Molecule which changed the view on skin treatment

2021 ◽  
pp. 44-55
Author(s):  
L.Ya. Fedorich
Keyword(s):  
Retinoic Acid ◽  
Nuclear Receptors ◽  
Mechanism Of Action ◽  
Molecular Mechanisms ◽  
Local Treatment ◽  
Mechanisms Of Action ◽  
Clinical Effects ◽  
Topical Retinoids ◽  
Acne Therapy ◽  
Universal Mechanism

Objective — to study the modern classification, mechanisms of action and clinical effects of vitamin A derivatives, to analyze retinoid for local treatment of various dermatoses with a universal mechanism of action at the epidermis and dermis levels. Materials and methods. A review of the literature and an analysis of the results of international clinical trials of drugs based on the natural retinoid of the first generation — tretinoin (retinoic acid) is presented. The works of dozens of authors since 1980s to the present day are analyzed. Most sources provide detailed information on the results of topical retinoids in acne therapy, which are the base of clinical guidelines. Long-term (6 months or more) studies of retinoic acid-based preparations carried out in recent decades have discovered the unique clinical effects of tretinoin in the treatment of skin photoaging, actinic keratosis, etc. They are achieved due to the effect of tretinoid on the nuclear receptors of keratinocytes and fibroblasts. Results and discussion. The molecular mechanisms of action of retinoic acid, realizing the cellular and tissue effects of the most studied retinoid, are systematized and grouped in a single review. It has been proven that a unique feature of tretinin is its ability to activate directly all subtypes of RARs- and, indirectly, RARs-nuclear receptors of skin cells. A new modern drug for external use is presented — AltrenoТМ lotion containing micronized 0.05 % tretinoin in combination with sodium hyaluronate, soluble collagen and glycerin. This combination exhibits the expected clinical efficacy in acne therapy and prevents side effects such as dryness, redness and exfoliation. AltrenoТМ is approved for use in children of 9 years of age and older. Conclusions. Tretinoin (retinoic acid) is a modern powerful retinoid with a universal mechanism of action, recommended for the treatment of acne.

scholarly journals Biochemistry and Molecular Biology of Mechanisms of Action of Fibrates – An Overview

2019 ◽  
pp. 1-12 ◽  
Author(s):  
A.S. V. Prasad
Keyword(s):  
Mechanism Of Action ◽  
Molecular Mechanisms ◽  
Organic Anion ◽  
Density Lipoprotein ◽  
The United States ◽  
Mechanisms Of Action ◽  
Lipid Lowering ◽  
Intervention Trial ◽  
Ligand Interaction ◽  
Cholesterol Acyl Transferase

Fibrates are a class of medication that mainly lowers the blood triglyceride levels. They reduce the LDL and increase the levels of HDL C, in the blood. Clofibrate, the first member to be discovered  in 1962 , and introduced in USA in 1967, is withdrawn in 2002, due to unexplained hepatomegaly, hepato-toxicity and possible risk of hepatic cancer. Other fibrates are introduced in the late 1970s and early 1980s, such as gemfibrozil in the United States and bezafibrate and ciprofibrate in Europe. Their lipid lowering effects are found to decrease CVS risk , progression of atherosclerosis and metabolic syndrome,  macrovascular and microvascular diabetic complications  like stroke, myocardial infarction, peripheral vascular disease  and  diabetic  retinopathy .Various clinical trials like VA-HIT trial (Veterans Affairs High-Density Lipoprotein Cholesterol Intervention Trial) ,  FIELD trail.  (the Fenofibrate Intervention and Event Lowering in Diabetes) Helsinki Heart Study,   ACCORD -Lipid trial  (The lipid component of the Action to Control Cardiovascular Risk in Diabetes trial ) and  BIP (Bezafibrate Infarction Prevention Study)  trial and angiography trials, like LOCAT (Lopid Coronary Angiography Trial)  and BECLAIT (Bezafibrate Coronary Atherosclerosis Intervention Trial) demonstrated the  beneficial effects of gemfibrozil and fenofibrate.  Their mechanism of action remained obscure for three decades, ie till 1990s, when their mode of action was found. The Mechanism of action of fibrates include limitation of substrate availability for triglyceride synthesis in the liver, promotion of the action of lipoprotein lipase, (LPL)  modulation of low density lipoprotein receptor/ligand interaction and stimulation of reverse cholesterol transport The biochemical and molecular mechanisms involving  the various  enzymes like LCAT (Lecithin-cholesterol acyl transferase)  and CYP7A1 etc.  (cholesterol 7-alpha-monooxygenase or cytochrome P450 7A1 (CYP7A1) ) ,  transporters like ABC , CETP (ATP-binding cassette transporter, Cholesterol ester binding protein) and NTCP, OATP (Na+-dependent taurocholate transporter / organic anion transporters) . These are the.) and nuclear factors like LXR, PPAR alfa etc. (liver orphan receptor α , and peroxisome proliferative nuclear factor) , in relation to the mechanisms  of action of fibrates are discussed . Areas of current interests in literature are briefed.

