scholarly journals Antidiabetic Effects of Resveratrol: The Way Forward in Its Clinical Utility

2016 ◽  
Vol 2016 ◽  
pp. 1-14 ◽  
Author(s):  
Omolola R. Oyenihi ◽  
Ayodeji B. Oyenihi ◽  
Anne A. Adeyanju ◽  
Oluwafemi O. Oguntibeju
Keyword(s):  
Diabetes Mellitus ◽  
Clinical Utility ◽  
Therapeutic Agent ◽  
Molecular Targets ◽  
Therapeutic Agents ◽  
Mechanisms Of Action ◽  
Antidiabetic Drug ◽  
Near Future ◽  
Antidiabetic Effects ◽  
The Way

Despite recent advances in the understanding and management ofdiabetes mellitus, the prevalence of the disease is increasing unabatedly with resulting disabling and life-reducing consequences to the global human population. The limitations and side effects associated with current antidiabetic therapies have necessitated the search for novel therapeutic agents. Due to the multipathogenicity ofdiabetes mellitus,plant-derived compounds with proven multiple pharmacological actions have been postulated to “hold the key” in the search for an affordable, efficacious, and safer therapeutic agent in the treatment of the disease and associated complications. Resveratrol, a phytoalexin present in few plant species, has demonstrated beneficial antidiabetic effects in animals and humans through diverse mechanisms and multiple molecular targets. However, despite the enthusiasm and widespread successes achieved with the use of resveratrol in animal models ofdiabetes mellitus, there are extremely limited clinical data to confirm the antidiabetic qualities of resveratrol. This review presents an update on the mechanisms of action and protection of resveratrol indiabetes mellitus, highlights challenges in its clinical utility, and suggests the way forward in translating the promising preclinical data to a possible antidiabetic drug in the near future.

scholarly journals Present and Prospective Pharmacotherapy for the Management of Patients with Type 2 Diabetes

2009 ◽  
Vol 1 ◽  
pp. CMT.S2109
Author(s):  
Leonor Corsino ◽  
Mary Elizabeth Cox ◽  
Jennifer Rowell ◽  
Jennifer B. Green
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Glycemic Control ◽  
Chronic Condition ◽  
Diabetes Management ◽  
Mechanisms Of Action ◽  
Glucose Lowering ◽  
Prevention Of Diabetes ◽  
Near Future

Diabetes Mellitus is a chronic condition prevalent worldwide. Type 2 diabetes is the most common form of diabetes, comprising 90% to 95% of all cases. Over the last few decades, the importance of glycemic control and its impact on prevention of diabetes-related complications has been documented in multiple clinical trials. As most patients with type 2 diabetes will require pharmacologic intervention to achieve and maintain appropriate glycemic control, new medications targeting different aspects of the pathophysiology of type 2 diabetes have been a significant focus of research and development. During the last decade, multiple new medications for diabetes management have become available: these medications have novel mechanisms of action, differences in effectiveness, and varying side effect profiles which will be reviewed in this article. Some of these newer medications, such as the GLP-1 analogues and DPP-4 inhibitors, have become widely accepted as therapeutic options for the management of type 2 diabetes. Additional classes of glucose-lowering medications are expected to become available in the near future. This manuscript will summarize available data regarding these newer and prospective medications for the management of type 2 diabetes.

Autophagy Modulators and Neuroinflammation

2020 ◽  
Vol 27 (6) ◽  
pp. 955-982 ◽  
Author(s):  
Kyoung Sang Cho ◽  
Jang Ho Lee ◽  
Jeiwon Cho ◽  
Guang-Ho Cha ◽  
Gyun Jee Song
Keyword(s):  
Neurodegenerative Disorders ◽  
Neurological Disorders ◽  
Mammalian Cells ◽  
Critical Role ◽  
Therapeutic Agents ◽  
Mechanisms Of Action ◽  
Scientific Interest ◽  
Therapeutic Tools ◽  
Underlying Mechanisms

Background: Neuroinflammation plays a critical role in the development and progression of various neurological disorders. Therefore, various studies have focused on the development of neuroinflammation inhibitors as potential therapeutic tools. Recently, the involvement of autophagy in the regulation of neuroinflammation has drawn substantial scientific interest, and a growing number of studies support the role of impaired autophagy in the pathogenesis of common neurodegenerative disorders. Objective: The purpose of this article is to review recent research on the role of autophagy in controlling neuroinflammation. We focus on studies employing both mammalian cells and animal models to evaluate the ability of different autophagic modulators to regulate neuroinflammation. Methods: We have mostly reviewed recent studies reporting anti-neuroinflammatory properties of autophagy. We also briefly discussed a few studies showing that autophagy modulators activate neuroinflammation in certain conditions. Results: Recent studies report neuroprotective as well as anti-neuroinflammatory effects of autophagic modulators. We discuss the possible underlying mechanisms of action of these drugs and their potential limitations as therapeutic agents against neurological disorders. Conclusion: Autophagy activators are promising compounds for the treatment of neurological disorders involving neuroinflammation.

