CL 284,846, a novel sedative-hypnotic: Evaluation of its metabolites for pharmacological activity in vitro and in vivo

1994 ◽  
Vol 33 (1) ◽  
pp. 39-45 ◽  
Author(s):  
Kimberly E. Vanover ◽  
Richard M. Mangano ◽  
James E. Barrett
Keyword(s):  
Pharmacological Activity ◽  
Cl 284,846

scholarly journals Evaluation of In vitro Antioxidant and In vivo Pharmacological Activity of Leaf Extracts of Hoya parasitica (Wall.)

2016 ◽  
pp. 163-170
Author(s):  
Ummee Tania ◽  
Md Hassan ◽  
Nusrat Eshita ◽  
Rumana Akhter ◽  
Mohammad Shahriar
Keyword(s):  
Pharmacological Activity ◽  
Leaf Extracts

scholarly journals Pharmacological Activity of Retinoic Acid Receptor Alpha-Selective Antagonists in Vitro and in Vivo

2013 ◽  
Vol 4 (5) ◽  
pp. 446-450 ◽  
Author(s):  
Sanny S. W. Chung ◽  
Rebecca A. D. Cuellar ◽  
Xiangyuan Wang ◽  
Peter R. Reczek ◽  
Gunda I. Georg ◽  
...  
Keyword(s):  
Retinoic Acid ◽  
Pharmacological Activity ◽  
Retinoic Acid Receptor ◽  
Retinoic Acid Receptor Alpha ◽  
Acid Receptor ◽  
Receptor Alpha ◽  
Selective Antagonists

scholarly journals High Accumulation and In Vivo Recycling of the New Antimalarial Albitiazolium Lead to Rapid Parasite Death

2017 ◽  
Vol 61 (8) ◽  
Author(s):  
Sharon Wein ◽  
Nicolas Taudon ◽  
Marjorie Maynadier ◽  
Christophe Tran Van Ba ◽  
Delphine Margout ◽  
...  
Keyword(s):  
Pharmacological Activity ◽  
Plasma Concentrations ◽  
Pharmacokinetic Studies ◽  
High Accumulation ◽  
Content Type ◽  
Viability Assay ◽  
Parasite Viability ◽  
Two Parameters

ABSTRACT Albitiazolium is the lead compound of bisthiazolium choline analogues and exerts powerful in vitro and in vivo antimalarial activities. Here we provide new insight into the fate of albitiazolium in vivo in mice and how it exerts its pharmacological activity. We show that the drug exhibits rapid and potent activity and has very favorable pharmacokinetic and pharmacodynamic properties. Pharmacokinetic studies in Plasmodium vinckei-infected mice indicated that albitiazolium rapidly and specifically accumulates to a great extent (cellular accumulation ratio, >150) in infected erythrocytes. Unexpectedly, plasma concentrations and the area under concentration-time curves increased by 15% and 69% when mice were infected at 0.9% and 8.9% parasitemia, respectively. Albitiazolium that had accumulated in infected erythrocytes and in the spleen was released into the plasma, where it was then available for another round of pharmacological activity. This recycling of the accumulated drug, after the rupture of the infected erythrocytes, likely extends its pharmacological effect. We also established a new viability assay in the P. vinckei-infected mouse model to discriminate between fast- and slow-acting antimalarials. We found that albitiazolium impaired parasite viability in less than 6 and 3 h at the ring and late stages, respectively, while parasite morphology was affected more belatedly. This highlights that viability and morphology are two parameters that can be differentially affected by a drug treatment, an element that should be taken into account when screening new antimalarial drugs.

scholarly journals Pharmacological Activity of Garcinia indica (Kokum): An Updated Review

2021 ◽  
Vol 14 (12) ◽  
pp. 1338
Author(s):  
Sung Ho Lim ◽  
Ho Seon Lee ◽  
Chang Hoon Lee ◽  
Chang-Ik Choi
Keyword(s):  
Traditional Medicine ◽  
Pharmacological Activity ◽  
Therapeutic Agent ◽  
Industrial Applications ◽  
Pharmacological Activities ◽  
Garcinia Indica ◽  
Hydroxycitric Acid ◽  
Promising Therapeutic Agent

