Sutherlandia and HIV/AIDS
Improvements in appetite, weight-gain, sleep, exercise
tolerance, anxiety and overall sense of well-being can be expected.
Researchers anticipate that there will be a delayed progression
of HIV into Aids, and actual remission of the disease is hoped for.
This will require compliance of appropriate does of the correct
selection of Sutherlandia take on an ongoing basis, in addition
to meticulous attention to diet. Alcohol, recreational drugs and
other drugs that damage the immune system should be avoided.
Most wasted patients show an increase in weight
within six weeks of starting treatment. Weight gains of 10-15 kg
have been documented in wasted cancer and AIDS patients. Interestingly
weight-gain is typically not seen in people without underlying wasting
Improvements in CD4 counts and decreases in the
viral load in AIDS patients taking Sutherlandia have been reported
by clinicians in South Africa and Australia. Anecdotal reports that
Sutherlandia can improve the immune status of some people living
with HIV still need to be verified by a controlled clinical trial.
People using Sutherlandia for improving quality of life in HIV should
do so under the supervision of a doctor or healthcare professional
A number of recent published scientific studies on Sutherlandia
have shown interesting results, including anti-HIV activity, anti-oxidant
activity, anti-inflammatory activity, anti-cancer activity, and
also potential drug interaction between Sutherlandia and anti-retroviral
drugs. Summaries of the published studies are included. People living
with HIV should discuss the potential use of Sutherlandia with their
doctor or healthcare professional.
J Ethnopharmacol. 2005 Jan 4;96(1-2):113-9.
Anti-HIV activities of organic and
aqueous extracts of Sutherlandia frutescens and Lobostemon
Harnett SM, Oosthuizen V, van de Venter M.
Department of Biochemistry and Microbiology,
University of Port Elizabeth, PO Box 1600, Port Elizabeth,
6000 South Africa.
A screening process was applied to extracts
made from Sutherlandia frutescens (L.) R. Br (Fabaceae)
and Lobostemon trigonus (Boraginaceae) as identified by the
Botany Department, University of Port Elizabeth to detect
if any of the extracts inhibited the human immunodeficiency
virus (HIV). For purposes of dereplication, sulphated polysaccharides
were removed and bovine serum albumin (BSA) was included in
the assays to adsorb non-specific tannins potentially present.
In the reverse transcriptase (RT) assay, an aqueous extract
of the Lobostemon leaves inhibited HIV-1 RT with an IC50 value
of 49 microg/ml, while in the protease assay no inhibition
was seen. In the alpha- and beta-glucosidase assays, no significant
inhibition was seen with the inclusion of BSA, indicating
tannin-based inhibitory effects on these two enzymes. The
beta-glucuronidase inhibitory activity, however, was retained
in the presence of BSA. The study shows that Sutherlandia
extracts contain inhibitory compounds active against HIV target
enzymes, while aqueous Lobostemon leaf extracts contain a
potent HIV-1 RT inhibitor, thus showing a potential mechanistic
action of these plants in aiding HIV-positive patients.
J Ethnopharmacol. 2004 Nov;95(1):1-5.
The antioxidant potential of Sutherlandia frutescens.
Fernandes AC, Cromarty AD, Albrecht C, van
Department of Pharmacology, Faculty
of Health Sciences, University of Pretoria, PO Box 2034, Pretoria
0001, South Africa.
One of the best-known multi-purpose medicinal
plants in Southern Africa, Sutherlandia frutescens subsp.
microphylla (family: Fabaceae/Leguminosa), is used for a wide
range of conditions, including cancer, viral diseases and
inflammatory conditions. Little scientific data has been documented
on the mechanism by which Sutherlandia frutescens acts on
the immune system. Phagocyte derived reactive oxygen species,
such as hydrogen peroxide and superoxide radicals, are responsible
for the pathogenesis of various inflammatory conditions. Anti-inflammatory
properties of various medicinal-plant extracts have been explained,
at least in part, by their antioxidant activities. We investigated
the effects of a hot water extract of Sutherlandia frutescens
on both luminol and lucigenin enhanced chemiluminescence of
neutrophils stimulated with L-formyl-L-methionyl-L-leucyl-L-phenylalanine
(FMLP) as well as its superoxide and hydrogen peroxide scavenging
properties in a cell free system. The results indicate that
Sutherlandia frutescens extract possesses superoxide as well
as hydrogen peroxide scavenging activities at concentrations
as low as 10 microg/ml, which could account for some of the
anti-inflammatory properties that have been described.
