Potential therapy of Sambiloto plant (Andrographis paniculata) using multi-compounds analysis

2021 ◽  
Vol 129 (4) ◽  
Author(s):  
Handayani ◽  
Wiwik Winarningsih
Keyword(s):  
Herbal Medicine ◽  
Receptor Antagonist ◽  
Mechanism Of Action ◽  
Receptor Agonist ◽  
Kinase Inhibitor ◽  
Therapeutic Potential ◽  
Andrographis Paniculata ◽  
Chemical Bonds ◽  
Receptor Kinase ◽  
Active Content

Introduction: Sambiloto plant (Andrographis paniculata) is often used as herbal medicine plant in Indonesia. Previous evidence indicates the use of a whole plant or single-compound approach. Analysis of multi-compounds is needed to determine the therapeutic potential for standardizing herbal medicine to provide a reliable effect. Methods: An exploratory study searching for the active content of A. paniculata was carried out in the Knapsack program. The chemical structure is analyzed computationally using Prediction of Activity Spectra for Substances (PASS) software. The analysis of the mechanism of action of drug molecules was analyzed using the Search Tool for Interacting Chemicals (STITCH) software. Results: The active content of A. paniculata is 46 types, with 5 of them having 6 effects based on chemical bonds and targeting 12 receptor proteins. Five active contents of A. paniculata include andrographidin A, caffeic acid, chlorogenic acid, wogonin 5-glucoside, and cinnamic acid. Analysis of the mechanism of action of A. paniculata based on 12 target proteins from active ingredients using a multi-compound approach shows 6 unique biological processes. Based on the chemical bonds, 5 active contents of A. paniculata have six effects, including anaphylatoxin receptor antagonist, a beta-adrenergic receptor kinase inhibitor, GABA C receptor agonist, G-protein-coupled receptor kinase inhibitor, Aryl hydrocarbon receptor agonist, and Nicotinic alpha6beta3beta4alpha5 receptor antagonist. Conclusion: There is a therapeutic potential of A. paniculata with multi-compounds analysis. A molecular docking analysis is needed to predict the affinity between the ligand (active ingredient) and the target protein.

scholarly journals TGF-β Type I Receptor Kinase Inhibitor EW-7197 Suppresses Cholestatic Liver Fibrosis by Inhibiting HIF1α-Induced Epithelial Mesenchymal Transition

2016 ◽  
Vol 38 (2) ◽  
pp. 571-588 ◽  
Author(s):  
Min-Jin Kim ◽  
Sang-A Park ◽  
Chun Hwa Kim ◽  
So-Yeon Park ◽  
Jung-Shin Kim ◽  
...  
Keyword(s):  
Liver Fibrosis ◽  
Rat Model ◽  
Transforming Growth Factor ◽  
Kinase Inhibitor ◽  
Epithelial Mesenchymal Transition ◽  
Therapeutic Potential ◽  
Type I ◽  
Receptor Kinase ◽  
Mesenchymal Transition ◽  
Duct Ligation

Background/Aims: Hypoxia is an environmental factor that aggravates liver fibrosis. HIF1α activates hepatic stellate cells (HSCs) and increases transforming growth factor-β (TGF-β) signaling and the epithelial mesenchymal transition (EMT), accelerating the progression of fibrosis. We evaluated the anti-fibrotic therapeutic potential of a small-molecule inhibitor of TGF-β type I receptor kinase, EW-7197, on HIF1α-derived TGF-β signaling in cholestatic liver fibrosis. Methods: We used a bile duct ligation (BDL)-operated rat model to characterize the role of HIF1α-derived TGF-β signaling in liver fibrosis. Cellular assays were performed in LX-2 cells (human immortalized HSCs). The anti-fibrotic effects of EW-7197 in liver tissues and HSCs were investigated via biochemical assays, immunohistochemistry (IHC), immunofluorescence (IF), chromatin immunoprecipitation (ChIP) assays, real-time PCR, and western blotting. Results: In our BDL rat model, orally administered EW-7197 inhibited fibrosis and attenuated HIF1α-induced activation of HSCs and EMT in vivo. In addition, EW-7197 inhibited HIF1α-derived HSC activation and expression of EMT markers in LX-2 cells in vitro. Conclusion: This study suggests that EW-7197 exhibits potential as a treatment for liver fibrosis because it inhibits HIF1α-induced TGF-β signaling.

