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PHARMACOLOGICAL EFFECTS AND
HERB-DRUG INTERACTIONS OF
HEAT-CLEARING HERBS

By John Chen, L.Ac., O.M.D., Pharm.D., Ph.D.

Below is a section from Dr. John Chen’s Chinese Medical Herbology and Pharmacology. It describes in details the pharmacological effects and possible herb-drug interaction of heat-clearing herbs.

Definition: Heat-clearing herbs address imbalances caused by excessive heat, whether mild or extreme, at various levels of pathological penetration of the body, by clearing heat, purging fire, or cooling organs or substances injured by heat.

Heat is a pathogenic factor in many disease patterns. Warmth, heat and fire refer to degrees of severity of the same pathological entity, with warmth being the mild expression, heat the moderate condition, and fire the extreme. Heat-clearing herbs address a range of heat disorders:

Invasion of heat from the exterior to the interior
Excess heat and fire affecting internal organs
Excess heat at ying (nutritive) and xue (blood) levels
Accumulation of damp-heat in various areas of the body
Febrile disorders
Formation of pus and abscesses in or outside of the body
Conditions characterized as deficiency heat

In general, cool herbs clear heat while cold herbs purge fire from the body.

PHARMACOLOGICAL EFFECTS

Antibiotic: This includes antibacterial, antiviral and antifungal effects. More than 150 commonly-prescribed herbs have been tested for their antibiotic properties. The sensitivity of micro-organisms to the herbs is well established. Overall, researchers have concluded that herbs that clear heat and eliminate toxins have the most potent antibiotic effects. The benefits of using herbs to treat infections include a broad range of therapeutic actions and low risk of resistance, both of which may be attributed to the large number of bioactive components present within each herb, and the number of herbs present in each herbal formula.

Antibacterial: Herbs with antibacterial action include Jin Yin Hua (Flos Lonicerae), Lian Qiao (Fructus Forsythiae), Da Qing Ye (Folium Isatidis), Ban Lan Gen (Radix Isatidis), Pu Gong Ying (Herba Taraxaci), Zhi Mu (Radix Anemarrhenae), Zhi Zi (Fructus Gardeniae), Xia Ku Cao (Spica Prunellae), Huang Qin (Radix Scutellariae), Huang Lian (Rhizoma Coptidis), Huang Bai (Cortex Phellodendri), Mu Dan Pi (Cortex Moutan), Chi Shao (Radix Paeoniae Rubrae), and Qing Hao (Herba Artemisiae Annuae).

Antiviral: Herbs with antiviral effects are Jin Yin Hua (Flos Lonicerae), Lian Qiao (Fructus Forsythiae), Da Qing Ye (Folium Isatidis), Ban Lan Gen (Radix Isatidis), Pu Gong Ying (Herba Taraxaci), She Gan (Rhizoma Belamcandae), Chuan Xin Lian (Herba Andrographis), Huang Qin (Radix Scutellariae), and Huang Bai (Cortex Phellodendri).

Antifungal: These include Ren Dong Teng (Caulis Lonicerae), Bai Tou Weng (Radix Pulsatillae), Yu Xing Cao (Herba Houttuyniae), Huang Bai (Cortex Phellodendri), Xuan Shen (Radix Scrophulariae), Mu Dan Pi (Cortex Moutan), Zi Cao Gen (Radix Lithospermi) and Qing Hao (Herba Artemisiae Annuae).

Antineoplastic:Many heat-clearing herbs have antineoplastic properties. While the exact mechanisms of this activity vary between herbs, the results include suppressed growth of cancer cells and enhanced immunity of host cells. Herbs with antineoplastic actions include Qing Dai (Indigo Naturalis), Ya Dan Zi (Fructus Bruceae), Bai Hua She She Cao (Herba Oldenlandia), Ku Shen Gen (Radix Sophorae Flavescentis), Huang Lian (Rhizoma Coptidis), Xia Ku Cao (Spica Prunellae), Yu Xing Cao (Herba Houttuyniae), Ban Zhi Lian (Herba Scutellariae Barbatae), and Long Kui (Herba Solanum Nigrum).

