Articles

Huang Lian

Coptis chinensis Franch, Coptis

Dosage

Decoction: 1.5-3g of the drug are taken for decoction.
Powder: 0.3-0.6g of its powder are taken each time.
The drug can be made into pills.
For external application, proper amount of the drug powder, extract or decoction can be applied to the local area or be used to wash the local area.
5:1 concentrated extract: 0.3-1g/day

Toxicity

It was reported that for stomach administration of Huang Lian decoction to mice the LD50 was 17.22 ± 1.75g/kg, and that of Berberine given to mice was 0.90 ± 0.04g/kg. (1)

In another report, when Huang Lian Tang (Coptis Decoction) was given orally to mice at a dosage of 27g/kg per day which was 400 times higher than clinical dosage, no significant toxic and side effects were noted. (2)

Chemical Composition

Berberine; Coptisine; Epiberberine; Palmatine; Jatrorrhizine; Worenine; Columbamine; Magnoflorine; Berberrubine; Ferulic acid; Chlorogenic acid; Obakunone; Obakulactone. (3) , (4) , (5) , (6) , (7) , (8)

Inorganic Chemicals

It also contains trace elements such as Cu, Zn, Mn, Fe, Sr, K, Ca and Mg.

Precautions

Huang Lian should be used with caution for those patients with vomiting due to deficiency of the stomach, splenasthenic diarrhea or diarrhea in early morning. One report described that gastrointestinal tract symptoms such as epigastric discomfort, constipation or diarrhea were observed in 14% of patients with arrhythmia taking Berberine orally. (9) In other reports, Berberine tablet administrated orally or injected intramuscularly occasionally caused allergic reaction such as drug rash, dermatitis and thrombocytopenia, even resulting in allergic shock. (10) , (11) , (12)

Pharmacology

Disinfecting root canal of deciduous teeth

Bacteriological test proved that Huang Lian extract had bactericidal power and bacteriostatic effect on anaerobic bacteria in an infected root canal of deciduous teeth. The effect was stronger than that of phenol camphor, but close to that of formo-cresol. At the same time, Huang Lian extracts did not stimulate mucosa or periapical tissues of deciduous teeth in tested animal. These results suggested that Huang Lian extract was an ideal sterilizing medicine for treating infected root canal of deciduous teeth. (13)

Hypoglycemic action

One report showed that both berberine and its liposome exerted significant hypoglycemic effects and caused by exogenous glucose. Berberine liposome, which was produced by combination of berberine with phospholipid, appeared to have a stronger hypolycemic effect than berberine alone and favored berberines absorption. (14)

Bacteriostasis

In one extracorporeal test, Huang Lian strongly inhibited HP growth. The minimum inhibition concentration (MIC) was 1:640-1:320. This suggested that the herb can inhibit in vitro HP growth. (15)

Effects on reducing blood-lipid

An in vitro test showed that Huang Lian decoction at 5% reduced the production of MDA in encephalic homogenate of mice. In vivo test, a Huang Lian decoction at 10% was given to rats via abdominal administration. Alloxan induced lipid peroxidation decreased the MDA level in rat spleen and liver. (16) Administration of Huang Lian water extract solution (10%) can significantly lower MDA and TG triglycerides levels in rats. (17)

Effects on human nasopharyngeal carcinoma cells

Tang Fa Qing, et al. reported that Huang Lian was effective in killing HNE1 either used as single herb or in a formula. As a single herb, the effect showed a strong correlation with the concentration. The half inhibition concentration was 1:729. When used in a formula, the effect was slightly reduced, with both concentration-response and time-effect correlation. The half inhibition concentration was 1:249. (18)

Tian Dao Fa reported that a Huang Lian decoction strongly suppressed rDNA activity in HNE3. (19) Another clinical study showed that Huang Lian, as a single drug or in formulas, exerted significant therapeutic effects on Nasopharyngeal Carcinoma Cells in nuke mice. When Huang Lian was removed from these formulas, the effect was decreased. (20)

Effect of preventing gastric mucosa from injury and antiemesis action

Qin Cai Ling et al. reported that Huang Lian Tang (Coptis Decoction) prevented gastric mucosa from injury caused by alcohol, hydrochloric acid, and aspirin. Also, it was very effective in suppressing the emesis of a pigeon induced by copper sulfate. (21)

Protection of Cardiac Muscle Cell

In one report, berberine hydrochloride, in a small dosage (10 mg/ml) acted on hypoxia cardiac muscle cells cultured in vitro by strongly preserving myocardial impulse, release of lactic dehydrogenase (LDH), cell survival rate, and cell ultrastructure. In a large dosage (30 mg/ml), it aggravated cardiac muscle cell injury caused by oxygen deficit. The results suggested that berberine hydrochloride, in small dosages, could protect cultured cardiac muscle cell against hypoxia injury. (22)

