ABSTRACT
Objective: To investigate the effect of berbamine hydrochloride on the absorption characteristics of berberine hydrochloride in different intestinal segments of rats in normal environment and high calcium environment. Method: Taking rat everted intestinal sac model,the content of berberine hydrochloride in absorbent solution of everted intestinal sac from different compatibility groups was determined by HPLC,and the uptake per unit area in different groups was analyzed by One-way ANOVA. Result: Compared with the normal J70 group(in normal environment,the concentration of berberine hydrochloride was 70 mg·L-1) at the same time point,the uptake per unit area of the normal J70+Ver100 group(in normal environment,the concentration of berberine hydrochloride was 70 mg·L-1,adding verapamil hydrochloride to a concentration of 100 mg·L-1) was significantly increased in the ileum(P-1,adding berbamine hydrochloride to a concentration of 35 mg·L-1) were significantly increased in the duodenum(P-1,adding berbamine hydrochloride to a concentration of 70 mg·L-1) were significantly increased in the ileum(PConclusion: Berbamine hydrochloride can promote the absorption of berberine hydrochloride in intestine to a certain extent,especially in the high calcium environment.
ABSTRACT
Objective To investigate whether berbamine (BBM) can induce FMS-like tyrosine kinase 3 (FLT3) acute myeloid leukemia cells apoptosis selectively and its possible mechanism. Methods The growth inhibitory activities of BBM were evaluated between acute myeloid leukemia cells with FLT3 mutant and other cell lines without FLT3 mutant by MTT assay. Apoptotic rate and cell cycle were analyzed by flow cytometry. The related proteins of FLT3 pathway and the apoptosis associated proteins expression were measured by Western blotting. Results The growth of MV4-11 with BBM was inhibited significantly in a dose and time dependent manner with IC50 (7.039 ± 0.700), (4.840 ± 0.271), and (2.088 ± 0.376) μmol/L at 24, 48, and 72 h, respectively. Meanwhile, the apoptotic rate was increased dose-dependently, cell cycle arrested in G0/G1 phase. Furthermore, phosphorylation of STAT5, which was the downstream signaling of FLT3, was significantly reduced by BBM in a dose-dependent manner. Conclusion BBM can induce apoptosis in MV4-11 cells by the inhibition of FLT3 and downstream P-STAT5 signal pathway.
ABSTRACT
Objective: To investigate the effect of berbamine (BBM) on the induction of apoptosis in human lung cancer cell A549 cells and the activity of TNF-α-JNK signaling pathway. Methods: After the A549 cells being treated with BBM at different concentration, the inhibitory effect of BBM on proliferation was detected by MTT assay. Cell morphological changes were detected by light microscope. Alteration of apoptosis rate of A549 cells was determined by Annexin V/PI double staining. Western blotting was used to detect the activity of apoptosis-related proteins, including Bcl-x, Caspase-3, and PAPR. The expressions of c-jun N-terminal kinase (JNK) and p-JNK were determined by Western blotting. Changes of tumor necrosis factor-alpha (TNF-α) were detected by fluorescent quantitative PCR and ELISA, respectively. Finally, the impacts of BBM on the proliferation and apoptosis of A549 cells were detected in the absence or presence of a JNK inhibitor. Results: BBM significantly inhibited the growth of A549 cells in a dose-dependent manner. The IC50 of 24 h was 9.01 μmol/L. Cells treated with BBM showed the typically morphological characteristics of apoptotic cells. Annexin V/PI double staining test indicated that BBM could induce the apoptosis of A549 cells in a dose-dependent manner. The early apoptotic population of cells treated with 10 μmol/L BBM was 13.8%, which was 5.6 times higher than that of the control. BBM decreased the expression of anti-apoptotic protein Bcl-x and increased the activity of proapoptotic proteins of caspase-3 and PARP. The mRNA and the protein expression levels of TNF-α were significantly increased by BBM treatment. The p-JNK expression was also dramatically up-regulated after BBM treatment. The effects of BBM on the proliferation and apoptosis in A549 cells were significantly reduced when JNK pathway was blocked. Conclusion: BBM could inhibit the growth and induce the apoptosis of A549 cells, and its mechanism may be related to the activated TNF-α-JNK signaling pathway.
