scholarly journals Recent Advances Regarding the Therapeutic Potential of Adapalene

2020 ◽  
Vol 13 (9) ◽  
pp. 217
Author(s):  
Aura Rusu ◽  
Corneliu Tanase ◽  
Georgiana-Andreea Pascu ◽  
Nicoleta Todoran
Keyword(s):  
Therapeutic Potential ◽  
Biological Effects ◽  
Acne Vulgaris ◽  
Therapeutic Drug ◽  
Oral Drugs ◽  
First Line ◽  
Biological Potential ◽  
Acne Treatment ◽  
Anti Inflammatory ◽  
Active Substances

Adapalene (ADP) is a representative of the third retinoids generation and successfully used in first-line acne treatment. ADP binds to retinoic acid nuclear receptors. The comedolytic, anti-inflammatory, antiproliferative, and immunomodulatory are the known ADP effects. Its safety profile is an advantage over other retinoids. ADP recently was found to be effective in the treatment of several dermatological diseases and photoaging besides the utility in the treatment of acne vulgaris. New biological effects of adapalene with therapeutic potential are highlighted in this review paper. Thus, adapalene could be a valuable therapeutic drug into the treatment of several types of cancer. Additionally, some neurodegenerative diseases could be treated with a suitable formulation for intravenous administration. The antibacterial activity against methicillin-resistant Staphylococcus aureus of an analogue of ADP has been proven. In different therapeutic schemes, ADP is more effective in combination with other active substances. New topical combinations with adapalene include ketoconazole (antifungal), mometasone furoate (anti-inflammatory corticosteroid), nadifloxacin (fluoroquinolone), and alfa and beta hydroxy acids. Combination with oral drugs is a new trend that enhances the properties of topical formulations with adapalene. Several studies have investigated the effects of ADP in co-administration with azithromycin, doxycycline, faropenem, isotretinoin, and valganciclovir. Innovative formulations of ADP also aim to achieve a better bioavailability, increased efficacy, and reduced side effects. In this review, we have highlighted the current studies on adapalene regarding biological effects useful in various treatment types. Adapalene has not been exploited yet to its full biological potential.

Pharmacological activities and Therapeutic potential of kaempferitrin in medicine for the treatment of human disorders: A review of medicinal importance and health benefits

2021 ◽  
Vol 21 ◽  
Author(s):  
Dinesh Kumar Patel
Keyword(s):  
Broiler Chickens ◽  
Therapeutic Potential ◽  
Scientific Information ◽  
Aloe Vera ◽  
Crocus Sativus ◽  
Related Complication ◽  
Food Material ◽  
Biological Potential ◽  
Anti Oxidant ◽  
Anti Inflammatory

Background: Herbal drugs and their derived phytochemicals are valuable for human being as a source of vital component of food material and drugs. Flavonoids are naturally occurring phytochemical produced in plants through metabolisms and they are having anti-hyperlipidemia, anti-inflammatory, anti-oxidant and anti-apoptotic activity. Flavonoids have been identified in the fruits, nuts, vegetables, seeds, stem, flowers and tea. Kaempferol is a natural flavonoidal compound present in edible plants such as apples, broccoli, strawberries, beans, grapefruit, propolis and medicinal plants such as Aloe vera, Ginkgo biloba, Rosmarinus officinalis, Crocus sativus L., Hypericum perforatum L. Kaempferol have anti-oxidant, anti-inflammatory, anti-apoptotic, pro-apoptotic, cardio-protective and anti-cancer activities. Methods: Glycosides of kaempferol such as kaempferitrin also called kaempferol 3,7-dirhamnoside are known to be more abundant than their flavonoid monomers in plants. Various literature databases have been searched to collect all the scientific information of kaempferitrin in the present investigation and analyzed in order to know the therapeutic benefit and biological potential of kaempferitrin. Moreover all the information has been presented here in two broad sections i.e. pharmacological and analytical. Results: From the analysis of all the collected and presented information, it was found that kaempferitrin has potent insulin-mimetic potential and could be used for the treatment of diabetes and related complication. However, it has also shown anti-oxidant, anti-inflammatory, anti-convulsant, anti-osteoporotic, anti-depressant, anthelmintic, immunostimulatory and natriuretic properties and inhibits cell proliferation and apoptosis. Kaempferitrin also improves meat quality of broiler chickens. Conclusions: The presented information in this work will be valuable to justify the biological importance and therapeutic potential of kaempferitrin in the scientific field.