947: Chemopreventive Effects of COX-2 Inhibitor and Epidermal Growth Factor (EGF)-Receptor Kinase Inhibitor on Rat Urinary Bladder Tumorigenesis

2004 ◽  
Vol 171 (4S) ◽  
pp. 251-251
Author(s):  
Kazunori Hattori ◽  
Katsuyuki Iida ◽  
Akira Johraku ◽  
Sadamu Tsukamoto ◽  
Taeko Asano ◽  
...  
Keyword(s):  
Growth Factor ◽  
Epidermal Growth Factor ◽  
Urinary Bladder ◽  
Egf Receptor ◽  
Kinase Inhibitor ◽  
Receptor Kinase ◽  
Rat Urinary Bladder ◽  
Epidermal Growth ◽  
Cox 2

From Ocean to Bedside: the Therapeutic Potential of Molluscan Hemocyanins

2018 ◽  
Vol 25 (20) ◽  
pp. 2292-2303 ◽  
Author(s):  
Negar Talaei Zanjani ◽  
Monica Miranda Saksena ◽  
Fariba Dehghani ◽  
Anthony L. Cunningham
Keyword(s):  
Antiviral Activity ◽  
Clinical Efficacy ◽  
Mechanism Of Action ◽  
Therapeutic Agent ◽  
Marine Invertebrates ◽  
Therapeutic Potential ◽  
Biological Functions ◽  
Anticancer Properties ◽  
Mechanistic Understanding

Hemocyanins are large and versatile glycoproteins performing various immunological and biological functions in many marine invertebrates including arthropods and molluscs. This review discusses the various pharmacological applications of mollusc hemocyanin such as antiviral activity, immunostimulatory and anticancer properties that have been reported in the literature between the years 2000 and 2016. Emphasis is placed on a better mechanistic understanding of hemocyanin as a therapeutic agent. Elucidation of the mechanism of action is essential to improve the clinical efficacy and for a better understanding of some endogenous immunological functions of this complex glycoprotein.

Medicinal Plants and Bioactive Compounds for Diabetes Management: Important Advances for Drug Discovery

2020 ◽  
Vol 26 ◽  
Author(s):  
Kondeti Ramudu Shanmugam ◽  
Bhasha Shanmugam ◽  
Gangigunta Venkatasubbaiah ◽  
Sahukari Ravi ◽  
Kesireddy Sathyavelu Reddy
Keyword(s):  
Herbal Medicine ◽  
Medicinal Plants ◽  
Bioactive Compounds ◽  
Diabetes Management ◽  
Therapeutic Potential ◽  
Public Health Problem ◽  
In Vivo Studies ◽  
Major Public Health Problem

Background : Diabetes is a major public health problem in the world. It affects each and every part of the human body and also leads to organ failure. Hence, great progress made in the field of herbal medicine and diabetic research. Objectives: Our review will focus on the effect of bioactive compounds of medicinal plants which are used to treat diabetes in India and other countries. Methods: Information regarding diabetes, oxidative stress, medicinal plants and bioactive compounds were collected from different search engines like Science direct, Springer, Wiley online library, Taylor and francis, Bentham Science, Pubmed and Google scholar. Data was analyzed and summarized in the review. Results and Conclusion: Anti-diabetic drugs that are in use have many side effects on vital organs like heart, liver, kidney and brain. There is an urgent need for alternative medicine to treat diabetes and their disorders. In India and other countries herbal medicine was used to treat diabetes. Many herbal plants have antidiabetic effects. The plants like ginger, phyllanthus, curcumin, aswagandha, aloe, hibiscus and curcuma showed significant anti-hyperglycemic activities in experimental models and humans. The bioactive compounds like Allicin, azadirachtin, cajanin, curcumin, querceitin, gingerol possesses anti-diabetic, antioxidant and other pharmacological properties. This review focuses on the role of bioactive compounds of medicinal plants in prevention and management of diabetes. Conclusion: Moreover, our review suggests that bioactive compounds have the potential therapeutic potential against diabetes. However, further in vitro and in vivo studies are needed to validate these findings.