Antipyretic:Fever is one of the main symptoms associated with infection. While elevation of body temperature is a defensive response, persistent high fever can cause a wide array of complications. The antipyretic effect of heat-clearing herbs is attributed to direct action on the central nervous system to reduce body temperature, or indirect action via treatment of infection. Herbs with distinct antipyretic action include Shi Gao (Gypsum Fibrosum), Zhi Mu (Radix Anemarrhenae), Huang Qin (Radix Scutellariae), Huang Lian (Rhizoma Coptidis), Zhi Zi (Fructus Gardeniae), Da Qing Ye (Folium Isatidis), Jin Yin Hua (Flos Lonicerae), Lian Qiao (Fructus Forsythiae), Di Gu Pi (Cortex Lycii), and others.

Anti-inflammatory: Herbs that clear heat treat both acute and chronic inflammation. Generally speaking, these herbs are more effective for acute cases of inflammation characterized by swelling and increased capillary permeability. Examples include: Jin Yin Hua (Flos Lonicerae), Lian Qiao (Fructus Forsythiae), She Gan (Rhizoma Belamcandae), Da Qing Ye (Folium Isatidis), Chuan Xin Lian (Herba Andrographis), Huang Lian (Rhizoma Coptidis), Huang Bai (Cortex Phellodendri) and Huang Qin (Radix Scutellariae).

Some herbs treat chronic cases of inflammation via stimulating the endocrine system to increase production of corticosteroids. When compared with oral steroids, herbs are gentler and less likely to cause side effects. Some examples are: Chuan Xin Lian (Herba Andrographis), Shan Dou Gen (Radix Sophorae Tonkinensis) and Bai Hua She She Cao (Herba Oldenlandia).

Immunologic:Heat-clearing herbs have various effects on the immune system: some herbs potentiate both specific and non-specific immune response, other heat-clearing herbs suppress the immune system.

Herbs that stimulate the immune system by increasing the phagocytic activities of macrophages include Huang Lian (Rhizoma Coptidis), Huang Qin (Radix Scutellariae), Zhi Zi (Fructus Gardeniae), Jin Yin Hua (Flos Lonicerae), Da Qing Ye (Folium Isatidis), Chuan Xin Lian (Herba Andrographis), Ye Ju Hua (Flos Chrysanthemi Indici), and Yu Xing Cao (Herba Houttuyniae).

Herbs that enhance cellular immunity include Bai Jiang Cao (Herba cum Radice Patriniae), Shan Dou Gen (Radix Sophorae Tonkinensis), Bai Hua She She Cao (Herba Oldenlandia), Huang Bai (Cortex Phellodendri) and Jin Yin Hua (Flos Lonicerae).

Herbs that suppress the immune system to treat allergy or auto-immune disorders include Huang Qin (Radix Scutellariae), Huang Lian (Rhizoma Coptidis), Mu Dan Pi (Cortex Moutan), and Chuan Xin Lian (Herba Andrographis).

Hematological: Unchecked febrile disorders often progress to heat attacking the ying (nutritive) and xue (blood) levels, conditions associated with increased activities of platelets, and coagulation. Therefore, many herbs that clear heat inhibit the aggregation of platelets and slow the coagulation process.

Herbs with antiplatelet activity include Chi Shao (Radix Paeoniae Rubrae), Ban Lan Gen (Radix Isatidis), Ye Ju Hua (Flos Chrysanthemi Indici), Niu Huang (Calculus Bovis), and Chuan Xin Lian (Herba Andrographis).

An herb with anticoagulant activity is Chi Shao (Radix Paeoniae Rubrae).

One example of an herb with thrombolytic action is Niu Huang (Calculus Bovis).

Antihypertensive: Many herbs that clear heat also act to lower blood pressure. The mechanism of action includes suppression of sympathetic stimulation, dilation of blood vessels, and diuresis. However, it is important to keep in mind that the antihypertensive actions of some of these herbs are only documented by in vitro studies via intravenous injection, and may not be replicated in clinical situations in vivo. Please refer to the monograph of each herb for additional details. Herbs with antihypertensive properties include Huang Lian (Rhizoma Coptidis), Huang Qin (Radix Scutellariae), Zhi Zi (Fructus Gardeniae), Zhi Mu (Radix Anemarrhenae), Di Gu Pi (Cortex Lycii), Mu Dan Pi (Cortex Moutan), Niu Huang (Calculus Bovis), Xuan Shen (Radix Scrophulariae), Lian Qiao (Fructus Forsythiae), Shan Dou Gen (Radix Sophorae Tonkinensis), Xia Ku Cao (Spica Prunellae), Long Dan Cao (Radix Gentianae), Ye Ju Hua (Flos Chrysanthemi Indici) and Ban Bian Lian (Herba Lobeliae Chinensis).

