A drug used in traditional medicine: Harpagophytum procumbens DC II. Cardiovascular activity

Circosta, Clara; Occhiuto, Francesco; Ragusa, S.; Trovato, A.; Tumino, G; Briguglio, Francesco; Pasquale, A. De

doi:10.1016/0378-8741(84)90072-2

Cited by 45 publications

(28 citation statements)

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Section: Discussionsupporting

confidence: 83%

“…These observations are in agreement with the findings of Circosta et al, (1984), who reported that high doses of dried, crude methanolic extract of Harpagophytum procumbens secondary root caused dose-dependent, significant reductions in the arterial blood pressures of conscious, normotensive rats. With high doses of H. procumbens dried root methanolic extract, Circosta et al,(1984) also observed concomitant decreases in the heart rates of conscious rats. In spontaneously-beating Langendorff preparations of rabbit hearts, Circosta et al, (1984) found that Harpagophytum procumbens dried root crude methanolic extract caused mild decreases in the heart rate with concomitant mild positive inotropic effects at lower doses, but marked negative inotropic effects at higher doses.…”

Section: Discussionsupporting

confidence: 83%

“…In the present study, however, the cardiac effects of harpagoside and harpagide were neither examined nor compared with those of the crude aqueous extract used. Hence, we are unable to comment appropriately on the latter findings of Circosta et al, (1984). It would appear, however, that both harpagoside and harpagide contribute significantly to the inotropic and chronotropic effects of Harpagophytum procumbens dried root extract.…”

Section: Discussionmentioning

confidence: 66%

“…In spontaneously-beating Langendorff preparations of rabbit hearts, Circosta et al, (1984) found that Harpagophytum procumbens dried root crude methanolic extract caused mild decreases in the heart rate with concomitant mild positive inotropic effects at lower doses, but marked negative inotropic effects at higher doses. According to Circosta et al, (1984), the negative chronotropic and positive inotropic effects of harpagoside (the major constituent of Harpagophytum procumbens dried root extract) were comparatively higher with respect to that of the extract, whereas harpagide (another constituent of the plant's root extract) only had a slight negative chronotropic effect and a considerable negative inotropic effect. In the present study, however, the cardiac effects of harpagoside and harpagide were neither examined nor compared with those of the crude aqueous extract used.…”

Section: Discussionmentioning

confidence: 99%

“…Reports on cardiovascular pharmacology of Harpagophytum procumbens DC secondary root extracts are sparse in the literature. Circosta et al, (1984) reported protective effects of crude methanolic extracts of the secondary roots of Harpagophytum procumbens DC in some experimental arrhythmias (induced by aconitine, calcium chloride, chloroform-epinephrine) in rats and rabbits. Similarly, Costa De Pasquale et al, (1985) have investigated the effects of pretreating rats with crude methanolic extracts of Harpagophytum procumbens secondary roots, and with harpagoside, on experimental model of hyperkinetic ventricular arrhythmias (HVA), using Langendorff preparations of rat heart.…”

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confidence: 99%

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Cardiovascular effects of <i>Harpagophytum procumbens</i> dc [Pedaliaceae] secondary root aqueous extract in some mammalian experimental animal models

Mahomed

Ojewole

2004

Afr. J. Trad. Compl. Alt. Med.

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In an attempt to scientifically appraise the 'healing powers' and medicinal value of Harpagophytum procumbens DC root aqueous extract (HPE), and throw some light on the efficacy and safety of the medicinal plant product, the cardiovascular effects of the herb's root aqueous extract (HPE) have been investigated in some mammalian experimental animal models. The results of this laboratory animal study indicate that relatively low to moderate doses of H. procumbens root aqueous extract (HPE, 10-400 mg/kg i. v.) produced dose-dependent hypotensive and cardio-depressant effects on systemic arterial blood pressures and heart rates of pentobarbitone-anaesthetized rats. Relatively low to high concentrations of the plant's extract (HPE, 10-1000 g/ml) also produced concentration-related biphasic responses in isolated cardiac muscle strips of guinea-pigs and isolated portal veins of rats. Relatively low concentrations of the plant's extract (HPE, 10-100 g/ml) always produced initial slight, transient and non-significant (P 0.05) positive chronotropic responses in isolated spontaneouslybeating right atria, but significant (P 0.05) positive inotropic responses in isolated electricallydriven left atria of guinea-pigs. However, moderate to high concentrations of the plant's extract (HPE, 400-1000 g/ml) always induced dose-dependent, significant (P 0.05-0.001), secondary longer-lasting, negative chronotropic and inotropic responses of the isolated spontaneouslybeating right-, and isolated electrically-driven left-, atrial muscle preparations of guinea-pigs. The plant's extract also produced concentration-related biphasic effects on rat isolated portal vein. Low to high concentrations of the plant's extract (HPE, 10-1000 g/ml) always produced dose-dependent, initial slight, transient and significant (P 0.05-0.001) contractions of the rat isolated portal veins, followed by secondary, longer-lasting, significant (P 0.05-0.001) relaxations of the muscle preparations. Although the precise mechanisms of the hypotensive and cardio-depressant actions of HPE are unknown, the vasorelaxant action of the plant's extract is speculated to contribute, at least in part, to the hypotensive action of the plant's extract. The results of this laboratory animal study lend pharmacological credence to the suggested folkloric uses of Harpagophytum procumbens secondary root in the management and/or control of hypertension and certain cardiac disorders in some communities of South Africa.

