This document summarizes several herbal medicines and their traditional uses, active ingredients, preparations, and pharmacological effects. It discusses Saint John's Wort, Ginkgo, Valerian, Kava-kava, Cola nut, Guarana, Chamomile, Ma-huang, and Feverfew. For each herb, it provides information on traditional and medicinal uses, how they are prepared and dosed, identified active ingredients, and known pharmacological effects when available. The document also discusses some drug-herb interactions between HIV/AIDS medications and herbs like Saint John's Wort, grapefruit, and garlic.

1. Herbal and traditional
medicines
Dr Liesl Brown
Department of Pharmacy
University of Limpopo
(Medunsa Campus)
Module 4.2: Health Systems
Pharmacy (2011)

2. Saint John’s Wort (Hypericum
perforatum)

3. Saint John’s Wort (Hypericum perforatum)
Preparation and dosage Medicinal uses
• Half cup of boiling water poured • Antidiarroheals
over two teaspoons of coarsely • Rheumatism
powdered drug, -> strained after • Gout
10 min
• Anti-depressant
• Treatment of wounds & 1st degree
Active ingredients burns
• Naphthodianthrone hypericum • Supportive rx of nervous
• Hypericum-like substances excitement + sleep disorders
• Flavanoids (Germany)
– Rutin • Back pain, groin pain, fevers and
– Hyperin rx of wounds (H. aethiopicum)
– Isoquercetrin
– Bioflavonoids Pharmacological effects
– Up to 3% of hyperforin (antibac.)
• Antidepressant (? Linked to MAO
inhibition) ?? Hypericin
• Antiviral activity

4. Ginkgo (Ginkgo biloba)

5. Ginkgo (Ginkgo biloba)
isiphemba, isiqumama (Zulu)
Preparation and dosage Medicinal uses
• Roots are smoked • Dried roots, smoked -> asthma
• ?? Methods of administration relief
• Smoke of whole plant -> nose
bleeding
Active ingredients
• Stem bark (X. spekei) -> general
• Chemical compounds are aches and pains, anti-inflam., post
poorly known partum haemorrhage
• Bioflavonoids have been
reported
Pharmacological effects
• Amento flavone (dimer
ofginkgo extract) • ?? Flavanoids response ->
effects ??
• Dipenteroids
• Capillary fragility
– Cleistanthatetraenes
– Cleistanthateranols • Antispasmodic
• Anti-allergic

6. Valerian (Valeriana officinalis and
Valeriana species)

7. Valerian (Valeriana officinalis and
Valeriana species)
Preparation and dosage Pharmacological effects
• Dried roots/root extracts • Terpenoids & Valepotriates =
GABA-A activity (V. officialis)
-> sedative effects
Active ingredients • Sesquiterpenoids -> sedatives
• Sesquiterpenoids (incl. • Terpenoid & valepotriate ->
valerenic acid & valeranone) spasmolytical activity
• Iridoids (aka valepotriates) • Insomnia
– Forms complex mixtures with
valerate as the main comp. • Symptoms of neurotonic
disorders
Medicinal uses
• Nervous disorders
• Hysteria
• Epilepsy
• Mixed with other plant
materials e.g.. ‘kattekruie’

8. Kava-kava (Piper methysticum)

9. Kava-kava (Piper methysticum)
Ava. Intoxicating Pepper. Ava Pepper
Preparation and dosage Pharmacological effects
• The peeled, dried and divided rhizome • Effect on the nerve centres ->
used stimulating, -> depressing, -> paralysis
• Fluid extract, ½ - 1 drachm. Powdered of the respiratory centre
root, 1 drachm. Solid extract, 1 - 15 • Local anesthetic (relieves pain;
grains aphrodisiac effect)
• The capsules contain 0.3 g; 2-4 caps. • Gonorrhea (acute and chronic),
several times per day vaginitis
• Leucorrhoea, nocturnal incontinence
Active ingredients • other ailments of the genitourinary
• Greenish-yellow resin – kawine tract
(strongly aromatic and acrid) • A 20% oil of Kava resin/oil of
• Kavaine Methysticcum yangonin – Sandalwood (= gonosan) - internally
volatile oil and alkaloid (< active than for gonorrhea
kawine) • Urine antiseptic
• Strong diuretic it is useful for gout,
Medicinal uses rheumatism, bronchial and other
• It resembles pepper in local action ailments, resulting from heart trouble
• Fermented liquor (rhizome - upper
portion) & base of the stems) - narcotic
& stimulant (drunk before important
religious rites)
• The root of the plant chewed & mixed
with the saliva, (->intoxicating juice,
mixed with pure H20/H20 of coco-nut)