ABSTRACT
Sankezhen (Berberidis Radix) is a traditional Chinese materia medica,cold in nature and bitter in taste,for treating syndromes of liver,stomach,and large intestinal meridians,in which berberine and berbamine are the major pharmacological components.Sankezhen has been readmitted in Chinese Pharmacopoeia 2010 following the 1977 version as the roots of Berberis spp.e.g.B.soulieana,B.wilsonae,B.poiretii,B.vernae,etc.Recent studies showed that Berberis spp.were potential phytomedicines with multiple spectrums therapeutic effects and various pharmaceutical parts.Here we reviewed Sankezhen in traditional use and phytochemistry,and its major active components berberine and berbamine with potential bioactivities recently discovered,such as antitumor,antidiabetic,antihyperlipidemic,anti-arrhythmic,and neuro-protective activities.It is necessary to mature the quality assessment of Sankezhen as a new admission of Chinese Pharmacopoeia 2010.Other parts of Berberis spp.should be investigated to better develop this herb in medicinal usage.
ABSTRACT
with flutamide has a syn-ergistic action in inhibiting the proliferation of LNCaP.
ABSTRACT
Objective To explore the efficacy of calmodulin antagonist berbamine(BBM) in down-regulating survivin mRNA. Methods Human breast cancer cell line MCF7 and its adriamycin-resistant counterpart MCF7/ADR were used in the study. The cells were cultured with different concentration of BBM for 72 hours. The mRNA expression level of survivin gene in both MCF and MCF7/ADR cells was detected by semi-quantitative RT-PCR. Results After treating MCF7 and MCF7/ADR cells by 20?mol/L BBM, the mRNA expression level of survivin gene decreased from 0.43?0.02 to 0.21?0.04 in MCF7 cells, and from 0.57?0.05 to 0.45?0.04 in MCF/ADR cells(P
ABSTRACT
AIM: To explore the effect of berbamine(BER) on apoptosis in K562 cells and its possible molecular mechanisms. METHODS: The apoptosis rate was measured by flow cytometry while electron microscopy and DNA electrophoresis were used to evaluate the characteristic changes of apoptosis, RT-PCR and Western blot were used to examine the expression levels of apoptosis related gene bcr/abl and BCR/ABL protein. RESULTS: By FCM, the apoptosis rate of K562 cells treated with 8.0 mg/L BER for 24 h and 72 h increased from (29.20?3.82)% to (61.77?4.35)% (P
ABSTRACT
The isolated working heart of guinea pig perfused with Tyrode's solution could work normally for at least 60 min. It was shown that berbamine ( BA ) could depress the function of isolated working heart of guinea pig in dose-dependent manner. BA 3 mol/L could decrease the left ventricular pressure, aortic pressure, -dP/dtmax, aortic blood flow and coronary blood flow, and increase left ventricular end-diastolic pressure. BA 100 mol/L could result in the ventricular asystole, however, no obvious influence the contraction of atrium.It was also demonstrated that BA could antagonise the arrhythmias induced by the adrenaline in isolated working heart of guinea Pig.
ABSTRACT
The cerebral infarction model was made according to Chen et al To evaluate the severity of infarction the quantity of Evan's blue was measured. The cerebral infarction size was determined by TTC stain. The results showed that ligating the right common carotid artery and the right middle cerebal artery and clamping the left common carotid artery could induce cerebral cortex in farction. Berbamine could decreased the level of Evan's blue and reduce the infarction size compared with control group. It suggests that berbamine possesses protective effect on experimental induced cerebral infarction.