Molecular Targets of Phytochemicals for Skin Inflammation

2018 ◽  
Vol 24 (14) ◽  
pp. 1533-1550 ◽  
Author(s):  
Jong-Eun Kim ◽  
Ki Won Lee
Keyword(s):  
Skin Diseases ◽  
Molecular Targets ◽  
Skin Inflammation ◽  
Mechanisms Of Action ◽  
The Body ◽  
Cellular Damage ◽  
Aesthetic Appearance ◽  
Immune Mediated ◽  
Skin Conditions ◽  
Effects Of Aging

Skin is a protective organ and the largest of the human body. Due to its pivotal role in aesthetic appearance, skin health has a significant impact on quality of life. Chronic inflammation of the skin often marks the beginning of various skin diseases. Immune-mediated responses serve to protect the body from external insults and require succinct control, and can lead to ongoing cellular damage and various skin conditions if left unchecked. Studies have shown that phytochemicals can alter processes involved in skin inflammation and alleviate the effects of aging, cancer, atopic dermatitis, psoriasis, and vitiligo. Direct molecular targets of some phytochemicals have been identified and their precise mechanisms of action investigated. In this review, we summarize recent findings on the effects of phytochemicals on skin inflammation and the mechanisms of action involved.

Identification of 2-Fluoropalmitic Acid as a Potential Therapeutic Agent Against Glioblastoma

2020 ◽  
Vol 26 (36) ◽  
pp. 4675-4684 ◽  
Author(s):  
Shabierjiang Jiapaer ◽  
Takuya Furuta ◽  
Yu Dong ◽  
Tomohiro Kitabayashi ◽  
Hemragul Sabit ◽  
...  
Keyword(s):  
Combination Therapy ◽  
Drug Screening ◽  
Therapeutic Agent ◽  
Gelatin Zymography ◽  
Therapeutic Agents ◽  
Drug Candidate ◽  
Potential Therapeutic Agent ◽  
Sphere Formation ◽  
Improve Patient

Background: Glioblastomas (GBMs) are aggressive malignant brain tumors. Although chemotherapy with temozolomide (TMZ) can extend patient survival, most patients eventually demonstrate resistance. Therefore, novel therapeutic agents that overcome TMZ chemoresistance are required to improve patient outcomes. Purpose: Drug screening is an efficient method to find new therapeutic agents from existing drugs. In this study, we explored a novel anti-glioma agent by drug screening and analyzed its function with respect to GBM treatment for future clinical applications. Methods: Drug libraries containing 1,301 diverse chemical compounds were screened against two glioma stem cell (GSC) lines for drug candidate selection. The effect of selected agents on GSCs and glioma was estimated through viability, proliferation, sphere formation, and invasion assays. Combination therapy was performed to assess its ability to enhance TMZ cytotoxicity against GBM. To clarify the mechanism of action, we performed methylation-specific polymerase chain reaction, gelatin zymography, and western blot analysis. Results: The acyl-CoA synthetase inhibitor 2-fluoropalmitic acid (2-FPA) was selected as a candidate anti-glioma agent. 2-FPA suppressed the viability and stem-like phenotype of GSCs. It also inhibited proliferation and invasion of glioma cell lines. Combination therapy of 2-FPA with TMZ synergistically enhanced the efficacy of TMZ. 2-FPA suppressed the expression of phosphor-ERK, CD133, and SOX-2; reduced MMP-2 activity; and increased methylation of the MGMT promoter. Conclusion: 2-FPA was identified as a potential therapeutic agent against GBM. To extend these findings, physiological studies are required to examine the efficacy of 2-FPA against GBM in vivo.