10. Cola nut (Dombeya rontundiflora)
inhlizya enkulu (Zulu); motubane (Tswana); mulanga (Venda); mohlabaphala (N. Sotho)

11. Cola nut (Dombeya rontundiflora)
inhlizya enkulu (Zulu); motubane (Tswana); mulanga (Venda); mohlabaphala (N. Sotho)
Preparation and dosage Medicinal uses
• Infusions / deconcotions of the • Internal ulcers -> infusions (orally /
bark (rarely roots) enemas)
– Give: orally / injected enemas • Haemorrhoids
– Sometimes mixed with other • Diarrhoea
ingredients
• Stomach problems
• Powdered root -> burnt and • ?? Nausea – pregnant women
smoke inhaled where after the
powder is used as snuff • When labour is delayed->
• decoctions of bark is given to
Bark is chewed
hasten birth
• Chest complaints
Active ingredients
• No published info. on chemical
Pharmacological effects
composition of Dombeya sp.
• No details about pharmacological
• Other members:
activity
– Purine bases e.g. caffeine

12. Guarana (Ginseng)

13. Guarana (Ginseng) Panax quinquefolium
Aralia quinquefolia. Five Fingers. Tartar Root. Red Berry. Man's Health,
人参 (ninjin = carrot, Japanese)
Preparation and dosage Medicinal uses (cont.)
A decoction of 1/2 oz. of the root, boiled in • Western medicine:
tea or soup and taken every morning – stomachic tonic
– stimulant, useful in loss of appetite
Active ingredients – digestive affections that arise from
• Starch (l/s), gum, some resin, volatile mental and nervous exhaustion
oil (s/s), sweetish body, Panaquilon (= – lower blood glucose
yellow powder, precipitating with water – beneficial effects on immune
a white, amorphous substance – function
Panacon)
Pharmacological effects
Medicinal uses • Adaptogenic effects (e.g. anti-fatigue,
• China: well-being, increase vigor, longevity)
– dyspepsia, vomiting and nervous • Heart & Circulation (e.g. regulate chol.
disorders Level, BP, BG)
• Remedy for consumption and other • Immunity enhancer
diseases • Reproductive fx (e.g. M+F menopause,
impotence)

14. Chamomile

15. Ma-huang (Ephedra)

16. Ma-huang (Ephedra)
Sea ephedrine, ephedra, ephedra alkaloids, sea grape, yellow horse, yellow
astringent, joint fir, squaw tea, Mormon tea, popotillo, teamsters tea
• Reported to cause serious, even fatal, side effects such as heart
attack, stroke, irregular heartbeats, and sudden death, the FDA has
recommended that consumers not take ma huang
• When considering the use of herbal supplements, consultation with
a primary health care professional (trained in the uses of
herbal/health supplements) is advisable
• Ma huang has been used as a stimulant and for weight loss and
appetite suppression
• Ma huang has not been evaluated by the FDA for safety,
effectiveness or purity
• All potential risks and/or advantages of ma huang may not be
known
• No regulated manufacturing standards in place for these
compounds
• Other uses, not listed here

17. Feverfew (Tanacetum parthenium)

18. Feverfew (Tanacetum parthenium)
Pyrethrum Parthenium (Sm.). Featherfew. Featherfoil. Flirtwort
Bachelor's Buttons
Preparation and dosage
• Not be used in children < 2 yrs Medicinal uses
• Fluid extract: dose, 1 – 2 drachms • hysterical complaints, nervousness,
• The cold infusion is made from 1 OZ. lowness of spirits, general tonic,
migraine
of the herb to a pint of boiling water,
cooled, and taken frequently in doses • Coughs, wheezing, asthma and
of half a teacupful (125 ml) difficult breathing (decoction with sugar
• Preparations to contain > 0.2% or honey)
parthenolide • The herb, bruised and heated, or fried
• Dosages are calculated on an average with a little wine and oil, -> warm
external application for wind and colic
of 70 kg adult
• Pain and swelling - bites of insects
and vermin (pain and swelling),
Active ingredients rheumatoid arthritis
• Parthenolide (-> relieves smooth • Distressing sensitiveness to pain (in a
muscle spasms) highly nervous subject)
• Parthenolide (-> inhibits the actions of • Face-ache or earache of a dyspeptic
compounds that cause inflammation) or rheumatic person
Pharmacological effects
• Inflammatory pathways; platelet
aggregation, vascular smooth muscle
contraction, migraine

19. Drug-herb interactions:
-HIV/ARV herb interactions
Indinavir, nevirapine and St John’s Wort
• Saint John’s Wort (SJW) (Rx depression)1
– ?? SJW enhances metabolism of CYP3A4 substrates1
– -> decrease in the plasma level of indinavir and halving its AUC2
– oral clearance of NVP is elevated -> ineffective if taken concurrently with
SJW3
- Induced P-gp expression at low, clinically relevant concentrations may
explain the decreased bioavailability of P-gp substrates (e.g. indinavir)
when co-administrated with SJW
Ioannides, (2002:451-478); 2 (Piscitelli et al., 2000:547); 3 (De Maat et al., 2001:420); 4 Hennessy et al., (2002:75)
1