ABSTRACT
AIM To investigate the effect of N methyl berbamine(NMB)on ATP sensitive potassium currents( I KATP )in single ventricular myocytes of guinea pig. METHODS Patch clamp technique with whole cell configuration. Holding potential was -40 mV, commanding potential was -100～+50 mV and duration was 600 ms. Pipette solution contained 0 3 mmol?L -1 ATP. RESULTS NMB inhibited I KATP in a concentration dependent manner. When holding potential was -40 mV and command potential was 0 mV, I KATP were reduced from (0 46?0 09) nA, (0 43?0 15) nA, and(0 47?0 10) nA to (0 37?0 07) nA( n=4,P
ABSTRACT
Berbamine ( Ber. ) is a bis-benzyl-isoquinoline alkaloid isolated from the traditional Chinese medical herb, Berberis poiretis, and has Vide pharmacological effects. Clinical studies have demonstrated that Ber. had an effect of ingreasing the number of leukocytes in various leukocytopenia. But, up till now it has not been reported that Ber. take effect on enzymic metablism of inner cell and isoenzyme in the process of increasing leukocyte. The experiment observed the mice dynamic change of LDH in leukocyte and LDH isoenzyme of serum by cytochemistry and plane polyacrylamide gel electrophoresis tech-nigue. The result indicates that LDH enzyme reaction of granulocyte have increased in Ber. group and intensity of enzyme reaction has a positive interralation with the time of administrations. All specimen show 5 zones after LDH isoenzyme pattern analyse. The proportion of LDH-5 was changed and LDH-5 sub-band was detected in control and combination group. The experiment indicated that Ber. can affeet enzymic metablism of inner cell in the process of increasing leukocyte. There was simultaneously with a change in ratio of LDH isoenzyme pattern.
ABSTRACT
In the Ca - free solution .the relaxation induced by acctylcholine ( Ach ) inthe rabbit aortic strips is inhibited and the inhibition is removed when the concentration of the Ca2+ is restored. In the groupe of ME ( norepinephrine ) 0.4 ?mol ? L-1 hydro-choloride berbamine (HBA ) 1, 10?mol ? L-1 and Verapamie (Ver) 0. 1, 1?mol ? L-1 did not inhibit the relaxation induced by Ach,and HBA has tendency of promoting the relaxation. While HBA 100?mol ? L-1 and Ver 10?mol ? L-1 inhibit the relaxation obviously. In the group of KCl,the three concentration of HBA and Ver all have the tendency of promoting the relaxation. The result suggest: thatthe effection of HBA to the relaxation of in-dothelium dependence is complicated, the higher concentration inhibit the relaxation and the lower promote it. It prove that the effection of HBA to the transportation of indothelium's Ca2+ or to the release of the EDRF is complicated
ABSTRACT
The contraction of the isolated rabbit renal arteries induced by noradrenaline, high K+ & calcium could be relaxed by berbamine ( BA ). BA shifted dose-response curve of noradrenaline, high K+ snd calcium to the right, but the maximal response was reduced. The antagonistic parameter pD' 2 of berbamine on calcium contrac-tion was 4.76, which is similar to the verapamil (pD'2=5.68). Therefore berbamine can be considered as a non-competitive calcium antagonist.
ABSTRACT
Objective To explore the efficacy of calmodulin antagonist berbamine(BBM)on multidrug resistance(MDR)reversal and its mechanism. Methods Human breast cancer cell line MCF7 and its adriamycin-resistant counterpart MCF7/ADR were used in the study.The cells were cultured with ADR and different concentration of BBM. MTT assay was used to analyze the effect of BBM on cell growth inhibition.According to the MTT assay,the 50% inhibitory concentration(IC 50 ),the multiples of drug resistance and increased sensitivity of ADR were calculated.The concentration of intracellular ADR and expression level of P-glycoprotein(P-gp)were detected by flowcytometry(FCM).The mRNA expression level of mdr1 gene was detected by semi-quantitative reverse transcriptase polymerase chain reaction(RT-PCR)with ?-actin as internal reference. Results The IC 50 of ADR in MCF7 and MCF7/ADR cells were(0.98?0.06)?mol/L and(101.20?5.72)?mol/L,respectively.The resistant multiple of MCF/ADR cells to ADR was 103 folds higher than that of MCF7 cells.BBM increased the chemo-sensitivity of ADR in MCF7/ADR cells with dose-dependent relationship,i.e.when 5*!?mol/L ,10*!?mol/L and 20*!?mol/L BBM was added into the culture the chemo-sensitivity of ADR was increased to 2.76,5.88,and 28.26 folds(P