Asian Journal of Pharmacodynamics and Pharmacokinetics

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Xu HY et al. Asian Journal of Pharmacodynamics and Pharmacokinetics 2009; 9(1):11-25 In mixed decoction of Rhizoma Coptidis and Radix et Rhizoma Glycyrrhizae, the former’s main constituent may be remained, but chemical constituents of Radix et Rhizoma Glycyrrhizae disappear completely. But no new chemical compound could be found in the process [6] . Studing on content variation of chemical constituents during combination of Rhizoma Coptidis with Fructus Evodiae,the dissolution rate of jateorhizine, coptisine, palmatine and berberine decreased obviously. At the same time, the dissolution rate lineared correlation with the proportion of Rhizoma Coptidis. It could be concluded that Rhizoma Coptidis’ Alkaloids reacted with Fructus Evodiae’s Flavonoids [7] . Berberine Coptisine Palmatine Jatrorrhizine Worenine Epiberberine Fig 3. Chemical structures of berberine,coptisine, palmatine, jatrorrhizine, worenine and epiberberine Magnoflorine Ferulaic acid Fig 4. Chemical structures of magnoflorine and ferulaic acid Pharmacological Actions In Traditional Chinese Medicine, Coptidis Rhizoma has the effects of suppressing fever, dispelling dampness and deintoxication. Through modern pharmacological studies, it has been proved to have many pharmacological effects including antimicrobial activity, hypoglycemic activity, anti-inflammatory, antioxygen and free radicals scavenging and anticancer effects etc..Berberine, the major component of this herb, has also many pharmacological effects including inhibition of adipocyte differentiation, anti-cancer effects, anti-microbial effects, LDL-lowering effects and anti-inflammatory potential [8] . Antimicrobial Activity Coptis and berberine showed wide inhibitory actionon bafungi prorozoon and virus in vitro and in vivo. [2] Berberine was found to be active against a number of Gram-positive and Gram-negative bacteria, such as Stephylococcus aureus, S. hemolylicus, 13
Xu HY et al. Asian Journal of Pharmacodynamics and Pharmacokinetics 2009; 9(1):11-25 Salmonella typhsa, Shigella dysenterial, S. paradysenterial, and so on. Berberine sulfate showed to be bacterial to vibrio chloral and and bacteriostatic to Stephylococcus aureus at concentrations of 35 and 50 µg·mL -1 , respectively. It showed bacteriadal activity against Stephylococcus aureus at 50-500 µg·ml -1 in culture medium. Berberine sulfate in concentrations 10-25µg·ml -1 inhibited the growth of 11 fugni. Oral administration of berberine sulfate at dose of 35-700 mg·kg -1 was effective in treating candicans infections of the intestine in mice. [9] Rhizoma Coptidis has strong antibacterial action and broad spectrum antibacterial activities, including Gram-positive and Gram-negative bacteria, aerobe and anaerobe. The biologically active constituent of C. chinensis extract is characterized as the isoquinoline alkaloids,such as berberine, palmatine,jateorhizine, coptisine etc.. Those constituents are potent inhibitors of sortase (a bacterial surface protein anchoring transpeptidase from Staphylococcus aureus ATCC 6538p), with an IC 50 value of 8.7 µg·mL -1 and have antibacterial activity against Gram-positive bacteria with a minimum inhibitory concentration (MIC) in the range of 50–400 µg·mL -1 . Among the four isoquinoline alkaloids tested, berberine chloride had the strongest inhibitory activity [10] . George Tegos [11] et al have reported that the activities of berberine were considerably against the gram-positive bacterium Staphylococcus aureus and Bacillus megaterium and that disabling of the MDRs (multidrug resistance pumps ) in gram-negative species leaded to a striking increase in antimicrobial activity. Gram-negative bacteria had an effective permeability barrier, comprised of the outer membrane, which restricts the penetration of amphipathic compounds, and multidrug resistance pumps (MDRs), which extrude toxins across this barrier. Direct measurement of the uptake of berberine, a model plant antimicrobial, confirmed that disabling of the MDRs strongly increases the level of penetration of berberine into the cells of gram-negative bacteria. Rhizoma Coptidis have long been used for the treatment of gastrointestinal disorders, insomnia, refractoriness dental ulcer, tinnitus in traditional oriental medicine [12] . According to the Basic Theory of Chinese Traditional Medicine, it has the efficacy of Clearing away heat, depriving evil wetness and purging fire for removing toxin. These pharmacologic actions attribute to antibacterial action which can cure infectious diseases. For example, Zuo-Jin-Wan, a Chinese medical formula including Rhizoma Coptidis and Fructus Evodiae, is used to cure gastrointestinal disorders, such as peptic ulcer, chronic gastritis, functional dyspepsia etc., which are correlated to Zuo-Jin-Wan on anti-Hp action [13] . Hypoglycemic Activity Rhizome Coptidis and its major constituent berberine have good hypoglycemic and hypolipidemic effects. The potential glucoselowering effect of berberine was noted when it was used for diarrhea in diabetic patients. In vitro and in vivo studies have showed its effects on hyperglycemia and dyslipidemia. Zhang Y [14] et al have reported that in the berberine group, fasting and postload plasma glucose decreased from 7.0 ±0.8 to 5.6 ± 0.9 and from 12.0 ± 2.7 to 8.9 ± 2.8 mM·L -1 , HbA1c from 7.5 ±1.0% to 6.6 ±0.7%, triglyceride from 2.51 ±2.04 to 1.61±1.10 mM·L -1 , total cholesterol from 5.31±0.98 to 4.35±0.96 mM·L -1 , and low-density lipoprotein-cholesterol from 3.23 ± 0.81 to 2.55 ± 0.77 mM·L -1 , with all parameters differing from placebo significantly. The glucose disposal rate was increased after berberine treatment. Mild to moderate constipation was observed in five participants in the berberine group. So berberine is effective and safe in the treatment of type 2 diabetes and dyslipidemia. In one clinical study, 60 patients with type 2 diabetes were treated with berberine for 1–3 months, and 90% of patients showed improvement in their clinical symptoms [15] . Recently, it has been reported that activating the AMP-activated protein kinase (AMPK) pathway is the underlying mechanism for berberine improving insulin resistance, lowering blood sugar, and correcting lipid metabolism disorders [16-19] . Berberine can reduce body weight and lipid levels and improve insulin action .Berberine acutely activates AMPK activity, and induces a variety of metabolic effects consistent with AMPK activation. These include activation of GLUT4 translocation; increasing phosphorylation of AMPK, ACC, and p38 MAPK; reducing lipid content in adipocytes; increasing expression of genes involved 14
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