Garcinia indica (commonly known as kokum), belonging to the Clusiaceae family (mangosteen family), is a tropical evergreen tree distributed in certain regions of India. It has been used in culinary and industrial applications for a variety of purposes, including acidulant in curries, pickles, health drinks, wine, and butter. In particular, G. indica has been used in traditional medicine to treat inflammation, dermatitis, and diarrhea, and to promote digestion. According to several studies, various phytochemicals such as garcinol, hydroxycitric acid (HCA), cyanidin-3-sambubioside, and cyanidin-3-glucoside were isolated from G. indica, and their pharmacological activities were published. This review highlights recent updates on the various pharmacological activities of G. indica. These studies reported that G. indica has antioxidant, anti-obesity, anti-arthritic, anti-inflammatory, antibacterial, hepatoprotective, cardioprotective, antidepressant and anxiolytic effects both in vitro and in vivo. These findings, together with previously published reports of pharmacological activity of various components isolated from G. indica, suggest its potential as a promising therapeutic agent to prevent various diseases.

scholarly journals An Insight into Sesamolin: Physicochemical Properties, Pharmacological Activities, and Future Research Prospects

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 5849
Author(s):  
Reny Rosalina ◽  
Natthida Weerapreeyakul
Keyword(s):  
Physicochemical Properties ◽  
Pharmacological Activity ◽  
Human Colon ◽  
Cytolytic Activity ◽  
Neuroprotective Activity ◽  
Future Research ◽  
Pharmacological Activities ◽  
Human Colon Cancer

Sesame seeds are rich in lignan content and have been well-known for their health benefits. Unlike the other sesame lignan compounds (i.e., sesamin and sesamol), the study of the pharmacological activity of sesamolin has not been explored widely. This review, therefore, summarizes the information related to sesamolin’s pharmacological activities, and the mechanism of action. Moreover, the influence of its physicochemical properties on pharmacological activity is also discussed. Sesamolin possessed neuroprotective activity against hypoxia-induced reactive oxygen species (ROS) and oxidative stress in neuron cells by reducing the ROS and inhibiting apoptosis. In skin cancer, sesamolin exhibited antimelanogenesis by affecting the expression of the melanogenic enzymes. The anticancer activity of sesamolin based on antiproliferation and inhibition of migration was demonstrated in human colon cancer cells. In addition, treatment with sesamolin could stimulate immune cells to enhance the cytolytic activity to kill Burkitt’s lymphoma cells. However, the toxicity and safety of sesamolin have not been reported. And there is also less information on the experimental study in vivo. The limited aqueous solubility of sesamolin becomes the main problem, which affects its pharmacological activity in the in vitro experiment and clinical efficacy. Therefore, solubility enhancement is needed for further investigation and determination of its pharmacological activity profiles. Since there are fewer reports studying this issue, it could become a future prospective research opportunity.

Quercetin Shows the Pharmacological Activity to Simultaneously Downregulate the Inflammatory and Fibrotic Responses to Tissue Injury in Association with its Ability to Target Multi-Kinases

Pharmacology ◽  
2018 ◽  
Vol 102 (3-4) ◽  
pp. 142-153 ◽  
Author(s):  
Ju-Yong Song ◽  
Do Vinh Truong ◽  
Beom-Seok Yang
Keyword(s):  
Signaling Pathways ◽  
Pharmacological Activity ◽  
Tissue Injury ◽  
Dermal Fibroblasts ◽  
Organ Injury ◽  
Cutaneous Wound ◽  
Raw264.7 Macrophages ◽  
Chronic Disorders

Aim: Previous studies have suggested that quercetin is effective for treating diverse chronic disorders including organ fibrosis and airway and cardiovascular disorders. To access the pharmacological background for its broad efficacy, we examined the ability of quercetin to modulate the inflammatory and fibrotic responses associated with organ injury that commonly underlie the pathogenesis of those disorders. Methods: A cutaneous wound model on rabbit ear was used for in vivo study. Quercetin was topically applied to the wounds, and the number of macrophages and myofibroblasts and the size of the hypertrophic scar formed were estimated. An in vitro study examined the ability of quercetin to inhibit cell-signaling pathways that activate RAW264.7 macrophages and primary dermal fibroblasts and the tyrosine kinase activity of discoidin domain receptor 2. Results: Quercetin reduced the population of macrophages and myofibroblasts and the scar formation in cutaneous wound healing. Quercetin suppressed the signaling pathways activating RAW264.7 macrophages and dermal fibroblasts, which is associated with its inhibition of multiple tyrosine kinases to regulate the pathways. This pharmacological activity of quercetin to simultaneously inhibit the inflammatory and fibrotic responses upon tissue damage by targeting multi-kinases could be the action mechanism to support its broad efficacy for various chronic disorders.

