Pharmacological Activity

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Pilar M Gomezserranillos - One of the best experts on this subject based on the ideXlab platform.

  • the Pharmacological Activity of camellia sinensis l kuntze on metabolic and endocrine disorders a systematic review
    Biomolecules, 2020
    Co-Authors: Marta Gutierrez Sanchez, Elena Gonzalezburgos, I Iglesias, Rafael Lozano, Pilar M Gomezserranillos
    Abstract:

    Tea made from Camellia sinensis leaves is one of the most consumed beverages worldwide. This systematic review aims to update Camellia sinensis Pharmacological Activity on metabolic and endocrine disorders. Inclusion criteria were preclinical and clinical studies of tea extracts and isolated compounds on osteoporosis, hypertension, diabetes, metabolic syndrome, hypercholesterolemia, and obesity written in English between 2014 and 2019 and published in Pubmed, Science Direct, and Scopus. From a total of 1384 studies, 80 reports met inclusion criteria. Most papers were published in 2015 (29.3%) and 2017 (20.6%), conducted in China (28.75%), US (12.5%), and South Korea (10%) and carried out with extracts (67.5%, especially green tea) and isolated compounds (41.25%, especially epigallocatechin gallate). Most Pharmacological studies were in vitro and in vivo studies focused on diabetes and obesity. Clinical trials, although they have demonstrated promising results, are very limited. Future research should be aimed at providing more clinical evidence on less studied pathologies such as osteoporosis, hypertension, and metabolic syndrome. Given the close relationship among all endocrine disorders, it would be of interest to find a standard dose of tea or their bioactive constituents that would be beneficial for all of them.

Jean Michel Scherrmann - One of the best experts on this subject based on the ideXlab platform.

  • Improved Brain Uptake and Pharmacological Activity Profile of Morphine-6-Glucuronide Using a Peptide Vector-Mediated Strategy
    Journal of Pharmacology and Experimental Therapeutics, 2005
    Co-Authors: Jamal Temsamani, Cécile Bonnafous, Christophe Rousselle, Yannik Fraisse, Philippe Clair, Luc-andré Granier, Anthony R. Rees, Michel Kaczorek, Jean Michel Scherrmann
    Abstract:

    Morphine-6-glucuronide (M6G), an active metabolite of morphine, has been shown to have significantly attenuated brain penetration relative to that of morphine. Recently, we have demonstrated that conjugation of various drugs to peptide vectors significantly enhances their brain uptake. In this study, we have conjugated morphine-6-glucuronide to a peptide vector SynB3 to enhance its brain uptake and its analgesic potency after systemic administration. We show by in situ brain perfusion that vectorization of M6G (Syn1001) markedly enhances the brain uptake of M6G. This enhancement results in a significant improvement in the Pharmacological Activity of M6G in several models of nociception. Syn1001 was about 4 times more potent than free M6G (ED 50 of 1.87 versus 8.74 μmol/kg). Syn1001 showed also a prolonged duration of action compared with free M6G (300 and 120 min, respectively). Furthermore, the conjugation of M6G results in a lowered respiratory depression, as measured in a rat model. Taken together, these data strongly support the utility of peptide-mediated strategies for improving the efficacy of drugs such as M6G for the treatment of pain.

Yoshio Kagitani - One of the best experts on this subject based on the ideXlab platform.

  • Synthesis and Pharmacological Activity of triazole derivatives inhibiting eosinophilia.
    Journal of Medicinal Chemistry, 1996
    Co-Authors: Youichiro Naito, Fumihiko Akahoshi, Shinji Takeda, Takehiro Okada, Masahiko Kajii, Hiroko Nishimura, Masanori Sugiura, Chikara Fukaya, Yoshio Kagitani
    Abstract:

    In order to develop novel antiasthmatic agents based on a new mechanism of action, a series of 3-substituted 5-amino-1-[(methylamino)(thiocarbonyl)]-1H-1,2,4-triazole derivatives were synthesized and evaluated in a model in which eosinophilia was induced in the airway through intravenous (iv) injection of Sephadex particles on days 0, 2, and 5. After screening of several hundred derivatives, we finally identified the highly potent eosinophilia inhibitor 5-amino-3-(4-chlorophenyl)-1-[(methylamino)(thiocarbonyl)]-1H-triazole (23c, GCC-AP0341), which had ID50 values of 0.3 and 0.07 mg/kg when administered orally (os) and intraperitoneally (ip), respectively. This compound showed complete inhibition of the hypersensitivity induced by ascaris inhalation at an ip dose of 1 mg/kg as well as low toxicity, with an LD50 value of >2.0 g/kg in mice. Extensive study of its mechanism of action revealed that 23c inhibited eosinophil survival induced by interleukin-5 (IL-5), but had little or no effect on leukotriene D4 ...