Methods Find Exp Clin Pharmacol.
Analgesic, antiinflammatory and hypoglycemic
effects of Sutherlandia frutescens R. BR. (variety Incana
E. MEY.) [Fabaceae] shoot aqueous extract.
Department of Pharmacology, Faculty of Health
Sciences, University of KwaZulu-Natal, Durban, South Africa.
Previous studies on the pharmacology of
South African medicinal plants in our laboratories and elsewhere
have shown that some plants possess therapeutic attributes.
One such ethnomedically useful plant is Sutherlandia frutescens
R. BR. (family: Fabaceae). S. frutescens is widely used in
South African traditional medicine for the management and/or
control of a plethora of human ailments. In order to scientifically
appraise some of the ethnomedical uses of S. frutescens, the
present study was undertaken to investigate the analgesic,
antiinflammatory and antidiabetic properties of the plant's
shoot aqueous extract in experimental animal models. The analgesic
effect of the herb's shoot extract was evaluated using the
hot-plate and acetic acid test models of pain in mice, while
the antiinflammatory and hypoglycemic effects of the plant's
shoot aqueous extract were investigated in rats, using fresh
egg albumin-induced pedal (paw) edema, and streptozotocin
(STZ)-induced diabetes mellitus. Diclofenac (100 mg/kg) and
chlorpropamide (250 mg/kg) were used, respectively, as reference
drugs for comparison. S. frutescens shoot aqueous extract
(50-800 mg/kg i.p.) produced significant (p < 0.05-0.001)
analgesic effects against thermally- and chemically-induced
nociceptive pain stimuli in mice. The plant extract (50-800
mg/kg p.o. or i.p.) also significantly (p < 0.05-0.001)
inhibited fresh egg albumin-induced acute inflammation and
caused significant (p < 0.05-0.001) hypoglycemia in rats.
The various chemical constituents and secondary metabolites
of the herb are speculated to account for the observed analgesic,
antiinflammatory and hypoglycemic effects of the plant. The
results of this experimental animal study suggest that S.
frutescens shoot aqueous extract possesses analgesic, antiinflammatory,
and hypoglycemic properties, and thus lend pharmacological
credence to the suggested folkloric uses of the herb in the
management and/or control of painful, arthritic and other
inflammatory conditions, as well as for adult-onset, type-2
diabetes mellitus in some communities of South Africa.
Inhibition of phorbol ester-induced
COX-2 expression by some edible African plants.
Na HK, Mossanda KS, Lee JY, Surh YJ.
Laboratory of Biochemistry
and Molecular Toxicology, College of Pharmacy, Seoul National
University, South Korea.
Cancer bush (CB, Sutherlandia frutescens),
Devil's claw (DEV, Harpagophytum procumbens), Rooibos tea
(RT, Aspalathus linearis), and Bambara groundnut (BB, Vignea
subterranean) have been used to treat some malignancies and
inflammatory disorders in Africa. However, biochemical basis
for chemopreventive effects of these medicinal plants remains
unclear. An abnormally elevated expression of cyclooxygenase-2
(COX-2) has been implicated in pathogenesis and progression
of carcinogenesis. In the present study, we found that the
methanol extracts of CB, DEV, RT, and BB inhibited, to a different
extent, 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced
COX-2 expression in human breast epithelial (MCF10A) cells
and in mouse skin in vivo. To determine the molecular mechanism
of COX-2 inhibition by the above medicinal plants, we examined
their effects on activation of NF-kappaB which is one of the
major transcription factors responsible for regulating COX-2
expression. Methanol extracts of both CB and BB inhibited
the DNA binding of NF-kappaB activated by TPA in MCF10A cells
in a dose-dependent manner. Based on above findings, CB and
BB are likely to inhibit TPA-induced COX-2 expression through
suppression of DNA binding of NF-kappaB, which may contribute
to the chemopreventive or chemoprotective activity of these
J Ethnopharmacol. 2005 Apr 8;98(1-2):163-70.
