Isorhyncophylline

The vine of Uncaria rhynchopylla

Isorhynchophylline (IRN), an alkaloid isolated from Uncaria rhynchophylla, possesses the effects of lowered blood pressure, vasodilatation and protection against ischemia-induced neuronal damage. IC50 value: Target: In vitro: Isorhynchophylline concentration-dependently inhibited the platelet-derived growth factor (PDGF)-BB-induced proliferation of PASMCs. Fluorescence-activated cell-sorting analysis showed that isorhynchophylline caused G0/G1 phase cell cycle arrest [2]. Isorhynchophylline can significantly attenuate the cardiomyocyte hypertrophy induced by AngⅡ [3]. In vivo: Isorhynchophylline significantly improved spatial learning and memory function in the D-gal-treated mice. Isorhynchophylline significantly increased the level of glutathione (GSH) and the activities of superoxide dismutase (SOD) and catalase (CAT), while decreased the level of malondialdehyde (MDA) in the brain tissues of the D-gal-treated mice [1]. Isorhynchophylline prevented monocrotaline induced pulmonary arterial hypertension in rats, as assessed by right ventricular (RV) pressure, the weight ratio of RV to (left ventricular+septum) and RV hypertrophy. Isorhynchophylline significantly attenuated the percentage of fully muscularized small arterioles, the medial wall thickness, and the expression of smooth muscle α-actin (α-SMA) and proliferating cell nuclear antigen (PCNA) [2].

References:
[1]. Yan-Fang Xian, et al. Isorhynchophylline improves learning and memory impairments induced by D-galactose in mice. Neurochemistry International Volume 76, October 2014, Pages 42–49 [2]. Guo H, et al. Isorhynchophylline protects against pulmonary arterial hypertension and suppresses PASMCs proliferation. Biochem Biophys Res Commun. 2014 Jul 18;450(1):729-34. [3]. LI Qiang, et al. Inhibitory effect of isorhynchophylline on cardiomyocyte hypertrophy induced by angiotensinⅡ. West China JOurnal of Pharmaceutical Sciences, 2013-05

Aqueous extracts from Uncaria tomentosa (Willd. ex Schult.) DC. reduce bronchial hyperresponsiveness and inflammation in a murine model of asthma.[Pubmed:29432856]

J Ethnopharmacol. 2018 May 23;218:76-89.

ETHNOPHARMACOLOGICAL RELEVANCE: Uncaria tomentosa (Willd. Ex Schult) DC is used by indigenous tribes in the Amazonian region of Central and South America to treat inflammation, allergies and asthma. The therapeutic properties of U. tomentosa have been attributed to the presence of tetracyclic and pentacyclic oxindole alkaloids and to phenolic acids. AIMS OF THE STUDY: To characterize aqueous bark extracts (ABE) and aqueous leaf extracts (ALE) of U. tomentosa and to compare their anti-inflammatory effects. MATERIALS AND METHODS: Constituents of the extracts were identified by ultra performance liquid chromatography-mass spectrometry. Anti-inflammatory activities were assessed in vitro by exposing lipopolysaccharide-stimulated macrophage cells (RAW264.7-Luc) to ABE, ALE and standard mitraphylline. In vivo assays were performed using a murine model of ovalbumin (OVA)-induced asthma. OVA-sensitized animals were treated with ABE or ALE while controls received dexamethasone or saline solution. Bronchial hyperresponsiveness, production of Th1 and Th2 cytokines, total and differential counts of inflammatory cells in the bronchoalveolar lavage (BAL) and lung tissue were determined. RESULTS: Mitraphylline, isomitraphylline, chlorogenic acid and quinic acid were detected in both extracts, while Isorhyncophylline and rutin were detected only in ALE. ABE, ALE and mitraphylline inhibited the transcription of nuclear factor kappa-B in cell cultures, ALE and mitraphylline reduced the production of interleukin (IL)-6, and mitraphylline reduced production of tumor necrosis factor-alpha. Treatment with ABE and ALE at 50 and 200mgkg(-1), respectively, reduced respiratory elastance and tissue damping and elastance. ABE and ALE reduced the number of eosinophils in BAL, while ALE at 200mgkg(-1) reduced the levels of IL-4 and IL-5 in the lung homogenate. Peribronchial inflammation was significantly reduced by treatment with ABE and ALE at 50 and 100mgkg(-1) respectively. CONCLUSION: The results clarify for the first time the anti-inflammatory activity of U. tomentosa in a murine model of asthma. Although ABE and ALE exhibited distinct chemical compositions, both extracts inhibited the production of pro-inflammatory cytokines in vitro. In vivo assays revealed that ABE was more effective in treating asthmatic inflammation while ALE was more successful in controlling respiratory mechanics. Both extracts may have promising applications in the phytotherapy of allergic asthma.

Isorhynchophylline (IRN), an alkaloid isolated from Uncaria rhynchophylla, possesses the effects of lowered blood pressure, vasodilatation and protection against ischemia-induced neuronal damage.

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