scholarly journals Balneotherapy with the Use of Radon–Sulphide Water: The Mechanisms of Therapeutic Effect

2021 ◽  
Vol 11 (6) ◽  
pp. 2849
Author(s):  
Lilla Pawlik-Sobecka ◽  
Joanna Górka-Dynysiewicz ◽  
Jadwiga Kuciel-Lewandowska
Keyword(s):  
Natural Resources ◽  
Therapeutic Effect ◽  
Mechanism Of Action ◽  
World Literature ◽  
Therapeutic Potential ◽  
Health Resort ◽  
The World ◽  
Spa Treatment ◽  
Combined Action

Despite its enormous therapeutic potential, spa treatment is not always properly perceived, hence the numerous attempts to assess its effectiveness. In the world literature, there are few reports on therapy using sulphur- and radon-containing therapeutic waters. In countries with a long tradition of balneotherapy, activity in this field of medicine is evident. Undoubtedly, the interest in balneotherapy results also from natural resources used in spa medicine, which, as geological and balneochemical research shows, are enormous in Poland. A particular example of the occurrence of radon–sulphide waters, rare on the European scale, is the Przerzeczyn-Zdrój health resort. The mechanism of action of therapeutic waters is not fully explored, but their effectiveness in therapy is confirmed by many authors. It is believed to be an effect of combined action of many factors, the most important of which are thermal, mechanical, and chemical.

scholarly journals Repurposing cabozantinib with therapeutic potential in KIT-driven t(8;21) acute myeloid leukaemias

2021 ◽  
Author(s):  
Kuan-Wei Su ◽  
Da-Liang Ou ◽  
Yu-Hsuan Fu ◽  
Hwei-Fang Tien ◽  
Hsin-An Hou ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Ribosome Biogenesis ◽  
Kinase Inhibitor ◽  
Therapeutic Potential ◽  
Xenograft Model ◽  
Sequencing Analysis ◽  
Dependent Manner ◽  
Leukocyte Activation ◽  
Mouse Xenograft Model ◽  
Acute Myeloid

AbstractCabozantinib is an orally available, multi-target tyrosine kinase inhibitor approved for the treatment of several solid tumours and known to inhibit KIT tyrosine kinase. In acute myeloid leukaemia (AML), aberrant KIT tyrosine kinase often coexists with t(8;21) to drive leukaemogenesis. Here we evaluated the potential therapeutic effect of cabozantinib on a selected AML subtype characterised by t(8;21) coupled with KIT mutation. Cabozantinib exerted substantial cytotoxicity in Kasumi-1 cells with an IC50 of 88.06 ± 4.32 nM, which was well within clinically achievable plasma levels. The suppression of KIT phosphorylation and its downstream signals, including AKT/mTOR, STAT3, and ERK1/2, was elicited by cabozantinib treatment and associated with subsequent alterations of cell cycle- and apoptosis-related molecules. Cabozantinib also disrupted the synthesis of an AML1-ETO fusion protein in a dose- and time-dependent manner. In a mouse xenograft model, cabozantinib suppressed tumourigenesis at 10 mg/kg and significantly prolonged survival of the mice. Further RNA-sequencing analysis revealed that mTOR-mediated signalling pathways were substantially inactivated by cabozantinib treatment, causing the downregulation of ribosome biogenesis and glycolysis, along with myeloid leukocyte activation. We suggest that cabozantinib may be effective in the treatment of AML with t(8;21) and KIT mutation. Relevant clinical trials are warranted.

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