoplasmic reticulum Ca(2+)-ATPase and decreased expression of calcineurin. Their combination had better effects on regressing of ventricular hypertrophy.

Animals ; Biphenyl Compounds ; administration & dosage ; Calcineurin ; metabolism ; Calcium-Transporting ATPases ; metabolism ; Cardiomegaly ; etiology ; metabolism ; Disease Models, Animal ; Drug Combinations ; Heart ; drug effects ; Hypertension ; complications ; metabolism ; Male ; Myocardium ; metabolism ; Myocytes, Cardiac ; drug effects ; metabolism ; Perindopril ; administration & dosage ; Pressure ; Rats ; Rats, Sprague-Dawley ; Sarcoplasmic Reticulum ; drug effects ; enzymology ; Tetrazoles ; administration & dosage

Honokiol is an active compound purified from magnolia that has been shown to induce cell differentiation, apoptosis, and anti-angiogenesis effects, as well as an enhancement in tumor growth delay in combination with chemotherapeutic agents in several mouse xenograft models. Our goal was to investigate the radiosensitization effect of honokiol on lung carcinoma. The radiosensitization effect of liposomal honokiol in Lewis lung carcinoma cells (LL/2) was analyzed using an in vitro clonogenic survival assay. For an in vivo study, Lewis lung carcinoma-bearing C57BL/6 mice were treated with either liposomal honokiol at 25 mg/kg or 5 Gy of single tumor radiation, or a combination of both over 12 days of treatment. The tumor growth delay and the survival time were evaluated. In addition, histological analysis of tumor sections was performed to examine changes by detecting the microvessel density and apoptosis in tumor tissues. In the clonogenic survival assay, LL/2 cells treated with IC50 Lipo-HNK for 24 h showed a radiation enhancement ratio of 1.9. After 12 days of combination treatment, the tumor volume decreased 78% and produced an anti-tumor activity 1.3-fold greater than a predicted additive effect of honokiol and radiation alone. This combination treatment also caused an 8.7 day delay in tumor growth. The cell cycle distribution and histological analysis demonstrated that liposomal honokiol has an anti-tumor effect via inducing apoptosis and inhibiting angiogenesis. Liposomal honokiol can enhance tumor cell radiosensitivity in vitro and in vivo, indicating that radiotherapy combined with liposomal honokiol can lead to greater anti-tumor efficacy.
Angiogenesis Inhibitors/administration & dosage/*therapeutic use ; Animals ; Apoptosis ; Biphenyl Compounds/administration & dosage/*therapeutic use ; Carcinoma, Lewis Lung/drug therapy/radiotherapy/*therapy ; Cell Cycle/drug effects/radiation effects ; Cell Line, Tumor ; Combined Modality Therapy ; Humans ; Lignans/administration & dosage/*therapeutic use ; Liposomes ; Lung Neoplasms/drug therapy/radiotherapy/*therapy ; Magnolia/chemistry ; Mice ; Neoplasm Transplantation ; Neovascularization, Pathologic/drug therapy/radiotherapy ; Radiation Tolerance ; Transplantation, Heterologous

The purpose of this study is to explore the feasibility and superiority of using rapid expansion of supercritical solution (RESS) technology in the field of traditional Chinese medicine. The extract of magnolia bark (EMB) was obtained by supercritical carbon dioxide (SCF-CO2) extraction technology. Microparticles of EMB were manufactured by RESS technology. The effects of operating temperature and pressure on the contents of the active ingredient in the particles were evaluated by HPLC. The effect of expansion conditions on the particle size distribution of EMB particles was investigated. The smallest sample (mean size: 4.7 microm) was obtained under the RESS condition: pressure of 25 MPa, temperature of 50 degrees C and a nozzle size of 100 microm. The characteristics of microparticles were also studied by differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and image analysis. The dissolution rate study showed that microparticles had a significantly faster dissolution rate than normal material particles. After oral raw EMB suspension, the mean areas under the plasma concentration-time curves (AUC(0-t)) of honokiol and magnolol were found to be (4.23 +/- 0.36) and (5.46 +/- 0.57) mg x h x L(-1), respectively, which were increased significantly, i.e. (5.41 +/- 0.63) and (7.24 +/- 0.83) mg x h x L(-1) when micronized EMB suspension was administered orally in SD rats (P < 0.05). Similarly, the mean maximum plasma concentrations of honokiol and magnolol increased from (1.55 +/- 0.22) and (2.35 +/- 0.14) mg x L(-1) (raw EMB) to (2.31 +/- 0.17) and (2.84 +/- 0.21) mg x L(-1) (micronized EMB), respectively. The results of t-test demonstrated that AUC(0-t) and Cmax value for honokiol and magnolol was significantly increased with the micronization compared to raw EBM (P < 0.05). This study demonstrated that the RESS was applicable for preparing microparticles of EMB at low operating temperature. The process was simple, free of environment pollution and without residual solvent.
Administration, Oral ; Animals ; Area Under Curve ; Biphenyl Compounds ; blood ; pharmacokinetics ; Drug Compounding ; methods ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; isolation & purification ; pharmacokinetics ; Lignans ; blood ; pharmacokinetics ; Magnolia ; chemistry ; Male ; Microspheres ; Particle Size ; Plant Bark ; chemistry ; Plants, Medicinal ; chemistry ; Rats ; Rats, Sprague-Dawley ; Solubility