Anticoagulant and anti-inflammatory activity of a triterpene from Protorhus longifolia stem bark

The epidemic of cardiovascular diseases is a global phenomenon that is exaggerated by the growing prevalence of diabetes mellitus. Coronary artery disease and diabetic cardiomyopathy are the major cardiovascular complications responsible for exacerbated myocardial infarction in diabetic individuals. Increasing research has identified hyperglycemia and hyperlipidemia as key factors driving the augmentation of oxidative stress and a pro-inflammatory response that usually results in increased fibrosis and reduced cardiac efficiency. While current antidiabetic agents remain active in attenuating diabetes-associated complications, overtime, their efficacy proves limited in protecting the hearts of diabetic individuals. This has led to a considerable increase in the number of natural products that are screened for their antidiabetic and cardioprotective properties. These natural products may present essential ameliorative properties relevant to their use as a monotherapy or as an adjunct to current drug agents in combating diabetes and its associated cardiovascular complications. Recent findings have suggested that triterpenes isolated from Protorhus longifolia (Benrh.) Engl., a plant species endemic to Southern Africa, display strong antioxidant and antidiabetic properties that may potentially protect against diabetes-induced cardiovascular complications. Thus, in addition to discussing the pathophysiology associated with diabetes-induced cardiovascular injury, available evidence pertaining to the cardiovascular protective potential of lanosteryl triterpenes from Protorhus longifolia will be discussed.

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Lanosteryl triterpenes from Protorhus longifolia as a cardioprotective agent: a mini review

Sangweni

Dludla

Mosa

et al. 2018

Heart Fail Rev

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Antithrombotic, anticoagulant and antiplatelet activity of betulinic acid and 3β-acetoxybetulinic acid from <i>Melaleuca bracteata</i> ‘Revolution Gold’ (Myrtaceae) Muell leaf

Osunsanmi¹,

Zaharare²,

Oyinloye³

et al. 2019

Trop. J. Pharm Res

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Purpose: To investigate the antithrombotic, anticoagulant and antiplatelet activity of betulinic acid (BA) and 3β-acetoxybetulinic acid (BAA) from Melaleuca bracteata 'Revolution Gold'. Methods: Betulinic acid was isolated from the ethyl acetate extract of M. bracteata leaves by column chromatography, from which BAA was subsequently synthesized by acetylation. Structural elucidation of the compounds was conducted using mass spectrometry (MS), infra-red (IR) spectroscopy and nuclear magnetic resonance (NMR). The antithrombotic potential of the compounds was assessed using chromogenic substrate. Anticoagulation studies were carried using bleeding tail time assay in a rat model. Plasma-rich platelets from rats were employed for platelet aggregation studies using light microscope. Results: The compounds significantly (p < 0.05) showed antithrombotic activities in a dose-dependent manner. BAA showed significantly (p < 0.05) higher half-maximal concentration (IC50) value of 1.10 ± 0.03 mg/mL than BA (2.36 ± 0.09 mg/mL) and aspirin (2.65 ± 0.01 mg/mL) which served as positive control. The compounds exhibited anticoagulation activity with poor bleeding time, compared to aspirin. Likewise, the compounds attenuated platelets aggregation induced by thrombin. Conclusion: BAA displays better antithrombotic, antiplatelet, and anticoagulant activities than BA. Therefore, it may be a promising remedy for the management of cardiovascular events.

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Anti-oxidant, anti-inflammatory and antiacetylcholinesterase activity of betulinic acid and 3β- acetoxybetulinic acid from <i>Melaleuca bracteata</i> ‘Revolution Gold’

Osunsanmi¹,

Zharare²,

Mosa³

et al. 2019

Trop. J. Pharm Res

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Purpose: To evaluate the anti-oxidant, anti-inflammatory and anti-acetylcholine esterase activities of betulinic acid (BA) and 3β-acetoxybetulinic acid (BAA) from Melaleuca bracteata. 'Revolution Gold'. Methods: Betulinic acid was isolated from the ethyl acetate extract of M. braceteata while BAA was synthesized by acetylation of BA. Structural elucidation of the compounds was achieved by spectroscopic methods. Antioxidant potential was determined using superoxide dismustase (SOD) and catalase assay kits while iron chelation activity assessed with ferrozin. Anti-inflammatory activity was determined using cotton pellet-induced granuloma rat model. Cyclooxygenase (COX) activity evaluated by COX kits; acetylcholine kit was used for anti-acetylcholinesterase (ACHE) study. Results: The compounds significantly (p < 0.05) dose-dependently inhibited ACHE and inflammatory activity. They also significantly decreased the inhibition of SOD, catalase activity but increased iron chelation activities in a dose-dependent manner. However, BAA showed higher activity than BA for all the parameters. BAA also had a greater inhibitory effect on COX-2 than on COX-1. BAA (IC50, 0.88 mg/mL) showed better iron chelation than citric acid (0.96 ± 0.04) and EDTA (1.04 ± 0.03), the positive control. Conclusion: BA and BAA possess anti-ACHE, anti-inflammatory, antioxidant and anti-COX activities. Structural modification of BAA influences its biological activities. Therefore, BAA can potentially serve as a scaffold in synthesizing potent neurodegeneration drugs.

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Anticoagulant and anti-inflammatory activity of a triterpene from Protorhus longifolia stem bark

Cited by 3 publications

References 31 publications

Lanosteryl triterpenes from Protorhus longifolia as a cardioprotective agent: a mini review

Lanosteryl triterpenes from Protorhus longifolia as a cardioprotective agent: a mini review

Antithrombotic, anticoagulant and antiplatelet activity of betulinic acid and 3β-acetoxybetulinic acid from <i>Melaleuca bracteata</i> ‘Revolution Gold’ (Myrtaceae) Muell leaf

Anti-oxidant, anti-inflammatory and antiacetylcholinesterase activity of betulinic acid and 3β- acetoxybetulinic acid from <i>Melaleuca bracteata</i> ‘Revolution Gold’

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