LEUNG'S
(CHINESE) HERB NEWS
Number 19
March/April 1999

Herbs in this issue:

Huperzia serrata

Astragalus root

Schisandra berry

Lycium fruit

 

A Note From Dr. Leung

     A major flaw of the Dietary Supplement Health and Education Act (DSHEA) is that it lumps together palliative (treatment) herbs with herbal foods and tonics in the same category as conventional supplements such as vitamins and minerals.  Due to this weakness in DSHEA, a sizable number of marketers are pushing for single-component drugs or highly purified chemical mixtures isolated from plants to be added to our diet, passed off as dietary supplements.  These chemicals, cleverly coined “nutraceuticals” to mean “nutritious chemicals” or “nutritional chemicals” and “functional foods” (as if regular foods don’t have any function) need not have a safe use history.  The only requirement is that they be originally present in plants (no matter how small the amount); and these plants need not have a history of being safely used as a food or true supplement.  Thus, huperzine A, basically a new drug isolated from a club moss (Huperzia serrata), is now on the market, with no restrictions.  So are some amphetamine analogs (tyramine, N-methyltyramine, synephrine, etc.) present

 

Dr. Leung is author of the Encyclopedia of Common Natural Ingredients Used in Food, Drugs, and Cosmetics (Wiley-Interscience), which was published in 1980 and revised in 1996. He is also creator of PHYTOMED, a prototype computer database on Chinese herbal medicine developed under contract with the National Cancer Institute.


 

in immature bitter orange (the drug called shizhi in Chinese), which are now used to replace ephedrine in mahuang; and chances are that their synthetic forms are being substituted.  Ginkgo leaf and kava extracts are now used in drinks, potato chips and other foods.  It won’t be long before many synthetic chemicals, originally present as minor constituents in plants, will be used in our foods, bypassing the regulations governing food additives or drugs.  And the consumers will be the guinea pigs.  Recently, I found an ad in a mail-order catalog pushing huperzine A: “Introducing the decade’s most exciting scientific discovery for improving memory!  Featured in the journal of the AMA, clinically-tested, filed with the FDA, and recommended by neurologists!”  That is rather scary.  I have nothing against this compound.  It can be an excellent drug for improving memory, but NOT as a daily supplement without being monitored for its potential long-term toxic side effects.  There is no history of food use for the herb from which this is derived!  After all, a natural chemical does not automatically attain “safety-hood,” allowing it to be ingested daily.  Look at atropine, aconitine, ephedrine, and cocaine, which are all natural.  The most logical thing to do is to allow its sale as an over-the-counter drug, and regulated it as such.  Or better still, make all treatment herbs a separate category from true herbal supplements (such as herbal foods and tonic herbs) and control them as natural therapeutics, distinct from drugs and true supplements.  The best option is to educate consumers so that they will be knowledgeable enough to make sensible personal choices and to “listen to their body” [Issue 18, pp.2-3].  Unfortunately, accurate and unbiased information on herbs is not easily available, thanks to self-interest groups who make sure whatever information disseminated to the public favors their interests, and to uninformed researchers, writers and editors who continue to report biased and meaningless information or misinformation.  That’s why we need to educate honest and unbiased researchers and writers/editors so that their publications will carry sound and meaningful, unbiased information.

                

Criteria for evaluating research on herbs and other natural products

        Too many scientists and researchers investigating botanical medicines frequently treat herbal materials as if they were pure single-component drugs.  This has resulted in countless numbers of publications that are meaningless (Issue 18, pp. 1-2), which in turn has wasted considerable amount of our precious resources and mental energy in disseminating and/or debunking.  To help scientists and writers/editors who are not familiar with the intricacies and complexities of natural product research, the following are some guidelines for evaluating and accepting natural products for study or manuscripts for publication. They also will serve as basic information for abstractors to include in their abstracts of published papers.  I have divided them into 2 standard levels.  The higher-level criteria should be ones whose attainment is our ultimate goal.  With this higher standard, results of investigations in this field are more likely to be consistently duplicated.  On the other hand, the minimal-level criteria are ones that should constitute the basic requirements for accepting a natural product for research or a manuscript for publication as well as minimal information to be included in abstracts.  This lower standard is necessary for now because, at present, there are not too many publications that meet the ideal criteria.  However, as researchers not trained in the comprehensive aspects of natural products research get acclimated to this field, the ideal criteria naturally will then be adopted.