scholarly journals A Novel Biocompatible Herbal Extract-Loaded Hydrogel for Acne Treatment and Repair

2021 ◽  
Vol 2021 ◽  
pp. 1-13
Author(s):  
Ying-Yi Lin ◽  
Shu-Hsu Lu ◽  
Rong Gao ◽  
Chia-Hung Kuo ◽  
Wen-Hisn Chung ◽  
...  
Keyword(s):  
Raw Materials ◽  
Acne Vulgaris ◽  
Morphological Characteristics ◽  
Zingiber Officinale ◽  
Herbal Extract ◽  
Gravimetric Analysis ◽  
Matrix Properties ◽  
Acne Treatment ◽  
Anti Inflammatory ◽  
Clinical Trial Results

A novel herbal extract-loaded gel containing several biofunctional extracts, including green tea, Zingiber officinale Rosc, Phyllanthus emblica, and salicylic acid, was developed for acne vulgaris. These natural raw materials were blended with suitable dosages of gelatin and carboxymethyl cellulose (CMC) to produce a biocompatible herbal gel. The physical chemistry properties of the hydrogel were determined by Fourier transform infrared spectroscopy (FTIR), thermal gravimetric analysis (TGA), rheometry, and scanning electron microscopy (SEM), and the hydrogel showed good mechanical and morphological characteristics. The herbal extract-loaded hydrogel mimicked extracellular matrix properties and showed good antioxidant and anti-inflammatory properties and various advantages, serving as a potential wound dressing material because of its high moisture retention ability, wound exudate absorption behavior, and biocompatibility. It exhibited moderate-high antioxidative and anti-inflammatory qualities that were important for dermis wound closure. The clinical trial results showed that most patients experienced moderate to high healing rates, and four of twenty-four individuals (16.67%) had recovery area ratios greater than 80%. This herbal extract-loaded hydrogel has effective ingredients and excellent mechanical properties as a bioactive dressing agent for acne treatment.

scholarly journals Therapeutic Potential of Iridoid Derivatives: Patent Review

Inventions ◽  
2019 ◽  
Vol 4 (2) ◽  
pp. 29 ◽  
Author(s):  
Hidayat Hussain ◽  
Ivan R. Green ◽  
Muhammad Saleem ◽  
Muhammad Liaquat Raza ◽  
Mamona Nazir
Keyword(s):  
Therapeutic Potential ◽  
Biological Effects ◽  
Antimalarial Drugs ◽  
Biologically Active ◽  
Future Research ◽  
Patent Review ◽  
Wide Range ◽  
Anti Inflammatory ◽  
Plant Families

Iridoids belong to a family of monoterpenoids comprising the cyclopentan[c]-pyran system; this class of compounds offers a wide range of biological effects, namely antileishmanial, anticancer, antiplasmodial, and anti-inflammatory potency. To date, a large number of biologically active iridoid derivatives have been reported from various plant families, including Rubiaceae, Plantaginaceae, Scrophulariaceae, and Verbenaceae. Furthermore, iridoids have the potential to form conjugates with other anticancer, antidiabetic, antileishmanial, and antimalarial drugs which synergistically have the potential to increase their effects. Additionally, future research should focus on the synthesis of halo analogs as well as preparing homo dimers or heterodimers of iridoids, since these might quite conceivably possess an increased bioactivity.

A Mini Review on Recent Advancements in the Therapeutic Potentials of Benzothiazoles

2019 ◽  
Vol 16 ◽  
Author(s):  
Rubina Bhutani ◽  
Garima Kapoor ◽  
Dharam Pal Pathak ◽  
Asif Husain ◽  
Ravi Kant ◽  
...  
Keyword(s):  
Medicinal Chemistry ◽  
Therapeutic Potential ◽  
Pharmaceutical Chemistry ◽  
Biological Potential ◽  
Heterocyclic Derivatives ◽  
Anti Inflammatory ◽  
Clinical Drugs