Sutherlandia frutescens extracts
can induce apoptosis in cultured carcinoma cells.
Laboratory of Biochemistry, Department of
Biotechnology, University of the Western Cape, Private Bag
X17, Bellville 7535, Cape Town, South Africa.
Sutherlandia frutescens popularly known
as cancer bush is endemic to Southern Africa. Whole plant
parts have been used and traditional healers claim that it
can treat cancer. In this study it is shown that a crude aqueous
Sutherlandia frutescens whole plant extract induced cytotoxicity
in neoplastic cells (cervical carcinoma) and CHO (Chinese
Hamster Ovary cells) cell lines. Morphological observation
and monitoring with other biological assays involving chromatin
condensation as well as phosphotidyl serine externalisation
point to apoptotic responses. Further biochemical assays showed
similar DNA fragmentation patterns induced by Sutherlandia
frutescens extracts compared to other inducers of apoptosis
such as staurosporine and ceramide. Furthermore, Sutherlandia
frutescens extracts induced apoptosis was confirmed by flow
cytometric analysis. These findings warrant further research
with a view to develop Sutherlandia frutescens extracts for
use in anti-cancer therapy.
Endocr Res. 2004 Nov;30(4):745-51.
The effect of Sutherlandia frutescens
on steroidogenesis: confirming indigenous wisdom.
Prevoo D, Smith C, Swart P, Swart AC.
Department of Biochemistry, University
of Stellenbosch, Stellenbosch, South Africa.
Sutherlandia frutescens (Cancer bush), a
Southern African indigenous plant, is traditionally used to
treat stress related maladies linked to the endocrine system.
Extracts of the shrub were used to investigate the claimed
stress-relieving properties of the shrub. Dysregulation of
the stress response is associated with elevated glucocorticoid
levels. A model of chronic intermittent immobilization stress
was investigated in 40 adult male Wistar rats to determine
the effect of Sutherlandia. Immobilization stress resulted
in increased corticosterone levels in the control group while
rats receiving Sutherlandia extract showed significantly decreased
corticosterone levels (P < 0.005). Since the biosynthesis
of glucocorticoids in the adrenals is catalyzed by the cytochrome
P450-dependent enzymes, the influence of Sutherlandia extracts
on adrenal steroidogenesis was determined in ovine adrenocortical
microsomes and mitochondria, using spectral binding and enzyme
conversion assays. Water extracts showed inhibition of substrate
binding to cytochrome P450 21-hydroxylase (CYP21) by 38% and
cytochrome P450 11beta-hydroxylase (CYP11B1) by 60%. The conversion
of progesterone and pregnenolone was inhibited by 34% and
30%, respectively. Subsequent extractions with chloroform
and methanol showed inhibition of substrate binding and conversion
with hydrophobic compounds exhibiting a greater inhibitory
effect on deoxycorticosterone binding to CYP11B1 (30%) and
on progesterone binding to CYP21 (50%). The inhibition of
binding of pregnenolone to CYP17 by the chloroform extract
was 62%, with negligible inhibition by the methanol extract.
The chloroform extract showed a greater inhibitory effect
than the methanol extract on progesterone and pregnenolone
Cancer Lett. 2005 Jan 31;218(1):21-31.
Inhibitory effects of the extracts
of Sutherlandia frutescens (L.) R. Br. and Harpagophytum procumbens
DC. on phorbol ester-induced COX-2 expression in mouse skin:
AP-1 and CREB as potential upstream targets.
Kundu JK, Mossanda KS, Na HK, Surh YJ.
Laboratory of Biochemistry and Molecular
Toxicology, College of Pharmacy, Seoul National University,
Shinlim-dong, Kwanak-ku, Seoul 151-742, South Korea.
Numerous anti-nflammatory agents have been
shown to exert chemopreventive activity by targeting cyclooxygenase
(COX)-2, a rate-limiting enzyme involved in the inflammatory
process. Sutherlandia frutescens (L.) R. Br. and Harpagophytum
procumbens DC., which are commonly known as Cancer bush (CB)
and Devil's claw (DC), respectively, have long been used in
South Africa for the management of pain and inflammation.