Xuan Bo, et al. reported that intraperitoneal injection of berberine to rats (which had undergone coronary artery ligation operation for 24 hours) in a dosage of 12mg/kg-1 significantly decreased myocardiac infarction scope, inhibited the increase in free fatty acid (FFA) in serum, and reduced incidence rate of pathologic Q wave after infarct occurred. This suggested that berberine had protective effects on ischemic cardiac muscle cells. (23)

Antiarrhythmic action

In one report, an intravenous injection of berberine in rats (1-4 mg/kg-1) decreased the incidence rate of ischemic arrhythmia. The effect showed dosage dependency. At 4 mg/kg-1, it significantly inhibited abnormal changes of blood rheology, such as increased agglutination of platelets and RBC’s, elevated blood viscosity, induced by myocardial ischemia in rats. At 30 mmol/L-1, it suppressed the shortening of action potential duration (APD) and effective refractory period (ERP) which was induced by hypoxia in extracorporeal cardiac muscle cell of a guinea pig, furthermore it decreased the action potential amplitude (APA), overshoot (OS) and action potential zero phase Vmax, which was probably berberine’s mechanism in counteracting ischemic arrhythmia. (24)

Another report showed that berberine (10 mg/kg-1) remarkably decreased incidence rate of VT after ischemia or reperfusion, and shortened VT enduring without VF ventricular fibrillation or death occurrence. One in vitro test showed that berberine (30 ì mol/L-1) suppressed Ca2+) influx in cardiac muscle cells under hypercalcemic conditions. The influx was promoted under hypocalcemic conditions. The above results suggest that berberine might prevent arrhythmia occurrence following reperfusion and produce bidirectional regulation on 45 Ca influx in cardiac muscle cells. According to the concentrations of 45 Ca, especially in hypercalcemic conditions, the suppressing effect might involve a mechanism, which could counteract arrhythmias. (25)

Against cerebral ischemia action

Wu Jun Fang, et al. reported that i.p. injection of berberine (20 mg/kg-1 per day) for 1, 3, and 5 days in rats which had suffered from reversible middle cerebral artery obstruction (MCAO) for 24 hours. Berberine was effective in decreasing platelet adhesiveness, inhibiting ADP induced platelet aggregation, collagen and arachidonic acid, and reducing TXB2 level in serum. The injection of the same dosage for 3 or 5 days inhibited thrombosis. The results of this experiment suggest that berberine probably affects anti-cerebral ischemia by preventing platelet adhesiveness and aggregation, while also affecting arachidonic acid metabolism. (26)

Effects on gastric ulcer of rats

Lu Gan, et al. reported that abdominal injection of berberine (20g/kg per day) in rats with a chronic gastric ulcer induced by acetic acid improved the gastric ulcer by significantly suppressing secretion of basal gastric acid and decreasing the chronic ulcerous area. (27)

Effects on rabbit’s diaphragm

It was reported that an intravenous injection of Berberine in rabbits (4mg/kg) increased the ratio of diaphragm myoelectric high frequency to low frequency, Fc and amplitude of evoked potential. It also exerted therapeutic effect on DiF in model rabbits. (28)

Effects on lymphocyte and vascular endotheliocyte ICAM-1

He Yu, et al. reported that Berberine inhibited adhesion of lymphocytes with endothelioid cells that was either quiescent or activated by IL-1 and TNF, the main molecular mechanism of which was that berberine hindered ICAM-1 expression on the endothelioid cell surface. Berberine had an obstructive effect on recirculation of lymphocyte by decreasing the adhesion of IL-1 activated lymphocyte with endothelioid cells, which may be one mechanism of berberine, which produces an immunosuppressant action. (29)

Protection of central nerve cell

It was reported that Berberine (1-25 m mol/L) acted to different degrees on decreasing injuries of pallial nerve cells in a rats fetal body cultured in vitro induced by glutamic acid, heme, ischemia or reperfusion, suppressing release of LDH in a supernatant fluid of culture fluid, significantly increasing the GSH level in cell hornogenate, and reducing MDA production. The results of the report suggested that berberine protected the central nerve cells from oxidation and irritable injury. The mechanism may be related to its efficacy in increasing glutathione level (an anti-oxidant) and hindering production of lipid peroxide. (30)

