• Title, Summary, Keyword: Berberine

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Studies on Bioavailability of Berberine Pamoate (I) (파모인산베르베린의 생체내(生體內) 이용률(利用率)에 관한 연구(硏究) (I))

  • Yang, Jae-Heon
    • Journal of Pharmaceutical Investigation
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    • v.16 no.2
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    • pp.76-84
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    • 1986
  • Berberine is one of alkaloids extracted from Phellodendri Cortex or Coptidis Rhizoma and has extensively used as an antibacterial and antidiarrheal drug. In order to increase the bioavailability of berberine preparation, berberine pamoate was synthesized and investigated on its usage in vitro and in vivo. Berberine was more rapidly extracted from herbal plants by hot water extraction method than soxhlet extraction method. Berberine pamoate was easily synthesized from berberine hydrochloride and potassium pamoate solution and identified using the infrared spectrum. Quantitative analysis of berberine was possible in methanol solution by fluorometric determination. The dissolution rate of berberine pamoate was more decreased than that of berberine hydrochloride in simulated gastric fluid and simulated intestinal fluid. The remaining proportion of berberine pamoate in the small intestine of rat was maintained at high concentration for a long time as compared with that of berberine hydrochloride.

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Effects of Berberine on Lymphocyte Proliferation and GM-CSF Production in Mice. (마우스 림프구증식과 GM-CSF생성에 미치는 Berberine의 효과)

  • Kim, Eun-Young;Rho, Min-Hee;Chung, Yang-Sook;Kim, Hyoung-Su;Kim, Kwang-Hyuk
    • Journal of Life Science
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    • v.17 no.5
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    • pp.694-698
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    • 2007
  • Berberine, an alkaloid initially isolated from chinese herbal medicine, has antibiotic activities against a variety of organisms including bacteria, viruses, fungi, protozoans, and chlamydia. Furthermore, berberine has shown a number of beneficial effects, including anti-tumor, anti-inflammation, and vasodilatory effects. In this work we have investigated the effects of berberine on lymphocyte proliferation and GM-CSF production in mice. Mouse splenocytes were incubated with berberine and concanavalin A(Con A) to observe the effects on cell proliferation. The culture supernatants of splenocytes exposed to berberine, berberine plus LPS, and berberine plus Con A were harvested to assay GM-CSF. The cell proliferation of nice splenocytes exposed to berberine only($1{\mu}g/ml$) was increased significantly more than PBS(control) group. But the Con A-induced cell growth was inhibited by berberine. The GM-CSF production from mice splenocyte culture exposed to berberine only was increased in comparison with PBS(control) group, but the production of it with LPS or Con A was inhibited by berbeline. The present findings may explain lympocyte proliferating and regulating effects of berberine.

Effects of Phosphate, Precursor and Exogenous Berberine on the Production of Alkaloid in Plant Cell Cultures

  • Kim, Dong-Il
    • Journal of Microbiology and Biotechnology
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    • v.1 no.1
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    • pp.79-83
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    • 1991
  • The effects of phosphate concentration in the medium, feeding of biosynthetic precursor, and the addition of exogenous berberine on cell growth and berberine production were studied in cell suspension cultures of Thalictrum rugosum. The depletion of phosphate in the medium enhanced the specific productivity up to twofold with significant release of berberine into the medium. Extracellular berberine was 19% of the total in the culture without phosphate while it was 2-5% of total berberine in the culture with even low amounts of phosphate. Precursor feeding was not effective in enhancing alkaloid formation. Initial presence of exogenous berberine did not have much effect on cell growth and alkaloid production. It was found that the cells have the capacity to take up large quantities of berberine. When $500{\;}mg{\cdot}l^{-1}$ of berberine was added exogenously at the beginning, 81% of total berberine was found in the cells.

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Berberine Inhibited Radioresistant Effects and Enhanced Anti-Tumor Effects in the Irradiated-Human Prostate Cancer Cells

  • Hur, Jung-Mu;Kim, Dong-Ho
    • Toxicological Research
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    • v.26 no.2
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    • pp.109-115
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    • 2010
  • The purpose of this study was to elucidate the mechanism underlying enhanced radiosensitivity to $^{60}Co\;{\gamma}$-irradiation in human prostate PC-3 cells pretreated with berberine. The cytotoxic effect of the combination of berberine and irradiation was superior to that of berberine or irradiation alone. Cell death and Apoptosis increased significantly with the combination of berberine and irradiation. Additionally, ROS generation was elevated by berberine with or without irradiation. The antioxidant NAC inhibited berberine and radiation-induced cell death. Bax, caspase-3, p53, p38, and JNK activation increased, but activation of Bcl-2, ERK, and HO-1 decreased with berberine treatment with or without irradiation. Berberine inhibited the anti-apoptotic signal pathway involving the activation of the HO-1/NF-${\kappa}B$-mediated survival pathway, which prevents radiation-induced cell death. Our data demonstrate that berberine inhibited the radioresistant effects and enhanced the radiosensitivity effects in human prostate cancer cells via the MAPK/caspase-3 and ROS pathways.