 

1.  1.  Commercial products without disclosure of formulas.  Frequently, researchers publish reports based on a commercial or proprietary product, without revealing what the product is.  In the Chinese herbal/medical literature, there are many publications of this type.  The information in them is meaningless and useless, except to manufacturers and marketers of the investigated products.

Minimal (to allow traceability):

          Name and address of manufacturer

          Concentration(s) used in the study

          Method(s) of administration

          Source of financial support if other than manufacturer/marketer

Ideal:

          Reject the material or manuscript

2.  

    2.   Pure natural compounds.  They should be treated as any pure natural chemicals (e.g., caffeine, ephedrine, huperzine A, synephrine), with indication of whether they are isolated from plants or chemically synthesized..

Minimal:

          Chemical name

          Purity

          Concentration(s) used in study

          Method(s) of administration

     Ideal: (all above, plus):

          Plant source (Latin binomial), with authenticating authority

          Plant part (s), with authenticating authority

3.       

   3. Purified extracts containing artificially high concentrations of specific chemical compounds or groups of chemicals.  They include extracts of green tea with high amounts (e.g., 90%) of certain polyphenols (catechin, epigallocatechin, epigallocatechin gallate, etc.), of Asian ginseng with high total ginsenoside content (e.g., 80-90%), of grape seed or pine bark with high proanthocyanidin content (e.g., >80%), and of milk thistle with silymarin.  Since the contained chemicals are present in such artificially high levels, they no longer bear resemblance to the botanicals from which they are extracted.  These extracts are the ones that can cause the most problems.  Unless the whole extraction process (including solvents) is revealed, there is no easy way to ascertain, besides the named chemicals (markers or actives), what else is present in the extract.  For example, does the remaining part of the extract contain other even more active components from the botanical drug, or is it made up of only excipients?  What is the chemical profile of the extract?  Is this chemical profile consistent and how comparable is it to ones previously reported?  Variations among these factors can greatly affect the biological activities of these extracts.  The more precisely we identify these parameters, the more likely can the results be duplicated by future studies.  To perform scientific studies on these natural materials without addressing these issues would not yield consistent and meaningful results.

Minimal:

          Plant source(s) (Latin binomials), with authenticating authority

          Plant part(s), with authenticating authority

          Percent purity of marker(s)/active(s) in extract

          Chemical profile of marker(s)/active(s) (minimum 2 of: HPLC, TLC, GC, etc.)

          Concentrations used in study

          Method(s) of administration

Ideal (all above, plus):

          Nature of extract (solvents used and ratios)

          Total chemical profile of extract (minimum 2 of: HPLC, TLC, GC, etc.)

          Excipients used in extract

4.  

     4.   Standardized extracts.  These are extracts with a standardized amount of one or more marker or active compounds.  There are 2 major types: total extracts containing specified amounts of markers or actives; and partial extracts containing specified amounts of markers and actives, but lacking other components present in total extracts.  As with purified extracts containing high concentrations of specific markers or active compounds, the same types of issues relating to solvents used and consistency of chemical profile apply. 

Minimal:

          Plant source(s) (Latin binomials), with authenticating authority

          Plant part(s), with authenticating authority

          Percent purity of marker(s)/active(s) in extract

          Total chemical profile of extract (minimum 1 of: HPLC, TLC, GC, etc.)

          Concentrations used in study

          Method(s) of administration

Ideal: (all above, plus):

          Nature of extract (solvents used and ratios)

          Chemical profile of marker(s)/active(s) (minimum 2 of: HPLC, TLC, GC, etc.)