Mechanisms of Action of Different Drugs of Abuse

2014 ◽  
Author(s):  
Lindsay M. McCracken ◽  
Mandy L. McCracken ◽  
R. Adron Harris
Keyword(s):  
Drug Use ◽  
Mechanism Of Action ◽  
Molecular Mechanisms ◽  
Drugs Of Abuse ◽  
Chronic Administration ◽  
Repeated Administration ◽  
Mechanisms Of Action ◽  
Neuronal Membrane ◽  
Sedative Hypnotics ◽  
Routes Of Drug Administration

Drugs of abuse represent a spectrum of chemically diverse compounds that are used via various routes of drug administration depending on the drug and its preparation. Although the exact molecular mechanisms by which these agents act to produce their intoxicating effects are not completely understood, many drugs of abuse are known to bind to specific neuronal membrane proteins that produce effects on cellular signaling and ultimately on behavior. With repeated administration of a drug, individuals often develop tolerance, and discontinuation of drug use following chronic administration typically results in withdrawal symptoms. This chapter describes the mechanism of action for the following classes of drugs of abuse: alcohol, cannabinoids, hallucinogens, inhalants, nicotine, opioids, sedative hypnotics, and stimulants. In addition, mechanisms of tolerance and withdrawal are discussed.

scholarly journals Anti-Angiogenic Alternative and Complementary Medicines for the Treatment of Endometriosis: A Review of Potential Molecular Mechanisms

2018 ◽  
Vol 2018 ◽  
pp. 1-28 ◽  
Author(s):  
Weilin Zheng ◽  
Lixing Cao ◽  
Zheng Xu ◽  
Yuanyuan Ma ◽  
Xuefang Liang
Keyword(s):  
Natural Products ◽  
Molecular Mechanisms ◽  
Experimental Studies ◽  
Mechanisms Of Action ◽  
Therapeutic Effects ◽  
Clinical Effects ◽  
Chinese Medicines ◽  
Complementary Medicines ◽  
Angiogenic Therapy ◽  
Keywords Endometriosis

Endometriosis is caused by the growth or infiltration of endometrial tissues outside of the endometrium and myometrium. Symptoms include pain and infertility. Surgery and hormonal therapy are widely used in Western medicine for the treatment of endometriosis; however, the side effects associated with this practice include disease recurrence and menopause, which can severely influence quality of life. Angiogenesis is the main biological mechanism underlying the development of endometriosis. Numerous natural products and Chinese medicines with potent anti-angiogenic effects have been investigated, and the molecular basis underlying their therapeutic effects in endometriosis has been explored. This review aims to describe natural products and compounds that suppress angiogenesis associated with endometriosis and to assess their diverse molecular mechanisms of action. Furthermore, this review provides a source of information relating to alternative and complementary therapeutic products that mediate anti-angiogenesis. An extensive review of the literature and electronic databases, such as the China National Knowledge Infrastructure, PubMed, and Embase, was conducted using the keywords ‘endometriosis,’ ‘traditional Chinese medicine,’ ‘Chinese herbal medicine,’ ‘natural compounds,’ and ‘anti-angiogenic’ therapy. Anti-angiogenic therapy is an emerging strategy for the treatment of endometriosis. Natural anti-angiogenic products and Chinese medicines provide several beneficial clinical effects, including pain relief. In this review, we summarize clinical trials and experimental studies of endometriosis using natural products and Chinese medicines. In particular, we focus on anti-angiogenic products and alternative and complementary medicines for the treatment of endometriosis and additionally examine their therapeutic efficacy and mechanisms of action. Anti-angiogenic natural products and/or compounds provide a new approach for the treatment of endometriosis. Future work will require randomized trials with larger numbers of subjects, as well as long-term follow-up to confirm the findings described here.

