Herbal and traditional herbal medication

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)