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Section: Discussionsupporting

confidence: 83%

Section: Discussionsupporting

confidence: 83%

Section: Discussionmentioning

confidence: 66%

Section: Discussionmentioning

confidence: 99%

mentioning

confidence: 99%

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Cardiovascular effects of <i>Harpagophytum procumbens</i> dc [Pedaliaceae] secondary root aqueous extract in some mammalian experimental animal models

Mahomed

Ojewole

2004

Afr. J. Trad. Compl. Alt. Med.

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Investigation of the in vivo metabolism of harpagoside and distribution of its metabolites in rats by HPLC‐IT‐TOF‐MSⁿ

Wang

Zhang

et al. 2018

Biomedical Chromatography

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Harpagoside, an iridoid glycoside, is the major bioactive constituent of the traditional Chinese medicine Scrophulariae Radix. High-performance liquid chromatography with a diode array detector combined with electrospray ionization ion trap time-of-flight multistage mass spectrometry (HPLC-ESI-IT-TOF-MS ) was used to profile and identify the metabolites of harpagoside in rats in vivo and to study the distribution of these metabolites in rats for the first time. A total of 45 metabolites were identified, 37 of which were postulated to be new compounds. The number of detected metabolites in the heart, liver, spleen, lung, kidney, stomach and small intestine was 2, 9, 6, 16, 4, 16 and 6, respectively, which indicated that the target organs of harpagoside should be spleen, lung and stomach. The main types of metabolic reactions of harpagoside in rats are hydrolysis, reduction, sulfuric acid addition, hydroxylation, methoxylation, sulfate substitution, methylation, glucose conjugation and amino acid conjugation. Furthermore, 23 metabolites were determined to have bioactivities based on the literature and 'PharmMapper' analysis. These findings are useful for better comprehension of the effective forms, target organs and pharmacological effects of harpagoside. Moreover, these findings provide a reference for studying the metabolism and distribution of iridoid compounds.

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Synthesis of Stable Genipin Derivatives and Studies of Their Neuroprotective Activity in PC12 Cells

et al. 2012

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Modifications at C1, C7, C8, and C10 of genipin were conducted, and the neurotrophic effects of all derivatives were studied. Genipin derivatives 1-4 were obtained in mild to high yield. Compounds 1 and 4 are more stable than genipin if exposed to nucleophiles. All the derivatives display higher neurotrophic activities than genipin. Compound 4 is the most active, with the least optimal dose. Both genipin and 4 up-regulated the activity of nNOS in PC12 cells. The effect of 4 is inhibited not only by 7-NI, a specific inhibitor of nNOS, but also by L-NIO, a specific inhibitor of eNOS; in the case of genipin, its effect is only inhibited by 7-NI. All the results indicate that 4 is a promising lead compound for the development of new drugs in the treatment of neurodegenerative diseases with the ability to address multiple drug targets.

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A drug used in traditional medicine: Harpagophytum procumbens DC II. Cardiovascular activity

Cited by 45 publications

References 1 publication

Cardiovascular effects of <i>Harpagophytum procumbens</i> dc [Pedaliaceae] secondary root aqueous extract in some mammalian experimental animal models

Cardiovascular effects of <i>Harpagophytum procumbens</i> dc [Pedaliaceae] secondary root aqueous extract in some mammalian experimental animal models

Investigation of the in vivo metabolism of harpagoside and distribution of its metabolites in rats by HPLC‐IT‐TOF‐MSⁿ

Synthesis of Stable Genipin Derivatives and Studies of Their Neuroprotective Activity in PC12 Cells

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A drug used in traditional medicine: Harpagophytum procumbens DC II. Cardiovascular activity

Cited by 45 publications

References 1 publication

Cardiovascular effects of <i>Harpagophytum procumbens</i> dc [Pedaliaceae] secondary root aqueous extract in some mammalian experimental animal models

Cardiovascular effects of <i>Harpagophytum procumbens</i> dc [Pedaliaceae] secondary root aqueous extract in some mammalian experimental animal models

Investigation of the in vivo metabolism of harpagoside and distribution of its metabolites in rats by HPLC‐IT‐TOF‐MSn

Synthesis of Stable Genipin Derivatives and Studies of Their Neuroprotective Activity in PC12 Cells

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Investigation of the in vivo metabolism of harpagoside and distribution of its metabolites in rats by HPLC‐IT‐TOF‐MSⁿ