: Among the various fused heterocyclic rings, benzothiazole and its analogues have been explored broadly in search of newer therapeutic medicinal agents. The benzothiazole scaffold has been associated with huge biological potential like anticancer, antidiabetic, anti-inflammatory, anti-tubercular, antiviral, anti-convulsant etc. The occurrence of benzothiazole core in various compounds proves its value in the sphere of pharmaceutical chemistry. The connected research and developments in benzothiazole based chemistry become an active topic for medicinal scientists. A large number of benzothiazole and its heterocyclic derivatives are available in the market and used for the treatment of as clinical drugs have been extensively used in practice to treat diverse types of ailments with high therapeutic potential. This review presents the latest therapeutic developments of benzothiazole containing compounds in the medicinal chemistry.

scholarly journals Oxidized Phospholipids in Healthy and Diseased Lung Endothelium

Cells ◽  
2020 ◽  
Vol 9 (4) ◽  
pp. 981 ◽  
Author(s):  
Pratap Karki ◽  
Konstantin G. Birukov
Keyword(s):  
Lung Injury ◽  
Therapeutic Potential ◽  
Biological Effects ◽  
Full Length ◽  
Oxidation Products ◽  
Lipid Mediator ◽  
Oxidized Phospholipids ◽  
Lipid Oxidation Products ◽  
Wide Range ◽  
Anti Inflammatory

Circulating and cell membrane phospholipids undergo oxidation caused by enzymatic and non-enzymatic mechanisms. As a result, a diverse group of bioactive oxidized phospholipids generated in these conditions have both beneficial and harmful effects on the human body. Increased production of oxidized phospholipid products with deleterious effects is linked to the pathogenesis of various cardiopulmonary disorders such as atherosclerosis, thrombosis, acute lung injury (ALI), and inflammation. It has been determined that the contrasting biological effects of lipid oxidation products are governed by their structural variations. For example, full-length products of 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphorylcholine oxidation (OxPAPC) have prominent endothelial barrier protective and anti-inflammatory activities while most of the truncated oxidized phospholipids induce vascular leak and exacerbate inflammation. The extensive studies from our group and other groups have demonstrated a strong potential of OxPAPC in mitigating a wide range of agonist-induced lung injuries and inflammation in pulmonary endothelial cell culture and rodent models of ALI. Concurrently, elevated levels of truncated oxidized phospholipids are present in aged mice lungs that potentiate the inflammatory agents-induced lung injury. On the other hand, increased levels of full length OxPAPC products accelerate ALI recovery by facilitating production of anti-inflammatory lipid mediator, lipoxin A4, and other molecules with anti-inflammatory properties. These findings suggest that OxPAPC-assisted lipid program switch may be a promising therapeutic strategy for treatment of acute inflammatory syndromes. In this review, we will summarize the vascular-protective and deleterious aspects of oxidized phospholipids and discuss their therapeutic potential including engineering of stable analogs of oxidized phospholipids with improved anti-inflammatory and barrier-protective properties.

Peptides with antimicrobial and anti-inflammatory activities that have therapeutic potential for treatment of acne vulgaris

Peptides ◽  
2012 ◽  
Vol 34 (2) ◽  
pp. 275-282 ◽  
Author(s):  
Suzana Popovic ◽  
Edit Urbán ◽  
Miodrag Lukic ◽  
J. Michael Conlon
Keyword(s):  
Therapeutic Potential ◽  
Acne Vulgaris ◽  
Anti Inflammatory

scholarly journals Therapeutic Potential of Ursolic Acid in Cancer and Diabetic Neuropathy Diseases

2021 ◽  
Vol 22 (22) ◽  
pp. 12162
Author(s):  
Manzar Alam ◽  
Sabeeha Ali ◽  
Sarfraz Ahmed ◽  
Abdelbaset Mohamed Elasbali ◽  
Mohd Adnan ◽  
...  
Keyword(s):  
Diabetic Neuropathy ◽  
Ursolic Acid ◽  
Water Solubility ◽  
Therapeutic Potential ◽  
Inflammatory Diseases ◽  
Therapeutic Drug ◽  
Protective Agent ◽  
Cancer Proliferation ◽  
Pentacyclic Triterpenoid ◽  
Anti Inflammatory