Marta Gutierrez Sanchez - One of the best experts on this subject based on the ideXlab platform.

  • the Pharmacological Activity of camellia sinensis l kuntze on metabolic and endocrine disorders a systematic review
    Biomolecules, 2020
    Co-Authors: Marta Gutierrez Sanchez, Elena Gonzalezburgos, I Iglesias, Rafael Lozano, Pilar M Gomezserranillos
    Abstract:

    Tea made from Camellia sinensis leaves is one of the most consumed beverages worldwide. This systematic review aims to update Camellia sinensis Pharmacological Activity on metabolic and endocrine disorders. Inclusion criteria were preclinical and clinical studies of tea extracts and isolated compounds on osteoporosis, hypertension, diabetes, metabolic syndrome, hypercholesterolemia, and obesity written in English between 2014 and 2019 and published in Pubmed, Science Direct, and Scopus. From a total of 1384 studies, 80 reports met inclusion criteria. Most papers were published in 2015 (29.3%) and 2017 (20.6%), conducted in China (28.75%), US (12.5%), and South Korea (10%) and carried out with extracts (67.5%, especially green tea) and isolated compounds (41.25%, especially epigallocatechin gallate). Most Pharmacological studies were in vitro and in vivo studies focused on diabetes and obesity. Clinical trials, although they have demonstrated promising results, are very limited. Future research should be aimed at providing more clinical evidence on less studied pathologies such as osteoporosis, hypertension, and metabolic syndrome. Given the close relationship among all endocrine disorders, it would be of interest to find a standard dose of tea or their bioactive constituents that would be beneficial for all of them.

Hafiz Muhammad Asif - One of the best experts on this subject based on the ideXlab platform.

  • Pharmacological Activity of althaea officinalis l
    Journal of Medicinal Plants Research, 2011
    Co-Authors: S Ali M Shah, Khalil Ahmed, Muhammad Akram, Naveed Akhtar, Pervaiz Akhtar Shah, Tariq Saeed, Hafiz Muhammad Asif
    Abstract:

    Althaea officinalis belongs to family Malvaceae. It is one of the medicinal plants used therapeutically since ancient time. The leaves of the A. officinalis plant as well as the root are used as medicine. Roots of A. officinalis contain mucilage, flavonoids and glycosides, additionally the leaves contain the coumarin scopoletin. Due to having valuable secondary metabolites it exert potential therapeutic effect. In vitro and in vivo study of A. officinalisindicates significant Pharmacological Activity in the cough, irritation of the throat, gastric inflammation, anti-tumor, antiviral and immunostimulant. Anti-bacterial and anti-inflammatory activities, effects on mucociliary transport, adhesion of polysaccharide to buccal membranes and reduction of cough are reported.   Key words: Pharmacological Activity, Althaea officinalis, pectin.

  • ISSN 1996-0875 ©2011 Academic Journals Review Pharmacological Activity of Althaea officinalis L.
    2011
    Co-Authors: S Ali M Shah, Khalil Ahmed, Muhammad Akram, Naveed Akhtar, Pervaiz Akhtar Shah, Tariq Saeed, Hafiz Muhammad Asif
    Abstract:

    Althaea officinalis belongs to family Malvaceae. It is one of the medicinal plants used therapeutically since ancient time. The leaves of the A. officinalis plant as well as the root are used as medicine. Roots of A. officinalis contain mucilage, flavonoids and glycosides, additionally the leaves contain the coumarin scopoletin. Due to having valuable secondary metabolites it exert potential therapeutic effect. In vitro and in vivo study of A. officinalis indicates significant Pharmacological Activity in the cough, irritation of the throat, gastric inflammation, anti-tumor, antiviral and immunostimulant. Anti-bacterial and anti-inflammatory activities, effects on mucociliary transport, adhesion of polysaccharide to buccal membranes and reduction of cough are reported