Hepatoprotective: In addition to clearing heat, many herbs also act to lower liver enzyme levels to protect the liver. These herbs may treat elevated liver enzymes, hepatitis, and drug- or chemical-induced liver damage. Herbs with hepatoprotective activity include Huang Qin (Radix Scutellariae), Lian Qiao (Fructus Forsythiae), Zhi Zi (Fructus Gardeniae), Bai Jiang Cao (Herba cum Radice Patriniae), Pu Gong Ying (Herba Taraxaci), and Long Dan Cao (Radix Gentianae).

Cholagogic: Herbs with cholagogic activity promote and regulate the normal production and release of bile acids, therefore minimizing liver- and gallbladder-related diseases. These herbs may be used to treat jaundice, cholecystitis, and cholelithiasis. Herbs with cholagogic actions include Jin Yin Hua (Flos Lonicerae), Yin Chen Hao (Herba Artemisiae Scopariae), and Chuan Xin Lian (Herba Andrographis).

Cardiotonic: Herbs with cardiotonic influence stimulate the heart tissues to treat cardiovascular diseases. Cardiotonic herbs include Lian Qiao (Fructus Forsythiae), Sheng Di Huang (Radix Rehmanniae), Xuan Shen (Radix Scrophulariae), and Zi Cao Gen (Radix Lithospermi).

POTENTIAL HERB-DRUG INTERACTIONS

Antibiotic, antipyretic and anti-inflammatory properties are the primary pharmacological characteristics of heat-clearing herbs. Such herbs are commonly used to treat infection, fever and inflammation, all characterized by increase in body temperature. Generally speaking, heat-clearing herbs with these therapeutic effects are not known to interact adversely with drug therapies.

Antibiotics: The concurrent use of herbs and drugs with antibiotic effects may enable these substances to exert a synergistic effect, or potentiate the effects of one another. The potentiating of antibiotic action offers a tremendous advantage, especially if the target micro-organism has high resistance or tolerance to standard pharmacological therapies. For example, the addition of baicalin, a component of Huang Qin (Radix Scutellariae), was effective in restoring the antibiotic potency of beta-lactam antibiotics (such as ampicillin, amoxicillin, methicillin and cefotaxime) against beta-lactam resistant Staphylococcus aureus and methicillin-resistant Staphylococcus aureus (MRSA). (i)

Ciprofloxacin (Cipro): Some heat-clearing herbs and antibiotic drugs should not be combined. It has been shown that the absorption of ciprofloxacin (Cipro), a quinolone antibiotic, may be affected by concurrent use of Pu Gong Ying (Herba Taraxaci), due to the high mineral content of the latter. While the bioavailability of ciprofloxacin was not altered significantly, there were changes to other pharmacokinetic parameters. (ii)

Antihypertensives: Some heat-clearing herbs also reduce blood pressure. Thus, concurrent use of some herbs and drugs that affect blood pressure should be prescribed carefully and monitored closely to avoid potential fluctuations of blood pressure.

REFERENCES
(i) J Pharm Pharmacol 2000 Mar; 52(3):361-6.
(ii) Journal of Pharmaceutical Sciences, 1999; June, 88(6):632-4.

ABOUT THE AUTHOR

John Chen, L.Ac., O.M.D., Pharm.D., Ph.D.

Dr. John Chen is a recognized authority in both western pharmacology and Chinese Herbal Medicine, having combined formal training in both fields with extensive research ‘on the ground’ in China. He teaches at the USC School of Pharmacy, Emperor’s College, Yo San University of TCM, OCOM, Five Branches, AOMA and ACTCM, and has taught numerous professional seminars across the U.S. and internationally. Dr. Chen’s published works include Chinese Medical Herbology and Pharmacology (2003, AOM Press) and the upcoming Chinese Herbal Formulas and Applications (2008, AOM Press) for which works he is lead author.

This article was taken from Dr. Chen’s book Chinese Medical Herbology and Pharmacologyand Pharmacology. To order a copy, click here.

To learn more about herbs, John Chen is speaking on the following topic for Lotus Institute. The class is approved for 8 CEUs/PDAs by the California Acupuncture Board and NCCAOM.

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