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Yohimbine as a Starting Point to Access Diverse Natural Product-Like Agents with Re-programmed Activities against Cancer-Relevant GPCR Targets

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G protein-coupled receptors (GPCRs) constitute the largest protein superfamily in the human genome. GPCRs play key roles in mediating a wide variety of physiological events including proliferation and cancer metastasis. Given the major roles that GPCRs play in mediating cancer growth, they present

Yohimbine ameliorates lipopolysaccharide-induced acute kidney injury in rats.

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Sepsis-induced acute kidney injury (AKI) is frequently observed in the intensive care unit. We previously revealed that yohimbine, an α₂-adrenoceptor antagonist, has protective effects on renal ischemia/reperfusion injury-induced AKI in rats. This study aimed to investigate the

Characterization of alpha 2-adrenergic receptors in the human colon adenocarcinoma cell line HT 29 in culture by [3H]yohimbine binding.

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The presence of specific binding sites for [3H]yohimbine, a labelled alpha 2-adrenergic agent, on crude membranes of HT 29 cells established in culture from a human colon adenocarcinoma, is reported. The estimated affinity and number of sites (KD = 6.3 +/- 0.9 nM; Bmax = 224 +/- 28 fmol/mg protein)

Cytotoxic Effect and Constituent Profile of Alkaloid Fractions from Ethanolic Extract of Ficus septica Burm. f. Leaves on T47D Breast Cancer Cells.

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The study aimed to investigate the profile of alkaloids in two ethyl acetate soluble fractions, namely fractions A and B from an ethanolic extract of Ficus septica leaves and cytotoxic effect on T47D breast cancer cells. Preparation of both fractions involved maceration of leaves with 70% (v/v)

A Tryptoline Ring-Distortion Strategy Leads to Complex and Diverse Biologically Active Molecules from the Indole Alkaloid Yohimbine.

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High-throughput screening (HTS) is the primary driver to current drug-discovery efforts. New therapeutic agents that enter the market are a direct reflection of the structurally simple compounds that make up screening libraries. Unlike medically relevant natural products (e.g., morphine), small

Cytotoxic yohimbine-type alkaloids from the leaves of Rauvolfia vomitoria

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Two new yohimbine-type monoterpene indole alkaloids rauvine A and B ( 1 - 2 ) and six known derivatives ( 3 - 8 ) were obtained from the leaves of R. vomitoria . The structures of the two new alkaloids were determined by extensive spectroscopic analyses, 13 C NMR and ECD calculations. This is the

Effects of alpha-adrenoreceptor antagonists on apoptosis and proliferation of pancreatic cancer cells in vitro.

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OBJECTIVE To discuss the expression of alpha-adrenoreceptors in pancreatic cancer cell lines PC-2 and PC-3 and the effects of alpha1- and alpha2-adrenoreceptor antagonists, yohimbine and urapidil hydrochloride, on the cell lines in vitro. METHODS We cultured the human ductal pancreatic

Reserpine induces apoptosis and cell cycle arrest in hormone independent prostate cancer cells through mitochondrial membrane potential failure.

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Reserpine, an indole alkaloid commonly used for hypertension, is found in the roots of Rauwolfia serpentina. Although the root extract has been used for the treatment of cancer, the molecular mechanism of its anti-cancer activity on hormonal independent prostate cancer remains elusive. Therefore, we

Tramadol inhibits proliferation, migration and invasion via α2-adrenoceptor signaling in breast cancer cells.

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OBJECTIVE The aim of this study was to examine the function of tramadol on cell proliferation, migration and invasion in breast cancer cells in vitro, and to evaluate the effect of tramadol in vivo. Further, we explore the mechanism accounting for the role of tramadol on breast cancer

Quetiapine reverses paclitaxel-induced neuropathic pain in mice: Role of alpha2- adrenergic receptors.

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UNASSIGNED Paclitaxel-induced peripheral neuropathy is a common adverse effect of cancer chemo -therapy. This neuropathy has a profound impact on quality of life and patient's survival. Preventing and treating paclitaxel-induced peripheral neuropathy is a major concern. First- and second-generation

Monoterpene indole alkaloids with diverse skeletons from the stems of Rauvolfia vomitoria and their acetylcholinesterase inhibitory activities

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Nine undescribed monoterpene indole alkaloids, rauvomitorine A-I, including an unprecedented C-9-methoxymethylene-sarpagine framework alkaloid, two rare suaveoline framework type alkaloids, and six yohimbine framework type alkaloids, as well as eleven known alkaloids, were isolated from the stems of

Neurotransmissions of antidepressant-like effects of kisspeptin-13.

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Kisspeptins are G protein-coupled receptor ligands originally identified as human metastasis suppressor gene products that have the ability to suppress melanoma and breast cancer metastasis and which have recently been found to play an important role in initiating the secretion of

Potentials of Mangifera indica in the treatment of depressive-anxiety disorders: possible mechanisms of action.

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BACKGROUND Mangifera indica (Anacardiaceae) is an important herb in the traditional African and Ayurvedic medicines. The stem barks are used in the treatment of hypertension, insomnia, tumour, depression, rheumatism and as a tonic. This study was carried out to investigate antidepressant- and

Current concepts in the treatment of genitourinary tract disorders in the older individual.

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Genitourinary problems, including neurogenic dysfunction, impotence, prostatism, urinary tract infections, and prostate cancer, are common in the elderly, and most of the symptoms can be alleviated through pharmacological management. Patients with neurogenic dysfunction who present with symptoms

A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity.

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With several notable exceptions, interest in the area of multiple molecular forms of phosphodiesterase remained relatively dormant during the decade following Thompson's discovery of more than one phosphodiesterase in brain in 1971. Within the last several years, however, over 20 novel agents have

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