<i>Sutherlandia frutescens</i> limits the development of insulin resistance by decreasing plasma free fatty acid levels

MacKenzie, Janine; Koekemoer, Trevor; Venter, Maryna van de; Dealtry, Gillian B.; Roux, Saartjie

doi:10.1002/ptr.2830

Cited by 20 publications

(14 citation statements)

References 33 publications

(42 reference statements)

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“…It has been investigated for many of the anecdotal claims. Many of such studies have suggested its potential for beneficial effects in HIV/AIDS (Harnett et al, 2005), cancer (Stander et al, 2007(Stander et al, , 2009Skerman et al, 2011), diabetes (Chadwick et al, 2007;Mackenzie et al, 2009Mackenzie et al, , 2012, inflammation (Ojewole, 2004), microbial infection (Katerere and Eloff, 2005), stress (Prevoo et al, 2004), and convulsion (Ojewole, 2008). Commercial twice-daily Sutherlandia capsules containing 300 mg of powdered dried leaves are also available in the herbal medicines shops in South Africa (Van Wyk and Albrecht, 2008).…”

Section: Introductionmentioning

confidence: 99%

The Potential ofSutherlandia frutescensfor Herb-Drug Interaction

et al. 2012

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In Africa, Sutherlandia frutescens is a popular medicinal herb widely consumed by people living with human immunodeficiency virus/ AIDS. Concomitant use with antiretroviral drugs has generated concerns of herb-drug interaction (HDI). This study investigated the inhibitory effects of the crude extracts of S. frutescens on the major cytochrome P450 isozymes with the use of pooled human liver microsomes. Its effect on the metabolic clearance of midazolam using cryopreserved hepatocytes was also monitored. The potential of S. frutescens to inhibit human ATP-binding cassette transporters (P-gp and BCRP) and the human organic anion transporting polypeptide (OATP1B1 and OATP1B3) activity was assessed using cell lines overexpressing the transporter proteins. S. frutescens showed inhibitory potency for CYP1A2 (IC 50 = 41.0 mg/ml), CYP2A6 (IC 50 = 160 mg/ml), CYP2B6 (IC 50 = 20.0 mg/ml), CYP2C8 (IC 50 = 22.4 mg/ml), CYP2C9 (IC 50 = 23.0 mg/ml), CYP2C19 (IC 50 = 35.9 mg/ml), and CYP3A4/5 (IC 50 = 17.5 mg/ml [with midazolam19-hydroxylation]; IC 50 = 28.3 mg/ml [with testosterone 6b-hydroxylation]). Timedependent (irreversible) inhibition by S. frutescens was observed for CYP3A4/5 (K I = 296 mg/ml, k inact = 0.063 min 21) under the conditions of this study. S. frutescens also delays the production of midazolam metabolites in the hepatocytes, decreasing its clearance by 40%. Furthermore, S. frutescens inhibited P-gp (IC 50 = 324.8 mg/ml), OATP1B1 (IC 50 = 10.4 mg/ml), and OATP1B3 (IC 50 = 6.6 mg/ml). The result indicates the potential for HDI between S. frutescens and the substrates of the affected enzymes, if sufficient in vivo concentration of the extract is attained.

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Section: Introductionmentioning

confidence: 99%

The Potential ofSutherlandia frutescensfor Herb-Drug Interaction

et al. 2012

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“…Normalizes glucose uptake in peripheral tissues and regulated 26 genes encoding vesicle transporters, receptors, signaling molecules, transcription factors, metabolic enzymes and modulated fatty acid biosynthesis [129][130][131][132] 91 Swertia punicea Gentianaceae Streptozotocin-induced type 2 diabetic BABL/c mice Improves insulin sensitivity by enhancing insulin signalling. The expression levels of InsR-α, IRS-1 and PI3K were also increased.…”

