Comparative investigation of the hypolipidemic properties of triterpenoids

Bioassay-directed fractionation of the cytotoxic antileukemic extracts of Prunella vulgaris, Psychotria serpens, and Hyptis capitata has led to the isolation of ursolic acid as one of the active principles. Ursolic acid showed significant cytotoxicity in the lymphocytic leukemia cells P-388 and L-1210 as well as the human lung carcinoma cell A-549. It also demonstrated marginal cytotoxicity in the KB and the human colon (HCT-8) and mammary (MCF-7) tumor cells. Esterification of the hydroxyl group at C-3 and the carboxyl group at C-17 led to compounds with decreased cytotoxicity in the human tumor cell lines, but with equivalent or slightly increased activity against the growth of L-1210 and P-388 leukemic cells.

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“…antiulcer (17), as well as hypolipidemic (18), and antiartheroscierotic (19) activities despite of its wide occurrence in plant kingdom (20).…”

Section: Resultsmentioning

confidence: 99%

The Cytotoxic Principles ofPrunella vulgaris, Psychotria serpens, andHyptis capitata: Ursolic Acid and Related Derivatives¹

et al. 1988

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“…Therefore, the use of weight reduction drugs, by increasing lipolysis, is usually accompanied by side effects. However, scientific studies have proved that UA could lower blood cholesterol (44%), and β‐lipoprotein levels (50%) in experimental animals 11, 12. Jayaprakasam et al .…”

Section: Discussionmentioning

confidence: 99%

“…Ursolic acid (UA), a natural pentacyclic triterpenoid carboxylic acid, is widely distributed in various plants such as fruits and herbs. Increasing evidence, in vitro and in vivo , suggests that UA has many important biological effects, including anti‐inflammatory 1, 2, anti‐oxidative 3, 4, anti‐mutagenic 5, 6, anti‐carcinogenic 7, hepatoprotective 8, 9, anti‐microbial 10, anti‐atherosclerotic, and anti‐hyperlipidemic effects 11, 12.…”

Section: Introductionmentioning

confidence: 99%

Ursolic acid stimulates lipolysis in primary‐cultured rat adipocytes

Kang

et al. 2010

Molecular Nutrition Food Res

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Ursolic acid (UA) is a pentacyclic triterpenic acid with many biological functions naturally existing in many kinds of food. To investigate whether UA can accelerate lipolysis, primary-cultured rat adipocytes were treated with UA, and glycerol release in the culture medium was measured. UA stimulated lipolysis significantly. Furthermore, the lipolytic effect of UA was inhibited by the protein kinase A (PKA) specific inhibitor H89, suggesting that UA exerted its lipolytic function through the cAMP-dependent PKA pathway. Downstream targets of the PKA pathway, hormone-sensitive lipase (HSL) and perilipin A were checked, UA enhanced lipolysis by promoting the translocation of HSL from the cytosol to the lipid droplets and inhibiting the expression of perilipin A. Additionally, adipose triglyceride lipase (ATGL), a novel rate-limiting lipase in the lipolytic catabolism, was upregulated by UA. UA-induced expression of ATGL could not be blocked by H89, suggesting that ATGL upregulation is not regulated by the PKA pathway. These findings suggest that UA significantly stimulates lipolysis by translocating HSL, decreasing perilipin A expression by the PKA pathway, and up-regulating ATGL in primary cultured adipocytes. Thus, UA is a promising candidate for the treatment of obesity.

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“…The hypolipidemic activity of natural PTs was first reported thirty years ago. 209,210 Since then, more reports have appeared regarding the hypolipidemic activity of natural PTs. Assamicin I (332) and assamicin II (333), which were isolated from the roots of Aesculus assamica, were determined as the active principles responsible for the insulin-like activity of this plant extract tested in in vivo (rat) and in vitro (3T3-L1 adipocytes) assays.…”

Section: In Vitro and In Vivo Evidencementioning

confidence: 99%

Synthesis, biology and clinical significance of pentacyclic triterpenes: a multi-target approach to prevention and treatment of metabolic and vascular diseases

2011

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This review (with 335 references cited) is devoted to pentacyclic triterpenes. The total synthesis, semi-synthesis, structural modification, and metabolic behavior of naturally occurring pentacyclic triterpenes are described. We also cover the in vivo evidence, mechanistic studies, and clinical significance of pentacyclic triterpenes as multi-target therapeutic agents for the prevention and treatment of metabolic and vascular diseases.

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Comparative investigation of the hypolipidemic properties of triterpenoids

Cited by 4 publications

References 2 publications

The Cytotoxic Principles ofPrunella vulgaris, Psychotria serpens, andHyptis capitata: Ursolic Acid and Related Derivatives¹

The Cytotoxic Principles ofPrunella vulgaris, Psychotria serpens, andHyptis capitata: Ursolic Acid and Related Derivatives¹

Ursolic acid stimulates lipolysis in primary‐cultured rat adipocytes

Synthesis, biology and clinical significance of pentacyclic triterpenes: a multi-target approach to prevention and treatment of metabolic and vascular diseases

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Comparative investigation of the hypolipidemic properties of triterpenoids

Cited by 4 publications

References 2 publications

The Cytotoxic Principles ofPrunella vulgaris, Psychotria serpens, andHyptis capitata: Ursolic Acid and Related Derivatives1

The Cytotoxic Principles ofPrunella vulgaris, Psychotria serpens, andHyptis capitata: Ursolic Acid and Related Derivatives1

Ursolic acid stimulates lipolysis in primary‐cultured rat adipocytes

Synthesis, biology and clinical significance of pentacyclic triterpenes: a multi-target approach to prevention and treatment of metabolic and vascular diseases

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The Cytotoxic Principles ofPrunella vulgaris, Psychotria serpens, andHyptis capitata: Ursolic Acid and Related Derivatives¹

The Cytotoxic Principles ofPrunella vulgaris, Psychotria serpens, andHyptis capitata: Ursolic Acid and Related Derivatives¹