Ursolic acid (UA) is a pentacyclic triterpenoid frequently found in medicinal herbs and plants, having numerous pharmacological effects. UA and its analogs treat multiple diseases, including cancer, diabetic neuropathy, and inflammatory diseases. UA inhibits cancer proliferation, metastasis, angiogenesis, and induced cell death, scavenging free radicals and triggering numerous anti- and pro-apoptotic proteins. The biochemistry of UA has been examined broadly based on the literature, with alterations frequently having been prepared on positions C-3 (hydroxyl), C12–C13 (double bonds), and C-28 (carboxylic acid), leading to several UA derivatives with increased potency, bioavailability and water solubility. UA could be used as a protective agent to counter neural dysfunction via anti-oxidant and anti-inflammatory effects. It is a potential therapeutic drug implicated in the treatment of cancer and diabetic complications diseases provide novel machinery to the anti-inflammatory properties of UA. The pharmacological efficiency of UA is exhibited by the therapeutic theory of one-drug → several targets → one/multiple diseases. Hence, UA shows promising therapeutic potential for cancer and diabetic neuropathy diseases. This review aims to discuss mechanistic insights into promising beneficial effects of UA. We further explained the pharmacological aspects, clinical trials, and potential limitations of UA for the management of cancer and diabetic neuropathy diseases.

scholarly journals A vimentin-targeting oral compound with host-directed antiviral and anti-inflammatory actions addresses multiple features of COVID-19 and related diseases

2021 ◽  
Author(s):  
Zhizhen Li ◽  
Jianping Wu ◽  
Ji Zhou ◽  
Baoshi Yuan ◽  
Jiqiao Chen ◽  
...  
Keyword(s):  
Immune Responses ◽  
Cultured Cells ◽  
Therapeutic Potential ◽  
Cellular Protein ◽  
New Drugs ◽  
Lung Damage ◽  
Therapeutic Drug ◽  
Endosomal Trafficking ◽  
Toxic Agent ◽  
Anti Inflammatory

ABSTRACTDamage in COVID-19 results from both the SARS-CoV-2 virus and its triggered overreactive host immune responses. Therapeutic agents that focus solely on reducing viral load or hyperinflammation fail to provide satisfying outcomes in all cases. Although viral and cellular factors have been extensively profiled to identify potential anti-COVID targets, new drugs with significant efficacy remain to be developed. Here, we report the potent preclinical efficacy of ALD-R491, a vimentin-targeting small molecule compound, in treating COVID-19 through its host-directed antiviral and anti-inflammatory actions. We found that by altering the physical properties of vimentin filaments, ALD-491 affected general cellular processes as well as specific cellular functions relevant to SARS-CoV-2 infection. Specifically, ALD-R491 reduced endocytosis, endosomal trafficking, and exosomal release, thus impeding the entry and egress of the virus; increased the microcidal capacity of macrophages, thus facilitating the pathogen clearance; and enhanced the activity of regulatory T cells, therefore suppressing the overreactive immune responses. In cultured cells, ALD-R491 potently inhibited the SARS-CoV-2 spike protein and human ACE2-mediated pseudoviral infection. In aged mice with ongoing, productive SARS-CoV-2 infection, ALD-R491 reduced disease symptoms as well as lung damage. In rats, ALD-R491 also reduced bleomycin-induced lung injury and fibrosis. Our results indicate a unique mechanism and significant therapeutic potential for ALD-R491 against COVID-19. We anticipate that ALD-R491, an oral, fast-acting, and non-toxic agent targeting the cellular protein with multipart actions, will be convenient, safe, and broadly effective, regardless of viral mutations, for patients with early- or late-stage disease, post-COVID complications and other related diseases.IMPORTANCEWith the Delta variant currently fueling a resurgence of new infections in the fully-vaccinated population, developing an effective therapeutic drug is especially critical and urgent in fighting COVID-19. In contrast to the many efforts to repurpose existing drugs or address only one aspect of COVID-19, we are developing a novel agent with first-in-class mechanism-of-actions that address both the viral infection and the overactive immune system in the pathogenesis of the disease. Unlike virus-directed therapeutics that may lose efficacy due to viral mutations and immunosuppressants that require ideal timing to be effective, this agent, with its unique host-directed antiviral and anti-inflammatory actions, can work against all variants of the virus, be effective during all stages of the disease, and even resolve post-disease damage and complications. A further development of the compound will provide an important tool in the fight against COVID-19, its complications, as well as future outbreaks of new viruses.