Bridging the Gap of Drug Delivery in Colon Cancer: The Role of Chitosan and Pectin Based Nanocarriers System

2020 ◽  
Vol 17 (10) ◽  
pp. 911-924
Author(s):  
Rohitas Deshmukh
Keyword(s):  
Drug Delivery ◽  
Colon Cancer ◽  
Targeted Drug Delivery ◽  
Targeted Delivery ◽  
Therapeutic Agent ◽  
Therapeutic Agents ◽  
Delivery Systems ◽  
Target Tissue ◽  
Polymer Carriers

Colon cancer is one of the most prevalent diseases, and traditional chemotherapy has not been proven beneficial in its treatment. It ranks second in terms of mortality due to all cancers for all ages. Lack of selectivity and poor biodistribution are the biggest challenges in developing potential therapeutic agents for the treatment of colon cancer. Nanoparticles hold enormous prospects as an effective drug delivery system. The delivery systems employing the use of polymers, such as chitosan and pectin as carrier molecules, ensure the maximum absorption of the drug, reduce unwanted side effects and also offer protection to the therapeutic agent from quick clearance or degradation, thus allowing an increased amount of the drug to reach the target tissue or cells. In this systematic review of published literature, the author aimed to assess the role of chitosan and pectin as polymer-carriers in colon targeted delivery of drugs in colon cancer therapy. This review summarizes the various studies employing the use of chitosan and pectin in colon targeted drug delivery systems.

Understanding Molecular Process and Chemotherapeutics for the Management of Breast Cancer.

2020 ◽  
Vol 14 ◽  
Author(s):  
Abhishek Kumar ◽  
Neeraj Masand ◽  
Vaishali M. Patil
Keyword(s):  
Breast Cancer ◽  
Molecular Mechanisms ◽  
Molecular Targets ◽  
Molecular Classification ◽  
Neoplastic Disease ◽  
Molecular Process ◽  
The Past ◽  
Anti Cancer ◽  
Molecular Etiology ◽  
Near Future

Abstract: Breast cancer is the most common and highly heterogeneous neoplastic disease comprised of several subtypes with distinct molecular etiology and clinical behaviours. The mortality observed over the past few decades and the failure in eradicating the disease is due to the lack of specific etiology, molecular mechanisms involved in initiation and progression of breast cancer. Understanding of the molecular classes of breast cancer may also lead to new biological insights and eventually to better therapies. The promising therapeutic targets and novel anti-cancer approaches emerging from these molecular targets that could be applied clinically in the near future are being highlighted. In addition, this review discusses some of the details of current molecular classification and available chemotherapeutics

scholarly journals Tetrandrine alleviates silicosis by inhibiting canonical and non-canonical NLRP3 inflammasome activation in lung macrophages

2021 ◽  
Author(s):  
Mei-yue Song ◽  
Jia-xin Wang ◽  
You-liang Sun ◽  
Zhi-fa Han ◽  
Yi-tian Zhou ◽  
...  
Keyword(s):  
Nlrp3 Inflammasome ◽  
Therapeutic Strategy ◽  
Molecular Targets ◽  
Mechanisms Of Action ◽  
Inflammasome Activation ◽  
Lung Macrophages ◽  
Nlrp3 Inflammasome Activation ◽  
Function Test ◽  
And Control ◽  
Therapeutic Administration

AbstractSilicosis caused by inhalation of silica particles leads to more than ten thousand new occupational exposure-related deaths yearly. Exacerbating this issue, there are currently few drugs reported to effectively treat silicosis. Tetrandrine is the only drug approved for silicosis treatment in China, and despite more than decades of use, its efficacy and mechanisms of action remain largely unknown. Here, in this study, we established silicosis mouse models to investigate the effectiveness of tetrandrine of early and late therapeutic administration. To this end, we used multiple cardiopulmonary function test, as well as markers for inflammation and fibrosis. Moreover, using single cell RNA sequencing and transcriptomics of lung tissue and quantitative microarray analysis of serum from silicosis and control mice, our results provide a novel description of the target pathways for tetrandrine. Specifically, we found that tetrandrine attenuated silicosis by inhibiting both the canonical and non-canonical NLRP3 inflammasome pathways in lung macrophages. Taken together, our work showed that tetrandrine yielded promising results against silicosis-associated inflammation and fibrosis and further lied the groundwork for understanding its molecular targets. Our results also facilitated the wider adoption and development of tetrandirne, potentially accelerating a globally accepted therapeutic strategy for silicosis.

Potential mechanisms of action of convalescent plasma in COVID-19

Diagnosis ◽  
2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Massimo Franchini ◽  
Claudia Glingani ◽  
Giancarlo Maria Liumbruno
Keyword(s):  
Therapeutic Agents ◽  
Mechanisms Of Action ◽  
Narrative Review ◽  
Hypercoagulable State ◽  
Human History ◽  
Catastrophic Events ◽  
Immune Mechanisms ◽  
Anti Inflammatory

Abstract The COVID-19 pandemic will be remembered as one of the worst catastrophic events in human history. Unfortunately, no universally recognized effective therapeutic agents are currently available for the treatment of severe SARS-CoV-2 infection. In this context, the use of convalescent plasma from recovered COVID-19 patients has gained increasing interest thanks to the initially positive clinical reports. A number of mechanisms of action have been proposed for convalescent plasma, including direct neutralization and suppression of viremia, anti-inflammatory and immunomodulation effects and mitigation of the COVID-19-associated hypercoagulable state. These immune and non-immune mechanisms will be critically discussed in this narrative review.

