Hypotensive and cardio-chronotropic constituents of Tinospora crispa and mechanisms of action on the cardiovascular system in anesthetized rats

Praman, Siwaporn; Mulvany, Michael J.; Williams, David E.; Andersen, Raymond J.; Jansakul, Chaweewan

doi:10.1016/j.jep.2012.01.006

Cited by 38 publications

(36 citation statements)

References 29 publications

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“…Our results showed that HG could decrease the blood pressure in normal and spontaneous hypertension rats. We observed a similar phenomenon regarding the hypotensive effect of HG in a study conducted by Praman and his colleagues (Praman, Mulvany, Williams, Andersen, & Jansakul, ). Even though HG could increase the beats per minute, it showed limited effect on the blood pressure.…”

Section: Discussionsupporting

confidence: 84%

Identification of higenamine as a novel α₁‐adrenergic receptor antagonist

Zhang

Wang

et al. 2019

Phytotherapy Research

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The α1‐adrenoceptor (α1‐AR) antagonists are potential candidates for the treatment of blood pressure. Higenamine (HG) is a novel α1‐AR antagonist. In this study, we investigated the effects of HG in HEK293A cells transfected with α1A‐, α1B‐, and α1D‐AR in vitro, rat mesenteric artery ex vivo, Wistar–Kyoto rats and spontaneously hypertensive rats in vivo. The radioligand binding assay showed that HG competitively inhibited the binding of [3H]‐prazosin to α1‐AR in a concentration‐dependent manner. The affinities (pKi) of HG for the cloned α1A‐, α1B‐, and α1D‐AR were 6.57, 6.48, and 6.35, respectively, indicating that HG displayed no selectivity for the three α1‐AR subtypes. In in vitro studies, HG was able to blunt inositol monophosphate production. It also displayed an inhibitory effect on the influx and entry of calcium ions and phosphorylation of extracellular signal‐regulated kinase 1 and 2 induced by phenylephrine (PE). In ex vivo studies, PE caused a dose‐dependent inotropic response curve, and the pA2 value for HG was 6.86 ± 0.29. In addition, the in vivo results showed that HG could decrease the blood pressure in normotension, spontaneous hypertension, and PE‐induced hypertension models. These results indicate that HG can directly bind to α1‐AR and it appears to be a novel antagonist for α1‐AR, which may contribute to its hypotensive effect.

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Section: Discussionsupporting

confidence: 84%

Identification of higenamine as a novel α₁‐adrenergic receptor antagonist

Zhang

Wang

et al. 2019

Phytotherapy Research

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“…One possible explanation for the consistency of higenamine in increasing heart rate in humans and various other models is its lack of a presser effect. Higenamine has been reported to decrease mean arterial pressure in rats (Praman et al, 2012). Thus there is no hypertensive response to higenamine, and baroreceptor reflexes are not stimulated to reduce the heart rate as can occur with PEA.…”

Section: Discussionmentioning

confidence: 94%

“…First, published data suggest they may enhance heart rate. Higenamine and PEA both have been documented to increase heart rate with in vivo experiments (Dunlop and Shanks, 1969;Feng et al, 2012;Liang and Sprecher, 1979;Praman et al, 2012). Ephedrine is known to increase heart rate, and was banned in 2004 because it was associated with deaths and severe cardiac adverse events.…”

Section: Introductionmentioning

confidence: 99%

A beating heart cell model to predict cardiotoxicity: Effects of the dietary supplement ingredients higenamine, phenylethylamine, ephedrine and caffeine

Calvert

Vohra

Ferguson

et al. 2015

Food and Chemical Toxicology

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“…Borapetoside C, isolated from T. crispa , improved insulin sensitivity in diabetic mice [51]. Praman et al isolated five compounds (uridine, adenosine, higenamine, salsolinol, and tyramine) from T. crispa and proved the effects of these compounds on the cardiovascular system, particularly on the reduction of blood pressure [52]. …”

Section: Discussionmentioning

confidence: 99%

Immunomodulatory effect of an isolated fraction from Tinospora crispa on intracellular expression of INF-γ, IL-6 and IL-8

Abood

Fahmi

Abdulla

et al. 2014

BMC Complement Altern Med

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BackgroundImmunomodulators are substances that modify immune system response to a threat. Immunomodulators modulate and potentiate the immune system, keeping it highly prepared for any threat. The immunomodulatory effect of the traditional medicine Tinospora crispa is investigated in this work.MethodsT. crispa ethanol extract was fractionated by using different solvents. The ethanol extract and effective isolated fraction were used to investigate the potential immunomodulatory effect of different T. crispa doses ranging from 25 μg/mL to 1000 μg/mL on RAW 246.7 cells by detecting intracellular INF-γ, IL-6, and IL-8 expressions. The antioxidant activity of T. crispa was evaluated through FRAP and DPPH. The total phenolic and total flavonoid contents were also quantified.ResultsResults show that T. crispa extract has higher antioxidant potential than ascorbic acid. The FRAP value of T. crispa extract is 11011.11 ± 1145.42 μmol Fe+2/g, and its DPPH inhibition percentage is 55.79 ± 7.9, with 22 μg/mL IC50. The results also reveal that the total phenolic content of T. crispa extract is 213.16- ± 1.31 mg GAE/g dry stem weight, and the total flavonoid content is 62.07- ± 39.76 mg QE/g dry stem weight. T. crispa crude extract and its isolated fraction significantly stimulate RAW264.7 cell viability (P ≤ 0.05) and intracellular INF-γ, IL-6, and IL-8 expressions. The results of LC-MS show that four of the active compounds detected in the T. crispa isolated fraction are cordioside, quercetin, eicosenoic acid (paullinic acid), and boldine.ConclusionsThe results of this study obviously indicate that T. crispa has immunomodulatory effects through the stimulation of INF-γ, IL-6, and IL-8 expressions. LC-MS phytochemical analysis showed that the T. crispa fraction has cordioside, quercetin, eicosenoic acid (paullinic acid), and boldine, which may be responsible for the immunostimulator effect of T. crispa.

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Hypotensive and cardio-chronotropic constituents of Tinospora crispa and mechanisms of action on the cardiovascular system in anesthetized rats

Cited by 38 publications

References 29 publications

Identification of higenamine as a novel α₁‐adrenergic receptor antagonist

Identification of higenamine as a novel α₁‐adrenergic receptor antagonist

A beating heart cell model to predict cardiotoxicity: Effects of the dietary supplement ingredients higenamine, phenylethylamine, ephedrine and caffeine

Immunomodulatory effect of an isolated fraction from Tinospora crispa on intracellular expression of INF-γ, IL-6 and IL-8

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Hypotensive and cardio-chronotropic constituents of Tinospora crispa and mechanisms of action on the cardiovascular system in anesthetized rats

Cited by 38 publications

References 29 publications

Identification of higenamine as a novel α1‐adrenergic receptor antagonist

Identification of higenamine as a novel α1‐adrenergic receptor antagonist

A beating heart cell model to predict cardiotoxicity: Effects of the dietary supplement ingredients higenamine, phenylethylamine, ephedrine and caffeine

Immunomodulatory effect of an isolated fraction from Tinospora crispa on intracellular expression of INF-γ, IL-6 and IL-8

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Product

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Identification of higenamine as a novel α₁‐adrenergic receptor antagonist

Identification of higenamine as a novel α₁‐adrenergic receptor antagonist