Effect of Berberine on the Proinflammatory Cytokines Production in Mice (베르베린이 마우스 전염증성 사이토카인의 생성에 미치는 영향)

  • Chung, Su-Ryoung;Choi, Myung-Won;Park, In-Dal;Kim, Kwang-Hyuk
    • Journal of Life Science
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    • v.20 no.8
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    • pp.1276-1280
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    • 2010
  • Berberine has shown a number of beneficial effects, including anti-tumor, anti-inflammation, and vasodilatory effects. In this work we investigated the effects of berberine on the production of proinflammatory cytokines such as TNF-$\alpha$, IL-$1{\beta}$, and IL-6 in mice. The supernatants of cultured splenocytes exposed with berberine or berberine plus LPS were harvested to assay TNF-$\alpha$, IL-$1{\beta}$, and IL-6. The sera from the mice injected with berberine or berberine plus LPS were then isolated to assay these cytokines. The TNF-$\alpha$ production in mice splenocyte cultures exposed to berberine was inhibited compared to the PBS control. The sera from LPS plus berberine injected mice showed lower levels of TNF-$\alpha$ compared to those of LPS only injected mice. The IL-$1{\beta}$ production in mice splenocyte cultures exposed to berberine was inhibited at a high dose (3.0 ${\mu}g/ml$) compared to the PBS control. Also, the increase of IL-$1{\beta}$ by LPS exposure in splenocyte cultures was inhibited by a high dose of berberine. The IL-6 in splenocyte culture supernatants showed lower levels after berberine compared to the PBS control. Also, production of IL-6 after LPS exposure in splenocyte cultures was inhibited by a low dose of berberine (0.3 ${\mu}g/ml$). These findings suggest the probability that berberine down-regulates the production of proinflammatory cytokines such as TNF-$\alpha$, IL-$1{\beta}$, and IL-6.

The protective effect of berberine on Propionibacterium acnes-induced inflammatory response in human monocytes (여드름균에 의해 염증 반응이 유도된 인간 단핵구 세포에서 알칼로이드 화합물 berberine의 항염증 효과)

  • Kim, Hyun Pyo;Yoon, Young Geol
    • Journal of Applied Biological Chemistry
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    • v.61 no.2
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    • pp.181-186
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    • 2018
  • In this study, we investigated the anti-inflammatory activity of berberine using human monocytes. Infection of Propionibacterium acnes induced the production of nitric oxide (NO) and the pro-inflammatory cytokines such as, $TNF-{\alpha}$, IL-8 and $IL-1{\beta}$ in THP-1 monocytic cells. However, when berberine was supplemented in these P. acnes-induced THP-1 cells, the production of pro-inflammatory cytokines and NO was significantly reduced. We also analyzed signaling pathways of the antiinflammatory function of berberine and found that berberine suppressed the phosphorylation of ERK1/2, JNK and p38 and the expression and nuclear translocation of $NF-{\kappa}B$ p65 in the P. acnes-induced cells. From these results, we concluded that berberine can effectively exert the anti-inflammatory activity via suppressing the $NF-{\kappa}B$ and mitogen-activated protein kinases signaling pathways in human monocytes. Moreover, these results suggest the feasibility of developing natural therapeutics using berberine for the treatment of P. acnes-induced inflammatory diseases.

Influence of berberine on the blood pressure of rabbits

  • Ko, Suk-Tai;Lim, Dong-Yoon
    • Archives of Pharmacal Research
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    • v.3 no.1
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    • pp.23-30
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    • 1980
  • Berberine, when administered into a ear-vein of the rabbit anesthetized with urethane, produced a long-lasting, dose related fall in blood pressure, but intraventricular berberline did not elicit the hypotensive response. This hypotensive activity of berberine was not influenced by pretreatment of vagotomization and atropine. Depressor responses induced by berberine were not impaired by diphenhydramine, chlorisondamine, guanethidine and propranolol, but reduced significantly by phentolamine pretreatment. Berberine attenuated markedly prossor responses of norepinephrine and epinephrine. These results suggest that berberine causes the hypotensive activity that is attributable to alpha adrenoceptor blockade, but not to a direct relaxant effect upon vascular smooth muscle.