          Total chemical profile of extract (1 more of: HPLC, TLC, GC, etc.)

          Excipients used in extract

5.        

    5.    Regular extracts.  These are extracts with no standardized amounts of marker or active compounds.  Their strength may be expressed in ratios between raw herbs and extracts (e.g., 4:1, meaning 1 kg of extract is derived from 4 kg of raw herb) or as percent of herb material in a specific solvent (e.g., 20% extract in 70% ethyl alcohol, meaning 100 g or mL of the hydroalcoholic extract is derived from 20 g of crude herb).  However, these strengths are meaningless unless solvents used in their extraction are given.  For example, a strength of 10:1 to describe extracts of astragalus root or Asian ginseng root is meaningless, unless the solvent(s) are clearly stated, because a normal exhaustive extraction of either herb with water will result in extracts of no more than a 3.5:1 strength.  On the other hand, an extraction with 1-butanol would yield very little extractives and thus would result in extracts of high strength (e.g., 10:1).  However, these extracts do not represent these botanicals in traditional properties or in chemical profiles.

Minimal:

          Plant source(s) (Latin binomials), with authenticating authority

          Plant part(s), with authenticating authority

          Type of extract (tincture, fluid extract, solid extract, powdered extract, etc.)

          Solvent(s) used and ratios

          Strength (ratio of crude herb to extract)

          Concentration(s) used in study

          Method(s) of administration

Ideal (all above, plus):

          Total chemical profile of extract (minimum 2 of: HPLC, TLC, GC, etc.)

          Dosage form used (tablets, capsule, syrup, drink, etc.)

6.  

     6.    Crude botanicals.  Sometimes powdered herbs and fresh herbs or juices are used in studies.  It is important to be sure the following minimum information is provided.

          Plant name(s) (Latin binomials), with authenticating authority

          Plant part(s), with authenticating authority

          Form used (fresh, juice, dried, dried after processing, etc.)

          Dosage form used (capsule, tablet, drink, etc.)

          Method of administration or application (oral, topical, etc.)

          Amount(s) used in study

       

        The above guidelines I have provided are by no means complete.  But at least they can serve as a start.  I am sure some of my esteemed colleagues who are well versed in this field will provide further suggestions and comments.  However, there are several caveats.  Thus, despite all these criteria, an uninformed investigator could always provide a plant name (Latin binomial) even though he/she may have no idea of its authenticity.  Consequently, it is imperative that the authority who authenticated the plant material be identified in the publication.  Also, fundamental problems relating to the influences of growing location, time of harvest, and age of plant at harvest, as well as other geographical and climatic factors, need to be addressed on an ongoing basis until resolution is achieved. 

        I am not the only scientist who sees as a major threat to natural product research, the use of dubious plant materials, which leads to the proliferation of published information that is biased, dubious, and often plain wrong.  As the few examples described in the last issue of this newsletter [Issue 18, pp.1-2] demonstrate, we, as responsible scientists, must take the challenge and responsibility to stop this “cancer” that is growing out of control.  We need to have relevant organizations such as the American Society of Pharmacognosy (ASP) take the lead in refining these guidelines and promoting their adoption by fellow scientists.  ASP should itself encourage its own members to follow them as well as enforcing them in its own publication and publications of its sister organizations.  If we, as a small group of scientists who understand the complexities of natural product research, do not take the lead, the scientific and medical fields would be drowned in quasi-scientific herbal gibberish in 10 years.  Just look at the sudden proliferation of books, journals, magazines, and newsletters on this subject over the past 5 years!  Too much damage has already been done!

 

Anti-fatigue Formulas

        To the general public, “energy” is often synonymous with stimulation of our central nervous system.  Substances that give us “energy” or a “high” include caffeine, ephedrine (in mahuang), synephrine or other amphetamine-type chemicals (in shizhi or immature bitter orange), or a hard drug like cocaine.  These chemicals really don’t give you more stamina or allow you to endure better on the long haul.  On the contrary, prolonged use of these substances as  “energy” sources can lead to very serious deleterious consequences, including irritability, nervousness, hypertension and stroke, among others.  Fortunately, the majority of us don’t go beyond caffeine.