scholarly journals Conjugation of Daunorubicin to Monoclonal Antihuman Sarcoma Antibody by a Novel Method

1992 ◽  
Vol 3 (suppl b) ◽  
pp. 101-105
Author(s):  
Michel Pagé ◽  
Denis Thibeault ◽  
Hélène Tremblay ◽  
Christiane Noël ◽  
Marie-Josée Perron
Keyword(s):  
Cell Lines ◽  
Pharmacological Activity ◽  
Tumour Cell ◽  
Immunological Specificity ◽  
Coupling Procedure ◽  
Novel Method ◽  
Tumour Cell Lines

Most of the reported methods for coupling anthracycline drugs to antibody result in either a loss of pharmacological activity or yield antibodies which have lost much of their immunological specificity. The use of glutaraldehyde for coupling saves both the pharmacological and immunological activities but it causes some polymerization of the antibody or of the macromolecular carrier which is undesirable for in vivo use. A new coupling procedure is reported which uses an activated derivative of daunorubicin added to monoclonal antihuman sarcoma antibody. This coupling procedure has not resulted in significant polymerization of the antibody or Joss of pharmacological activity determined by testing normal and tumour cell Lines in vitro.

scholarly journals Salmeterol, a novel, long-acting β2-adrenoceptor agonist: characterization of pharmacological activity in vitro and in vivo

1991 ◽  
Vol 104 (3) ◽  
pp. 665-671 ◽  
Author(s):  
D.I. Ball ◽  
R.T. Brittain ◽  
R.A. Coleman ◽  
L.H. Denyer ◽  
D. Jack ◽  
...  
Keyword(s):  
Pharmacological Activity ◽  
Adrenoceptor Agonist ◽  
Long Acting

scholarly journals The Gastrointestinal Irritation of Polygala Saponins and Its Potential Mechanism In Vitro and In Vivo

2015 ◽  
Vol 2015 ◽  
pp. 1-8 ◽  
Author(s):  
Li Wen ◽  
Nan Xia ◽  
PeiPei Tang ◽  
Yi Hong ◽  
ZiZhen Wang ◽  
...  
Keyword(s):  
Pharmacological Activity ◽  
Gastrointestinal Toxicity ◽  
Potential Mechanism ◽  
Gut Motility ◽  
Sleeping Time ◽  
Sedative Activity

Processing alters the pharmacological activity and reduces the gastrointestinal toxicity of the polygalae. To investigate the effect of processing, different glycosyl substituent products were tested. Hypnotic and subhypnotic doses of pentobarbital-induced sleep tests on mice were used to evaluate the sedative activity of polygala saponins with different glycosyl substituents; isolated gut motility experiment was employed to study excitatory effects of different polygala saponins; the gastrointestinal irritation effects of different polygala saponins were compared by measuring the levels of gastric PGE2 and intestinal TNF-αon mice. When compared with control, Onjisaponin B (OJB) and tenuifolin (TEN), but not senegenin (SNG), significantly increased the number of sleeping mice and prolonged the sleeping time (P<0.05); 80, 40, and 20 mg/L of OJB and 80 mg/L of TEN, but not SNG, obviously changed the amplitude and frequency of isolated jejunum (P<0.05); all the three compounds significantly decreased the level of gastric PGE2 but had no obvious influences on the reduction of intestinal TNF-αlevel. For sedative and hypnotic effects, OJB > TEN > SNG; for the protection form gastrointestinal irritation and damages, OJB > TEN > SNG. Therefore, in processing Polygala, glycosyl breaking may be related to the decline of pharmacological activity and gastrointestinal toxicity of polygala saponins.

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