ABSTRACT
The aim of the present work was to investigate permeability characteristics of an anticancer berberine chloride, inpresence and absence of bioenhancer quercetin on goat intestine using Franz diffusion cell. A 32 full factorial designapproach was employed to investigate the effect of independent variables such as the concentration of bioenhancer(X1) and pretreatment time (X2) on dependent variable % cumulative drug release (% CDR) (Y) using design expertsoftware. The effect of quercetin was examined at three different levels of pretreatment time (30, 45, and 60 minutes)and at three different concentrations (2, 6, and 10 mg) on goat intestine. The apparent permeability (Papp), flux (J), andenhancement ratio (ER) were determined. Further, in vitro anticancer activity of optimized batch was performed onvarious cancer cell lines K562, A459, and Hela. During pretreatment studies, it was observed that an increase in theconcentration of quercetin yielded a positive effect on % CDR while the increase in pretreatment time by quercetinhad a detrimental effect on % CDR. When goat intestine was pre-treated for 30 minutes with 10 mg of quercetin,90.91% ± 1.66% CDR was obtained while the minimum value of 17.45% ± 2.12% CDR was observed at 2 mgquercetin pre-treated for 60 minutes. In vitro anticancer activity of optimized batch demonstrated non-significanteffect as compared with parent drug. In conclusion, quercetin could be successfully utilized as bioenhancer to improveex vivo permeability of berberine chloride, which would be expected to improve its bioavailability and reduce the doseresulting in improved patient compliance.
ABSTRACT
The aim of this study was to analyze compounds from the methanolic extract of fruits of Helicteres isora for antidiabetic activity. Sanguinarine, berberine chloride (BC) and muscimol were found to be as major compounds in the methanolic fruits extract of H. isora. BC was isolated from the methanolic fruit extract of H. isora by using HPLC and other compounds were commercially acquired. Diabetes was induced in rats by a single dose of intraperitonial injection of streptozotocin (STZ). Sanguinarine (50 mg/kg b.w), BC (50 mg/kg b.w) and muscimol (50 mg/kg b.w) were evaluated by Oral Glucose Tolerance Test (OGTT) in normal and STZ induced diabetic rats. Among the three compounds, BC significantly reduced the blood glucose levels when compared to sanguinarine and muscimol. The OGTT study clearly indicates, BC possess promising antidiabetic activity against STZ induced diabetic rats.
ABSTRACT
Objective To examine neuroinflammation,oxidative damage and neuron loss in the contralateral parie-tal lobecortex of TBI model mice, and to investigate effects of berberine chloride on such secondary damage.Methods TBI model was established by a weight-drop hitting device and mice in berberine group were administered intragastrically with berberine chloride (50mg/kg.day) for 21 days.Immunofluorescence staining was used to assess activity of microglia and astrocyte.Immunohistochemistry was used to assess DNA oxidative damage, neuron loss and expression of COX-2 and iN-OS.Results Activation of microglia and astrocyte, expressions of COX-2 and iNOS and DNA oxidative damage were ob-viously increased by TBI,(19.82 ±1.88)and(16.96 ±1.69)、(13.79 ±4.32)and(8.67 ±0.96)、(27.86 ±5.38) and (16.00 ±7.59)、(31.92 ±6.57)and(24.79 ±2.78)respectively (P0.05). Conclusions TBI can cause neuroinflammation and oxidative damage but not neuron loss in the contralateral parietal lobe cortex.Berberine chloride can significantly suppress neuroinflammtion in the contralateral parietal lobe cortex after TBI.
ABSTRACT
Objective To determinate Berberine chloride in compound Wuzhigan capsules and develop a steady and reliable method for the quality control of the capsules.Methods A HPLC method was adopted.The column was Diamonsil C18 (250 mm?4.6 mm,5 ?m) with the column temperature of 30 ℃,the mobile phase was acetonitrile-0.033 mol/L potassium dihydrogen phosphate (30∶70) with the flow rate of 1.0 mL/min,and the detection wavelength was at 347 nm.Results Berberine chloride has a linearity in the range of 2.52～12.6 ?g/mL,and the average content in the capsules was 1.686 mg/capsules.Conclusion This method is sample,accurate,and can be used for the quality control of compound Wuzhigan capsules.
ABSTRACT
Study on some methods used to quantify berberine chloride showed that the UV measuring and volumetric titration methods did not express only amount of berberine chloride itself. It is necessary to apply high- performance liquid chromatography (HPLC) to achieve the optimal conditions for better splitting, higher accuracy…in order to apply more widely in testing products commonly in market with many components combined to berberine chloride. To find out optimal methods, which are suitable with condition of present some pharmaceutical units, it is necessary to experiment continuously methods such as UV measuring and volumetric titration,… using HPLC method to compare.
Subject(s)
Berberine , TabletsABSTRACT
Objective To determine the berberine chloride content in Lianpu Shuangqing Tablet and to develop a steady and reliable method for the quality control of the tablet.Method A HPLC method was adopted.The column was Dionex C18 (5 ?m,4.6 mm ?150 mm)with the column temperature of 28 ℃,the mobile phase was acetonitrile-0.033 mol/L potassium dihydrogen phosphate(25 ∶75) with the flow rate of 1.0 mL/min,and the detection wavelength was at 346 nm.Results Berberine chloride has a linearity in the range of 0.153～1.224 ?g,and the average content in the tablet was 1.26 mg/tablet.Conclusion This method is simple,accurate,and can be used for the quality control of Lianpu Shuangqing Tablet.
ABSTRACT
AIM To study the effects of coadministration of berberine chloride(Ber) with cyclosporin (CsA) on liver microsomal cytochrome P450 isoenzyme and multi drug resistance gene in rats. METHODS The activities of liver microsomal erythromycin demethylase(ERD) and aminopyrence N demethylase(ADM) were determined. The levels of mRNA expression of CYP3A1, CYP1A1, CYP2E1, mdr1a and mdr1b were assayed with RT PCR. RESULTS After administration for 6 days, all treatment groups except Ber at 100 mg?kg -1 exhibited inhibitory action on ERD activity in rats. ERD activity markedly decreased in all drug treatment groups after taking drug for 12 days. After administration for 6 days, 45 mg?kg -1 CsA, 100 mg?kg -1 Ber coadministrated with 45 mg?kg -1 CsA and 200 mg?kg -1 Ber plus 45 mg?kg -1 CsA had significant inhibitory effects on ADM activity in rats. All groups except 100 mg?kg -1 Ber and 150 mg?kg -1 ketoconazole had the same effects on ADM activity after treatment for 12 days. Again, after 12 days, all drug treatment groups except 100 mg?kg -1 Ber group was found of remarkable inhibition of the mRNA expression of CYP3A1, CYP2E1, mdr1a and mdr1b. The CYP1A1 gene was not detected in all groups. CONCLUSION The mechanism of Ber to increase CsA concentration is that Ber decreases the expression of CYP3A, mdr1a and mdr1b thereby reduces the metabolism and elimination of CsA by liver.