In the present study, we investigated the effects of methanolic
extracts of CB and DC on 12-O-tetradecanoylphorbol-13-acetate
(TPA)-induced COX-2 expression in mouse skin. Topical application
of both extracts inhibited TPA-induced COX-2 expression. As
an underlying mechanism of COX-2 inhibition, these extracts
diminished TPA-stimulated catalytic activity of extracellular
signal-regulated protein kinase (ERK), which is known to regulate
the activation of eukaryotic transcription factors mediating
COX-2 induction. While TPA-induced activation of nuclear factor-kappaB
remained unaffected by both extracts, they inhibited TPA-induced
activation of activator protein-1 (AP-1) and attenuated the
expression of its key component c-Fos. In another study, topical
application of TPA induced DNA binding of cyclic AMP response
element binding (CREB) protein in mouse skin in vivo, which
was abrogated by pretreatment with either CB or DC
AIDS. 2005 Jan 3;19(1):95-97.
Impact of African herbal medicines
on antiretroviral metabolism.
Mills E, Foster BC, Heeswijk RV, Phillips
E, Wilson K, Leonard B, Kosuge K, Kanfer I.
Department of Clinical Epidemiology
and Biostatistics, McMaster University, Hamilton, Ontario,
University of British Columbia, British Columbia Centre for
Excellence in HIV/AIDS, Vancouver, British Columbia, Canada
Division of Infectious Diseases, Ottawa General Hospital,
Ottawa, Ontario, Canada
Department of Medicine, University of Toronto, Toronto, Ontario,
Canadian College of Naturapathic Medicine, Toronto, Ontario,
Faculty of Pharmacy, Rhodes University, Grahamstown, South
We examined the effects of two African herbal
medicines recommended for HIV/AIDS patients on antiretroviral
metabolism. Extracts from Hypoxis and Sutherlandia showed
significant effects on cytochrome P450 3A4 metabolism and
activated the pregnane X receptor approximately twofold. P-glycoprotein
expression was inhibited, with Hypoxis showing 42-51% and
Sutherlandia showing 19-31% of activity compared with verapamil.
Initiating policies to provide herbal medicines with antiretroviral
agents may put patients at risk of treatment failure,
viral resistance or drug toxicity.
J Ethnopharmacol. 2004 Jul;93(1):9-19.
In vitro culture studies of Sutherlandia
frutescens on human tumor cell lines.
Tai J, Cheung S, Chan E, Hasman D.
Departments of Pathology and Pediatrics,
Center for Complementary Medicine Research, BC's Research
Institute for Children's and Women's Health, University of
British Columbia, 4480 Oak Street, Vancouver, BC, Canada V5Z
Sutherlandia frutescens is a South African
herb used traditionally by the natives to treat cancer, and
more recently to improve the overall health in HIV/AIDS patients.
Gas chromatography/mass spectrometer profiling and liquid
chromatographic/mass spectral investigation confirmed and
quantified the presence of canavanine, GABA and arginine in
the herbal preparation used in this study. In vitro study
demonstrated a concentration dependent effect of Sutherlandia
on several tumor cell lines, with 50% inhibition (IC50) of
proliferation of MCF7, MDA-MB-468, Jurkat and HL60 cells at
1/250, 1/200, 1/150 and 1/200 dilutions, respectively. Sutherlandia
treatment did not induce HL60 differentiation along the macrophage/monocyte
or granulocyte lineage. It demonstrated antioxidant activity
in reducing free radical cations with an estimated activity
of 0.5 microl of Sutherlandia extract equivalent to that of
10 microM of Trolox. However, it did not significantly suppress
lipopolysaccharide stimulated nitric oxide production by murine
macrophage/monocyte RAW 264.7 cells, nor did it significantly
inhibit IL-1beta and TNF-alpha mRNA expression in RAW 264.7
cells. In conclusion, Sutherlandia ethanolic extract showed
a concentration dependent antiproliferative effect on several
human tumor cell lines but did not show significant antioxidant
effects. Further studies are needed to explore the activities
of this multipurpose South African herbal preparation.