Section: Stevia Rebaudianamentioning

confidence: 99%

Antidiabetic plants improving insulin sensitivity

Eddouks¹,

Bidi²,

Bouhali³

et al. 2014

Journal of Pharmacy and Pharmacology

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Background Globally, the prevalence of diabetes mellitus is increasing at an alarming rate. This chronic pathology gravely troubled the human health and quality of life. Both insulin deficiency and insulin resistance are involved in the pathophysiology of diabetes mellitus. Moreover, insulin resistance is being diagnosed nowadays in a growing population of diabetic and obese patients, especially in industrialized societies. There are lots of conventional agents available to control and to treat diabetes, but total recovery from this disorder has not been reported up to this date. Plants provided a potential source of hypoglycemic drugs and are widely used in several traditional systems of medicine to prevent diabetes. A few reviews with less attention paid to mechanisms of action have been published on antidiabetic plants. Objectives The present review focuses on the various plants that have been reported to be effective in improving insulin sensitivity associated with diabetes. Key findings In this work, an updated systematic review of the published literature has been conducted to review the antidiabetic plants improving insulin sensitivity and 111 medicinal plants have been reported to have a beneficial effect on insulin sensitivity using several in-vitro and in-vivo animal models of diabetes. Conclusion The different metabolic and cellular effects of the antidiabetic plants improving insulin sensitivity are reported indicating the important role of medicinal plants as potential alternative or complementary use in controlling insulin resistance associated with diabetes mellitus.

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“…() found no indication of toxicological effects after 3 months treatment with 800 mg/day S. frutescens , however, the optimal dosage has yet to be determined. Two studies of high‐fat diet (HFD) induced IR in male Wistar rats were previously conducted, showing that an aqueous extract of S. frutescens restored the blood glucose clearance rate and blood insulin levels to normal (Chadwick et al ., ); and, when the extract was given to rats in conjunction with HFD, prevented the development of IR through lowering the circulating free fatty acids (FFA) (MacKenzie et al ., ). This study now reports the action of S. frutescens in treating established IR in the Wistar rat model and examines its effect on the lipid metabolism.…”

Section: Introductionmentioning

confidence: 97%

“…Their model of diacylglycerol‐induced IR accounts for the IR seen in obese individuals, in young lean offspring of patients with T2DM, as well as in elderly patients. These hypotheses tie in with our previous observation of an early elevation of plasma FFAs in rats after 2 weeks on HFD, preceding the onset of IR (MacKenzie et al ., ). A commercial extract of S. frutescens administered to a parallel group of rats from the start of the HFD regime prevented this rise in FFA levels, and prevented the development of IR (MacKenzie et al ., ).…”

Section: Introductionmentioning

confidence: 97%

“…These hypotheses tie in with our previous observation of an early elevation of plasma FFAs in rats after 2 weeks on HFD, preceding the onset of IR (MacKenzie et al ., ). A commercial extract of S. frutescens administered to a parallel group of rats from the start of the HFD regime prevented this rise in FFA levels, and prevented the development of IR (MacKenzie et al ., ). The present study investigates the effects of the same commercial extract of S. frutescens given as a treatment for IR in rats that were fed HFD for 12 weeks prior to daily administration of S. frutescens for 4 weeks whilst continuing on HFD.…”

Section: Introductionmentioning

confidence: 97%

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Effect of Sutherlandia frutescens on the Lipid Metabolism in an Insulin Resistant Rat Model and 3T3‐L1 Adipocytes

MacKenzie

Koekemoer

Roux

et al. 2012

Phytotherapy Research

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High fat diet induced insulin resistance correlates with dyslipidaemia and ectopic fat deposits in skeletal muscle and liver. The effects of Sutherlandia frutescens, an antidiabetic medicinal plant, on lipid metabolism were evaluated in an insulin resistant (IR) rat model and in 3 T3-preadipocytes. Wistar rats received normal diet (ND) or high fat diet (HFD). After the onset of IR in the HFD group, the rats were subdivided into two subgroups, which either continued with HFD or were treated with 50 mg S. frutescens/kg BW/day and HFD (HFD + SF). After 4 weeks, the HFD + SF rats had a significantly lower body weight than the HFD rats (p < 0.05). Blood plasma analysis showed a decrease in insulin, free fatty acids and triglycerides. Related changes in lipid parameters were observed in the liver, skeletal muscle and adipose tissue. To investigate the effects of S. frutescens on adipose tissue, 3 T3-L1 cells were used as a model. Treatment with S. frutescens led to a decrease in triglyceride accumulation, whilst glucose consumption and lactate production were increased (p < 0.05). These results indicate that S. frutescens directly affects mitochondrial activity and lipid biosynthesis in adipose tissue and provide a mechanism by which S. frutescens can restore insulin sensitivity by modulating fatty acid biosynthesis.

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Sutherlandia frutescens limits the development of insulin resistance by decreasing plasma free fatty acid levels

Cited by 20 publications

References 33 publications

The Potential ofSutherlandia frutescensfor Herb-Drug Interaction

The Potential ofSutherlandia frutescensfor Herb-Drug Interaction

Antidiabetic plants improving insulin sensitivity

Effect of Sutherlandia frutescens on the Lipid Metabolism in an Insulin Resistant Rat Model and 3T3‐L1 Adipocytes

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