scholarly journals Activity of Anti-Microbial Peptides (AMPs) against Leishmania and Other Parasites: An Overview

Biomolecules ◽  
2021 ◽  
Vol 11 (7) ◽  
pp. 984
Author(s):  
Rima El-Dirany ◽  
Hawraa Shahrour ◽  
Zeinab Dirany ◽  
Fadi Abdel-Sater ◽  
Gustavo Gonzalez-Gaitano ◽  
...  
Keyword(s):  
Innate Immune System ◽  
Therapeutic Agents ◽  
Mechanisms Of Action ◽  
Innate Immune ◽  
Biologically Active ◽  
Neglected Tropical Disease ◽  
Parasitic Diseases ◽  
Promising Alternative ◽  
Parasitic Effect ◽  
Anti Fungal

Anti-microbial peptides (AMPs), small biologically active molecules, produced by different organisms through their innate immune system, have become a considerable subject of interest in the request of novel therapeutics. Most of these peptides are cationic-amphipathic, exhibiting two main mechanisms of action, direct lysis and by modulating the immunity. The most commonly reported activity of AMPs is their anti-bacterial effects, although other effects, such as anti-fungal, anti-viral, and anti-parasitic, as well as anti-tumor mechanisms of action have also been described. Their anti-parasitic effect against leishmaniasis has been studied. Leishmaniasis is a neglected tropical disease. Currently among parasitic diseases, it is the second most threating illness after malaria. Clinical treatments, mainly antimonial derivatives, are related to drug resistance and some undesirable effects. Therefore, the development of new therapeutic agents has become a priority, and AMPs constitute a promising alternative. In this work, we describe the principal families of AMPs (melittin, cecropin, cathelicidin, defensin, magainin, temporin, dermaseptin, eumenitin, and histatin) exhibiting a potential anti-leishmanial activity, as well as their effectiveness against other microorganisms.

scholarly journals Treatment patterns, persistence and adherence rates in patients with type 2 diabetes mellitus in Japan: a claims-based cohort study

BMJ Open ◽  
2019 ◽  
Vol 9 (3) ◽  
pp. e025806 ◽  
Author(s):  
Rimei Nishimura ◽  
Haruka Kato ◽  
Koichi Kisanuki ◽  
Akinori Oh ◽  
Shinzo Hiroi ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Drug Class ◽  
Japanese Patients ◽  
Medical Data ◽  
Treatment Patterns ◽  
Administrative Claims ◽  
Antidiabetic Drug

ObjectiveTo determine real-world trends in antidiabetic drug use, and persistence and adherence, in Japanese patients with type 2 diabetes mellitus (T2DM).DesignRetrospective evaluation of administrative claims data (2011–2015) using the Japan Medical Data Center (JMDC) and Medical Data Vision (MDV) databases.SettingAnalysis of two administrative claims databases for Japanese patients with T2DM.ParticipantsAdults (aged ≥18 years) with an International Classification of Diseases, 10th Revision code of T2DM and at least one antidiabetic drug prescription.Main outcome measuresTreatment patterns in untreated (UT) or previously treated (PT) patients receiving antidiabetic therapy; persistence with treatment at 12 months; adherence to treatment at 12 months.Results40 908 and 90 421 patients were included from the JMDC and MDV databases, respectively. The most frequently prescribed therapy at the index (first prescription) date was dipeptidyl peptidase-4 inhibitor (DPP-4i) in UT patients (JMDC: 44.0%, MDV: 54.8%) and combination therapy in PT patients (74.6%, 81.1%). Most common combinations were DPP-4i plus: biguanide (BG; 11.4%, 10.9%), sulfonylurea (SU; 8.4%, 11.0%) or BG+SU (7.8%, 9.1%). In UT or PT patients from either database whose index prescription was for any antidiabetic drug class(es) other than DPP-4i, the most frequent add-on or switch was to DPP-4i. 12-month persistence with index monotherapy was highest with DPP-4i and BG. Adherence was high (≥80%) for all monotherapy schedules, except insulin and glucagon-like peptide-1 agonist, and for the five most frequent two-drug and three-drug combinations. Persistence was greater in elderly UT patients and in those receiving ≤5 medications, but comparatively worse in UT patients with ≥3 index antidiabetic drug classes.ConclusionsThe findings indicate that DPP-4i is the most commonly used antidiabetic drug class in Japanese patients with T2DM, and persistence and adherence to this antidiabetic drug class are high.

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