References

  1. Li Jian Rong, et al. Huang Lian decoction’s effects on mice acute toxicity and Berberine level. China Journal of TCM Information. 1999;6(10):32-33.
  2. Qin Cai Ling, et al. Research on Huang Lian Tang (Coptis decoction)’s preventive effects on experimental stomach mucosa injuries and suppression on vomiting. China Journal of Chinese Medicine. 1994;19(7):427-429.
  3. Xiao Pei Gen, et al. Research on pharmacy of the Chinese herb Huang Lian. Journal of Chinese Materia Medica. 1984;p15(3):30.
  4. Fang Xin Ping, et al. Quantity determination of 5 kinds of Huang Lian that are produced in China. China Journal of Chinese Medicine. 1989;14(2):97-99.
  5. Chinese Materia Medica. State Drug Administration of China, Shanghai Science & Technology Press, Inc. 1998.
  6. Fang Xin Ping, et al. Research on alkaloids in rhizome, stem, and leaf of Huang Lian genus. Journal of Traditional Chinese Medicine Material. 1989;12(3):33-35.
  7. Wang Ben Xiang. Modern TCM Pharmacology. Tianjin Science & Technology Press, Inc. 1997.
  8. Ye Yu Lan, et al. Analysis of 8 kinds of trace elements in Huang Lian and prepared Huang Lian products.” Journal of Traditional Chinese Medicine Material. 1994;17(11):27-28.
  9. Huang Wei Ming. Therapeutic observations on Berberine’s treatment for 50 cases of ventricular arrhythmia. Journal of Applied Internal Medicine. 1985;5(11):587.
  10. Bao Yu Qin. Adverse reactions of Berberine and Huang Lian. Journal of Integrated Traditional Chinese and Western Medicine. 1983;3(1):31-33.
  11. Zhan Rui Lin. One case of allergic reaction due to Huang Lian administration. China Journal of Chinese Medicine. 1994;19(1)-47.
  12. Pang Chong. Report of two cases of Huang Lian induced allergic reaction. China Journal of TCM Information. 1997;4(1).
  13. Su Rui Yun, et al. Research on Huang Lian extract’s disinfecting effects on root canal of deciduous tooth. China Journal of Stomatology. 1992;27(5):302-305.
  14. Liu Yan Xin, et al. Experimental research on hypoglycemic effects of Berberine and its liposome. Primary Journal of Traditional Chinese Medicine. 1999;13(1):18-19.
  15. Chen Zhi Yun, et al. Experimental research on 100 Chinese herbs’ antibacterial effects on helicobacteria. Journal of Shizhen Medicinal Material Research. 1996;7(1):25-26.
  16. Song Lu Cheng, et al. Huang Lian’s effects on lipid peroxidation and MDA in rats. Journal of Integrated Traditional Chinese and Western Medicine. 1992;12(7):421-423, 390.
  17. Song Lu Cheng, et al. Huang Lian’s effects on MDA and TG activities. Shaanxi Journal of TCM. 1996;17(3):137-138.
  18. Tang Fa Qing, et al. Research on killing effects of Huang Lian and its formulas on human nasopharyngeal carcinoma cells. Journal of Hunan College of TCM. 1995;15(4):41-44.
  19. Tian Dao Fa, et al. Comparison between suppression effects of Huang Lian and anti-tumor drugs on HNE3 cell’s rRNA activity. Journal of Hunan College of TCM. 1990;10(3):152-154.
  20. Tian Dao Fa, et al. Therapeutic effects of Huang Lian and its formulas on nasopharyngeal carcinoma cells in nuke mice. Journal of Hunan College of TCM. 1996;16(1):43-45.
  21. Qin Cai Ling, et al. Research on Huang Lian Tang (Coptis decoction)’s preventive effects on experimental stomach mucosa injuries and suppression on vomiting. China Journal of Chinese Medicine. 1994;19(7):427-429.
  22. Chen Qin Ming, et al. Protective effects of berberine cultivated cardiac muscular cell hypoxia injuries. Journal of Pharmacology and Clinical Application of TCM. 1993;9(2): 34-37.
  23. Xuan Bo, et al. Berberine’s protective effects on rats with experimental myocardiac infarction. Chinese Pharmacology Bulletin. 1995;11(3):221-223.
  24. Wang Yong Xiao, et al. Berberine’s effects and mechanism in counteracting ischemic cardiac arrhythmia. China Journal of Pharmacology and Toxicology. 1993;7(2):108-111.
  25. Li Ping, et al. Berberine’s effects on rats reperfusion induced cardiac arrhythmia and calcium regulation. Chinese Pharmacology Bulletin. 1995;11(3):217-220.
  26. Wu Jun Fang, et al. Berberine’s effects on platelet aggregation and serum levels of TXB2 and 6-keto-PGF1a in rats with cerebral ischmia. Journal of Pharmacy. 1995;30(2):98-102.
  27. Lu Gan, et al. Experimental research on Berberine’s promotion of recovery from stomach ulcer in rats. New Journal of Digestive Diseases. 1996;4(3):130-131.
  28. Ge Min, et al. Berberine’s effects on diaphragm function in rabbits. Journal of Bangbu Medical College. 1996;21(2):76-77.
  29. Hao Yu, et al. Berberine’s effects on adhesion and adhesive factors in lymphocytes and blood vessel endothelial cells. China Journal of Immunology. 1999;15(11):523-525.
  30. Wu Jun Fang, et al. Berberine’s protective effects on central nervous cells from oxidation stress. China Journal of Pharmacy. 1999;34(8):525-529.