New insights into the mechanism of action of the cyclopalladated complex - CP2 in Leishmania : Calcium Dysregulation, Mitochondrial Dysfunction and Cell Death

2021 ◽  
Author(s):  
Angela M. A. Velásquez ◽  
Paula J. Bartlett ◽  
Irwin A. P. Linares ◽  
Thais G. Passalacqua ◽  
Daphne D. L. Teodoro ◽  
...  
Keyword(s):  
Cell Death ◽  
Mechanism Of Action ◽  
Molecular Mechanisms ◽  
Parasite Load ◽  
Current Treatment ◽  
Mechanisms Of Action ◽  
S Phase ◽  
Comprehensive Understanding ◽  
Calcium Dysregulation ◽  
Cycle Arrest

The current treatment of leishmaniasis is based on few drugs that present several drawbacks such as high toxicity, difficult administration route, and low efficacy. These disadvantages raise the necessity to develop novel antileishmanial compounds allied to a comprehensive understanding of their mechanisms of action. Here, we elucidate the probably mechanism of action of the antileishmanial binuclear cyclopalladated complex [Pd(dmba)(μ-N 3 )] 2 ( CP2 ) in Leishmania amazonensis . CP2 causes oxidative stress in the parasite resulting in disruption of mitochondrial Ca 2+ homeostasis, cell cycle arrest at S-phase, increasing the ROS production and overexpression of stress-related and cell detoxification proteins, collapsing the Leishmania mitochondrial membrane potential and promotes apoptotic-like features in promastigotes leading to necrosis or directs programmed cell death (PCD)-committed cells toward necrotic-like destruction. Moreover, CP2 is able to reduce the parasite load in both liver and spleen in Leishmania infantum -infected hamsters when treated for 15 days with 1.5 mg/Kg/day CP2 , expanding its potential application in addition to the already known effectiveness on cutaneous leishmaniasis for the treatment of visceral leishmaniasis, showing the broad spectrum of action of this cyclopalladated complex. The data herein presented bring new insights into the CP2 molecular mechanisms of action, assisting to promote its rational modification to improve both safety and efficacy.

scholarly journals Mechanisms of Action of Ribosomally Synthesized and Posttranslationally Modified Peptides (RiPPs)

2021 ◽  
Author(s):  
Li Cao ◽  
Truc Do ◽  
A James Link
Keyword(s):  
Natural Products ◽  
Mechanism Of Action ◽  
Molecular Mechanisms ◽  
Structural Information ◽  
Genome Mining ◽  
Mechanisms Of Action ◽  
Detailed Mechanism ◽  
Modified Peptides ◽  
Drug Leads

Abstract Natural products remain a critical source of medicines and drug leads. One of the most rapidly growing superclasses of natural products is RiPPs: ribosomally synthesized and posttranslationally modified peptides. RiPPs have rich and diverse bioactivities. This review highlights examples of the molecular mechanisms of action that underly those bioactivities. Particular emphasis is placed on RiPP/target interactions for which there is structural information. This detailed mechanism of action work is critical toward the development of RiPPs as therapeutics and can also be used to prioritize hits in RiPP genome mining studies.

Maintenance acne therapy: prophylactic efficacy of fixed combination of adapalene and benzoyl peroxide

2020 ◽  
pp. 57-62
Author(s):  
L. S. Kruglova ◽  
N. V. Gryazeva
Keyword(s):  
Maintenance Therapy ◽  
Fixed Combination ◽  
Psychological Impact ◽  
Supportive Therapy ◽  
Prophylactic Efficacy ◽  
Severe Acne ◽  
Topical Retinoids ◽  
Acne Therapy ◽  
Group 2 ◽  
Treatment Observation

Acne is a chronic disease and even reliable therapies do not completely ensure absence of relapses. Acne relapses have a negative psychological impact on patients, as they feel unable to control the disease and achieve complete and long-lasting recovery. Supportive therapy is necessary to prolong the remission of acne achieved with initial successful treatment and to minimize the risk of relapse. According to the literature sources, the most justified as a maintenance therapy is the use of topical retinoids, which have been shown to be effective in the prevention of exacerbations of acne. In the present study 54 patients were involved who after the active therapy used a fixed combination of adapalene 0.1% / BPO 2.5% as maintenance treatment. Only 1 patient (2.9%) with moderate acne and 2 patients (5.8%) with severe acne had a relapse within 6 months of maintenance therapy. The absence of adverse events during the course of treatment was recorded, as well as high adherence of patients to the treatment. During the period of post-treatment observation (6 months after maintenance therapy), among the patients without exacerbations during maintenance therapy, a relapse occurred in 2 (7.1%) patients of group 1 (n = 28) and 2 (8.7%) patients of group 2 (n = 23). The obtained data indicates that maintenance therapy with Effezel® gel can extend the achieved effectiveness of the treatment and prevent the development of relapses.

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