scholarly journals Antioxidative and Anti-Inflammatory Properties of Cannabidiol

Antioxidants ◽  
2019 ◽  
Vol 9 (1) ◽  
pp. 21 ◽  
Author(s):  
Sinemyiz Atalay ◽  
Iwona Jarocka-Karpowicz ◽  
Elzbieta Skrzydlewska
Keyword(s):  
Cannabinoid Receptors ◽  
Cannabis Sativa ◽  
Therapeutic Potential ◽  
Biological Effects ◽  
Antioxidant Properties ◽  
Endocannabinoid System ◽  
Anti Inflammatory ◽  
Pharmacologically Active ◽  
Preclinical And Clinical Studies ◽  
Synthetic Derivatives

Cannabidiol (CBD) is one of the main pharmacologically active phytocannabinoids of Cannabis sativa L. CBD is non-psychoactive but exerts a number of beneficial pharmacological effects, including anti-inflammatory and antioxidant properties. The chemistry and pharmacology of CBD, as well as various molecular targets, including cannabinoid receptors and other components of the endocannabinoid system with which it interacts, have been extensively studied. In addition, preclinical and clinical studies have contributed to our understanding of the therapeutic potential of CBD for many diseases, including diseases associated with oxidative stress. Here, we review the main biological effects of CBD, and its synthetic derivatives, focusing on the cellular, antioxidant, and anti-inflammatory properties of CBD.

scholarly journals Structural Design, Synthesis and Antioxidant, Antileishmania, Anti-Inflammatory and Anticancer Activities of a Novel Quercetin Acetylated Derivative

Molecules ◽  
2021 ◽  
Vol 26 (22) ◽  
pp. 6923
Author(s):  
Saul Vislei Simões da Silva ◽  
Orlando Maia Barboza ◽  
Jéssica Teles Souza ◽  
Érica Novaes Soares ◽  
Cleonice Creusa dos Santos ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Cell Cultures ◽  
Biological Effects ◽  
Lung Fibroblasts ◽  
C6 Glioma Cells ◽  
Anticancer Activities ◽  
Healthy Human ◽  
Rat Glioma ◽  
Biological Potential ◽  
Anti Inflammatory

Quercetin (Q) is a bioflavonoid with biological potential; however, poor solubility in water, extensive enzymatic metabolism and a reduced bioavailability limit its biopharmacological use. The aim of this study was to perform structural modification in Q by acetylation, thus, obtaining the quercetin pentaacetate (Q5) analogue, in order to investigate the biological potentials (antioxidant, antileishmania, anti-inflammatory and cytotoxicity activities) in cell cultures. Q5 was characterized by FTIR, 1H and 13C NMR spectra. The antioxidant potential was evaluated against the radical ABTS•+. The anti-inflammatory potential was evaluated by measuring the pro-inflammatory cytokine tumor necrosis factor (TNF) and the production of nitric oxide (NO) in peritoneal macrophages from BALB/c mice. Cytotoxicity tests were performed using the AlamarBlue method in cancer cells HepG2 (human hepatocarcinoma), HL-60 (promyelocytic leukemia) and MCR-5 (healthy human lung fibroblasts) as well as the MTT method for C6 cell cultures (rat glioma). Q and Q5 showed antioxidant activity of 29% and 18%, respectively, which is justified by the replacement of hydroxyls by acetyl groups. Q and Q5 showed concentration-dependent reductions in NO and TNF production (p < 0.05); Q and Q5 showed higher activity at concentrations > 40µM when compared to dexamethasone (20 µM). For the HL-60 lineage, Q5 demonstrated selectivity, inducing death in cancer cells, when compared to the healthy cell line MRC-5 (IC50 > 80 µM). Finally, the cytotoxic superiority of Q5 was verified (IC50 = 11 µM), which, at 50 µM for 24 h, induced changes in the morphology of C6 glioma cells characterized by a round body shape (not yet reported in the literature). The analogue Q5 had potential biological effects and may be promising for further investigations against other cell cultures, particularly neural ones.

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