20. Drug-herb interactions
Interactions between HIV/ART
drugs and grapefruit
• Soldner et al., (1999:478) investigated the role of grapefruit juice (GFJ)
in P-gp mediated drug transport
– ?? GFJ significantly activated P-gp mediated efflux of drugs that
were substrates for P-gp, potentially counteracting its CYP3A4
inhibitory effects
• Romiti et al., (2004) explained that the inhibitory effect of GFJ in the
down regulation of P-gp as well as the inhibition of its functions or
related components in tubular cells could have a role in changing
disposition of some important therapeutic agents

21. Drug-herb interactions
-HIV/ARV herb interactions
Interactions between HIV/ART drugs and garlic
-Foster et al, (2001) found that garlic inhibits cytochrome P450 2C9*1,
2C19, 3A4, 3A5 and 3A7 mediated metabolism of marker substrates
-The activity of CYP2D6 mediated-metabolism was unaffected
-The extracts of garlic exhibited a very low to moderate P-gp
inhibition as compared to the + control VER
-Saquinavir  displayed a 51% drop in its AUC, probably due to
induction of CYP enzymes by garlic supplementation
-Back et al., (2003:S12) warn against the potential interactions of herbs,
including garlic, milk thistle and ginseng
-Conway & Bartlett (2003:61) reported on interactions between both
NVP and NFV with garlic
De Maat et al, 2003:273
1

22. References
DE MAAT, M.M.R., HOETELMANS R.M.W., MATHÔT R.A.A., VAN GORP, E.C.M., MEENTHORST P.L., MULDER J.W. & BEIJNEN J.H.
2001. Drug interactions between St John’s wort and nevirapine. AIDS, 15:420-421.
DE MAAT, M.M.R., EKHART, C.G., HUITEMA, A.D.R., KOKS, C.H.W., MULDER, J.W & BEIJNEN, J.H. 2003. Drug interactions between
ARV drugs and comedicated agents. Clin. Pharmacokinet., 42(3):223-282.
HENNESSY, M., KELLEHER, D., SPIERS, J.P., BARRY, M., KAVANAGH, P., BACK, D., MULCAHY, F AND FEELY, J. 2002. St John’s
Wort increases expression of P-gp: Implications for drug interactions. Brit. J. Clin. Pharmaco., 53:75-82.
IOANNIDES, C. 2002. Pharmacokinetic interactions between herbal remedies and medicinal drugs. Xenobiotica, 32(6):451-478.
KATZUNG, BG. 2001. Basic & Clinical Pharmacology. 9th edition. Lange Medical Books/McGraw-Hill:New York
PISCITELLI S.C., BURSTEIN A.H., CHAITT, D, ALFARO, R.M. & FALLOON J. 2000. Indinavir concentrations and St John’s wort. Lancet,
355:547-548.
VAN WYK B-E, VAN OUTSHOORN, GERICKE N. 1997. Medicinal plants of South Africa, Briza Publications: Pretoria, South Africa
WONG, AHC, SMITH M, BOON HS. Year unknown. Herbal remedies in: Psychiatric practice. Journal of American Medicine. Volume and
edition unknown, pp44-51
INTERNET SOURCES - available at request
http://www.botanical.com/botanical/mgmh/comindxg.html
http://nccam.nih.gov/health/asianginseng/
http://www.eden.rutgers.edu/~piyun/ginseng.htm#Effects
http://www.botanical.com/botanical/mgmh/f/feverf10.html
http://www.umm.edu/altmed/ConsHerbs/Feverfewch.html#Composition
http://www.campbell.edu/faculty/nemecz/George_home/references/Feverfew.html

23. PhD study:
Anti-retroviral drug transport across intestinal
epithelial cells: influence of tuberculosis drugs and
traditional medicines (L Brown, 2007)
HIV/ARV drugs: AZT, NVP
TB drug: rifampicin
Traditional herbal medicines: Sutherlandia frutescens (Cancer Bush), Hypoxis
hemerocallidea ( African Potato)
Active compound of S. frutescens: L-canavanine
P-glycoprotein (efflux drug transporter)

24. Aim
Sutherlandia frutescens
Rifampicin + L-canavanine
(TB drug) Hypoxis hemerocalidea (active of S. frutescens)
(Traditional herbal
medicines)
?
P-gp
Nevirapine
(HIV ARV drug)
Intestinal epithelial cells

25. Conclusions of the NVP experiments
Experimental group P-gp involvement Comments
NVP 1: (alone) √ NVP substrate Influences F of NVP
(effluxed in BL-AP
direction, P < 0.05)
NVP 2: (NVP + VER) Inhibition (effluxed, Increases NVP F
⇓BL-AP, P < 0.05)
NVP 3: (NVP + RIF) Inhibition (effluxed, Increase NVP F
⇓BL-AP, P < 0.05)
NVP 4: (NVP + H. h) Inhibition (effluxed, Increase NVP F
⇓BL-AP, P < 0.05)
NVP 5: (NVP + S. f) Inhibition (effluxed, Increase NVP F
⇓BL-AP, P < 0.05)
NVP 6: (NVP + L- Inhibition (effluxed, Increase NVP F (first
CAV) ⇓BL-AP, P < 0.05) finding documented)