        Currently, most “energy” products sold as dietary supplements are formulated with central stimulants, such as caffeine, ephedrine, synephrine, and N-methyltyramine.  Needless to say, apart from eliciting a temporary sense of “energy,” most of these products offer little or no lasting benefits.  Although they are not meant for long-term use, many consumers do use them on a prolonged basis.  As the herbs (from which these chemicals are derived) have no long history of regular use as foods, teas, and tonics (hence true supplements), this new use has not been time-tested, consequently their long-term toxic side effects are unknown [Issue No. 13, pp. 1-2].

        True energy or anti-fatigue products do exist in the Chinese tradition.  However, they are not widely known to formulators and manufacturers of herbal products in the West.  Nevertheless, in the past 2 years, consumers have gotten a glimpse of Asian ginseng as an “energizer,” despite the fact that only ginsenosides have been primarily used in such “energy” products.  And ginsenosides, like ephedrine, synephrine, and N-methyltyramine, have no traditional safe-use history as central stimulants.  Nevertheless, their use is at least a step in the right direction, as ginsenosides are potentially much less toxic than the amphetamine analogs, because Asian ginseng (from which these ginsenosides are derived) does have a long and safe use history as a tonic.  Unlike mahuang and shizhi, both of which are drugs used only for treating specific conditions, Chinese ginseng has been used for thousands of years as a tonic (or supplement) for disease prevention rather than treatment.  Nevertheless, Asian ginseng is warming and traditionally considered a yang tonic, which is not recommended for people who have a robust constitution, tend to have a ruddy complexion, and are rather active.  Hence, healthy Americans, especially athletes and people who work out, should exercise extreme caution!

        There are many traditional Chinese formulas for improving stamina, increasing energy, or relieving fatigue.  They all contain tonic herbs, some of which are common among these formulas.  The most commonly used herbs in these energy or anti-fatigue formulas include the following: schisandra berry (wuweizi), lycium fruit (gouqizi), astragalus root (huangqi), epimedium herb (yinyanghuo), ophiopogon root (maidong), cured rehmannia (shudihuang), Chinese ginseng root, codonopsis root (dangshen), atractylodes rhizome (baizhu), poria (fuling), licorice root, cordyceps (dongchong xiacao, caterpillar fungus), cured fo-ti (zhiheshouwu), Siberian ginseng, Solomon’s seal rhizome (huangjing), Chinese yam rhizome (shanyao), Cherokee rosehip (jinyingzi), cassia bark (rougui or Chinese cinnamon), white peony root (baishaoyao), etc.  Unlike most of the currently available “energy” products on the American market, these formulas don’t provide you with a fast “high” and then promptly let you down.  Rather, they work subtly and are meant for balancing your system to restore whatever was lacking in you to cause your fatigue or lack of energy in the first place.  Like vitamin and mineral products, they often don’t start working until you have taken them for a number of days or even weeks.  Since they are made up of tonics that by nature don’t elicit single specific effects, these formulas usually exert more than one of the following pharmacological activities, such as immunomodulating, anti-fatigue, antioxidant, hypotensive, anti-atherosclerotic, hepatoprotective, central stimulant, sedative, anti-inflammatory, hypoglycemic, anti-stress, hypolipemic, etc.  It is a combination of some of these effects that bring about a balance in one’s body functions to restore the person to his/her normal “energy” level.  Thus, in the field of true dietary supplements, it is important to formulate products with herbal ingredients that are safe and which can provide true benefits to the consumer.

Leung, A.Y. and S. Foster, Encyclopedia of Common Natural Ingredients Used in Food, Drugs, and Cosmetics, 2nd Ed., Wiley-Interscience, New York, 1996, pp. 50-53, 185-187, 225-227, 250-253, 277-182, 358-361, 435-437, 469-472, 545-547.