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Effects of Berberine on L-DOPA Therapy in 6-Hydroxydopamine-induced Rat Models of Parkinsonism (Berberine이 백서의 6-Hydroxydopamine-유도 파킨슨병 모델에서의 L-DOPA 요법에 미치는 영향)

  • Shin, Kun-Seong;Kwon, Ik-Hyun;Choi, Hyun-Sook;Lim, Sung-Cil;Hwang, Bang-Yeon;Lee, Myung-Koo
    • YAKHAK HOEJI
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    • v.55 no.6
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    • pp.510-515
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    • 2011
  • Isoquinoline compounds including berberine enhance L-DOPA-induced cytotoxicity in PC12 cells. In this study, the effects of berberine on L-DOPA therapy in unilateral 6-hydroxydopamine (6-OHDA)-induced rat models of parkinsonism were investigated. Rats were prepared for the models of Parkinson's disease by 6-OHDA-lesioning for 14 days and then treated with L-DOPA (10 mg/kg) with or without berberine (5 and 30 mg/kg, i.p.) for 21 days. Treatment with berberine (5 and 30 mg/kg, i.p.) showed a dopaminergic cell loss in substantia nigra of 6-OHDA-lesioned rats treated with L-DOPA: 30 mg/kg berberine was more intensive neurotoxic. The levels of dopamine were also decreased by berberine (5 and 30 mg/ kg) in striatum-substantia nigra of 6-OHDA-lesioned rats treated with L-DOPA. These results suggest that berberine aggravates cell death of dopaminergic neurons in L-DOPA-treated 6-OHDA-lesioned rat models of Parkinson's disease. Therefore, the long-term L-DOPA therapeutic patients with isoquinoline compounds including berberine may need to be checked for the adverse symptoms.

Effects of Berberine on 6-hydroxydopamine-induced Parkinsonism in Rats (Berberine이 백서의 6-hydroxydopamine-유도 파킨슨병 모델에 미치는 영향)

  • Kwon, Ik-Hyun;Choi, Hyun-Sook;Shin, Kun-Seong;Hwang, Bang-Yeon;Lee, Myung-Koo
    • Korean Journal of Pharmacognosy
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    • v.40 no.4
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    • pp.351-356
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    • 2009
  • Many isoquinoline alkaloids including berberine lower dopamine content by reducing tyrosine hydroxylase (TH) activity and aggravate L-DOPA-induced cytotoxicity in PC12 cells. In this study, the effects of berberine on 6-hydroxydopamine (6-OHDA)-induced cytotoxicity in PC12 cells and on unilateral 6-OHDA-lesioned rat models were investigated. Berberine at 10-30 ${\mu}M$ did not affect cell viability in PC12 cells. However, berberine at concentrations higher than $50{\mu}M$ caused cytotoxicity at 24 h. Berberine (10-50 ${\mu}M$) also enhanced 6-OHDA (10-50 ${\mu}M$)-induced cytotoxicity at 24 h compared to 6-OHDA alone with an apoptotic process. In addition, treatment with berberine (5 and 30 mg/kg, i.p.) for three weeks showed a dopaminergic cell loss in substantia nigra of 6-OHDA-lesioned rats: 30 mg/kg berberine was more intensive cytotoxic. The levels of dopamine were also decreased by berberine (5 and 30 mg/kg) in the ipsilateral substantia nigra of 6-OHDA-lesioned rats. These results suggest that berberine aggravated 6-OHDA-induced cytotoxicity in PC12 cells and treatment with berberine (5 and 30 mg/kg) in 6-OHDA-lesioned rats also enhanced the degeneration of dopaminergic cell death and the decrease in dopamine levels in substantia nigra. Therefore, the long-term L-DOPA therapeutic patients with isoquinoline compounds including berberine may need to be checked for the adverse symptoms.

The Role of ROS and p38 MAP kinase in Berberine-Induced Apoptosis on Human Hepatoma HepG2 Cells (Berberine에 의한 HepG2 세포의 사멸과정에서 활성기산소와 p38 MAP kinase의 역할에 관한 연구)

  • Hyun, Mee-Sun;Woo, Won-Hong;Hur, Jung-Mu;Kim, Dong-Ho;Mun, Yeun-Ja
    • Applied Biological Chemistry
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    • v.51 no.2
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    • pp.129-135
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    • 2008
  • Berberine is an isoquinoline alkaloid used in traditional Chinese medicine and has been isolated from a variety of plants, such as Coptis chinensis and Phellodendron amurense. It has a wide spectrum of clinical applications such as in anti-tumor, anti-microbial, and anti-inflammatory activities. However, it is still unknown that berberine related with reactive oxygen species (ROS)-mediated apoptosis pathway in human hepatoma HepG2 cells. In the present study, we are examined the molecular mechanism of ROS- and p38 MAP kinase-mediated apoptosis by berberine in HepG2 cells. Berberine increased cytotoxicity effects by time- and does-dependent manner. $LD_{50}$ was detected 50 ${\mu}M$ at 48h of exposure to berberine. Nuclei cleavage and apoptotic DNA fragmentation were observed in cells treated with 50 ${\mu}M$ of berberine for 48h. Moreover, berberine induced the activating of caspase-3, p53, p38 and Bax expression, whereas the expression of anti-apoptotic signaling pathways, Bcl-2, was decreased. Additionally, berberine-treated cells had an increased level of generation of ROS and nitric oxide (NO). These results indicated that berberine induces apoptosis of HepG2 cells may be mediated oxidative injury acts as an early and upstream change, triggers mitochondrial dysfunction, Bcl-2 and Bax modulation, p38 and p53 activation, caspase-3 activation, and consequent leading to apoptosis.