LNS8801: An enantiomerically pure agonist of the G protein-coupled estrogen receptor suitable for clinical development.

Estrogen effects in tissue are mediated in part through activation of the surface estrogen receptor GPER, a broadly expressed G protein-coupled receptor that impacts a wide range of normal and pathologic processes, including metabolism, vascular health, inflammation, and cancer. A commonly used synthetic and specific GPER agonist, named G-1, antagonizes tumors by promoting cellular differentiation and enhancing tumor immunogenicity. G-1 is a racemic compound, and since its discovery, the question of whether both enantiomers display agonist activity or the agonist activity resides primarily in a single enantiomer has never been fully resolved.

12-(S)-Hydroxyeicosatetraenoic Acid and GPR31 Signaling in Spinal Cord in Neuropathic Pain.

Neuropathic pain is a pressing unmet medical need requiring novel nonopioid-based therapeutic approaches. Using unbiased transcriptomic analysis, we found that the expression of , a G protein-coupled receptor, increased in the dorsal horn of the spinal cord in rats with traumatic nerve injury-induced neuropathic pain. Daily intrathecal injections of si reversed behavioral hypersensitivities in a time-dependent manner.

Antioxidant activities of peptide hydrolysates obtained from the seeds of Decne (African breadfruit).

Protein hydrolysates usually possess higher nutritive value than an equivalent mixture of free amino acids. This study was aimed at determining the antioxidant activities of protein hydrolysates of seeds. Soluble protein was isolated from seed flour by alkaline solubilization and acid precipitation, and further hydrolyzed with three proteases (trypsin, pancreatin and pepsin) individually and in a sequential two- and three-protease systems.

In vitro antioxidant and enzyme inhibitory properties of the n-butanol fraction of Senna podocarpa (Guill. and Perr.) leaf.

Background This study evaluates the antioxidant activity and enzyme inhibitory properties of the n-butanol fraction of Senna podocarpa leaves on α-amylase, α-glucosidase, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, arginase, phosphodiesterase 5 (PDE-5), and angiotensin converting enzyme (ACE). Methods The total phenol and flavonoids, iron (Fe) chelation, and 2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) free radical scavenging were used to determine the antioxidant activity, and the inhibitory activities of α-glucosidase, α-amylase, AChE, BChE, tyrosinase, arginase, PDE-5 and ACE were also assessed. Results The n-butanol fraction of S.

Nephroprotective Effect of Essential Oils from Ginger (Zingiber officinale) and Turmeric (Curcuma longa) Rhizomes against Cadmium-induced Nephrotoxicity in Rats.

Several studies have shown that cadmium (Cd) induces nephrotoxicity and many plant foods phytochemicals have been found useful but their possible mechanism of action still remains unexplored. Hence, this study aimed to investigate the nephroprotective effect of essential oils from Nigeria ginger and turmeric rhizomes in cadmium-treated rats by examining their effect on renal function biomarkers (creatinine, urea and BUN), inflammatory cytokines (IL-6, IL-10 and TNF-Alpha) and renal adenosine deaminase (ADA) activity. The result revealed that essential oils from ginger and turmeric rhizomes exert anti-inflammatory effect by preventing alterations of renal function markers and cytokines (IL-6, IL-10 and TNF-Alpha) levels in Cd-treated rats.

Aqueous extract of Linn. roots potentially attenuates arsenic induced biochemical and genotoxic effects in Wistar rats.

In Africa, the fruit, leaf, seed and roots of Linn. are generally used to treat a variety of diseases such as malaria, cancer, and cardiovascular diseases. In this study, we evaluated the protective potentials of aqueous extract of roots on arsenic-induced biochemical and genotoxic effects in Wistar rats.

Curcumin inhibits adenosine deaminase and arginase activities in cadmium-induced renal toxicity in rat kidney.

In this study, the effect of enzymes involved in degradation of renal adenosine and l-arginine was investigated in rats exposed to cadmium (Cd) and treated with curcumin, the principal active phytochemical in turmeric rhizome. Animals were divided into six groups (n = 6): saline/vehicle, saline/curcumin 12.5 mg/kg, saline/curcumin 25 mg/kg, Cd/vehicle, Cd/curcumin 12.

Effect of Cadmium Stress on Non-enzymatic Antioxidant and Nitric Oxide Levels in Two Varieties of Maize (Zea mays).

Cadmium (Cd) is one of the most toxic heavy metals that inhibit physiological processes of plants. Hence, the present study sought to investigate the effect of cadmium-contaminated seeds from two varieties of maize (Zea mays) on non-enzymatic antioxidant and nitric oxide levels. Seeds of yellow and white maize were exposed to different concentrations of Cd (0, 1, 3 and 5 ppm) for two weeks.

Curcumin improves episodic memory in cadmium induced memory impairment through inhibition of acetylcholinesterase and adenosine deaminase activities in a rat model.

Curcumin, the main polyphenolic component of turmeric (Curcuma longa) rhizomes has been reported to exert cognitive enhancing potential with limited scientific basis. Hence, this study sought to evaluate the effect of curcumin on cerebral cortex acetylcholinesterase (AChE) and adenosine deaminase (ADA) activities in cadmium (Cd)-induced memory impairment in rats. Animals were divided into six groups (n = 6): saline/vehicle, saline/curcumin 12.

Evaluation of acute and subacute toxicity of aqueous extract of Crassocephalum rubens leaves in rats.

Ethnopharmacological Relevance: Crassocephalum rubens is found throughout tropical Africa including the Indian Ocean islands. The leaves are commonly eaten in form of soups and sauces in South-Western Nigeria, also in other humid zones of Africa. Traditionally, it is used as an antidote against any form of poisoning; used to treat stomach and liver complaints; and externally to treat burns, sore eyes, earache, leprosy and breast cancer.