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.

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 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.

Structure-Bioactivity Relationship Study of Xanthene Derivatives: A Brief Review

2020 ◽  
Vol 16 (8) ◽  
pp. 1071-1077
Author(s):  
Aref G. Ghahsare ◽  
Zahra S. Nazifi ◽  
Seyed M.R. Nazifi
Keyword(s):  
Biological Activities ◽  
Cyclic Compound ◽  
Research Field ◽  
Pharmaceutical Chemistry ◽  
Therapeutic Effects ◽  
Main Research ◽  
Research Fields ◽  
Xanthene Derivatives ◽  
Anti Cancer ◽  
Heterocyclic Derivatives

: Over the last decades, several heterocyclic derivatives compounds have been synthesized or extracted from natural resources and have been tested for their pharmaceutical activities. Xanthene is one of these heterocyclic derivatives. These compounds consist of an oxygen-containing central heterocyclic structure with two more cyclic structures fused to the central cyclic compound. It has been shown that xanthane derivatives are bioactive compounds with diverse activities such as anti-bacterial, anti-fungal, anti-cancer, and anti-inflammatory as well as therapeutic effects on diabetes and Alzheimer. The anti-cancer activity of such compounds has been one of the main research fields in pharmaceutical chemistry. Due to this diverse biological activity, xanthene core derivatives are still an attractive research field for both academia and industry. This review addresses the current finding on the biological activities of xanthene derivatives and discussed in detail some aspects of their structure-activity relationship (SAR).

scholarly journals A Comprehensive Review of the Ethnotraditional Uses and Biological and Pharmacological Potential of the Genus Mimosa

2021 ◽  
Vol 22 (14) ◽  
pp. 7463
Author(s):  
Ismat Majeed ◽  
Komal Rizwan ◽  
Ambreen Ashar ◽  
Tahir Rasheed ◽  
Ryszard Amarowicz ◽  
...  
Keyword(s):  
Web Of Science ◽  
Scientific Literature ◽  
Therapeutic Potential ◽  
Current Knowledge ◽  
Folk Medicine ◽  
Nutritional Values ◽  
Biological Potential ◽  
The World ◽  
The Future ◽  
Pharmacological Potential

The Mimosa genus belongs to the Fabaceae family of legumes and consists of about 400 species distributed all over the world. The growth forms of plants belonging to the Mimosa genus range from herbs to trees. Several species of this genus play important roles in folk medicine. In this review, we aimed to present the current knowledge of the ethnogeographical distribution, ethnotraditional uses, nutritional values, pharmaceutical potential, and toxicity of the genus Mimosa to facilitate the exploitation of its therapeutic potential for the treatment of human ailments. The present paper consists of a systematic overview of the scientific literature relating to the genus Mimosa published between 1931 and 2020, which was achieved by consulting various databases (Science Direct, Francis and Taylor, Scopus, Google Scholar, PubMed, SciELO, Web of Science, SciFinder, Wiley, Springer, Google, The Plant Database). More than 160 research articles were included in this review regarding the Mimosa genus. Mimosa species are nutritionally very important and several species are used as feed for different varieties of chickens. Studies regarding their biological potential have shown that species of the Mimosa genus have promising pharmacological properties, including antimicrobial, antioxidant, anticancer, antidiabetic, wound-healing, hypolipidemic, anti-inflammatory, hepatoprotective, antinociceptive, antiepileptic, neuropharmacological, toxicological, antiallergic, antihyperurisemic, larvicidal, antiparasitic, molluscicidal, antimutagenic, genotoxic, teratogenic, antispasmolytic, antiviral, and antivenom activities. The findings regarding the genus Mimosa suggest that this genus could be the future of the medicinal industry for the treatment of various diseases, although in the future more research should be carried out to explore its ethnopharmacological, toxicological, and nutritional attributes.

scholarly journals Biological Properties and Prospects for the Application of Eugenol—A Review

2021 ◽  
Vol 22 (7) ◽  
pp. 3671
Author(s):  
Magdalena Ulanowska ◽  
Beata Olas
Keyword(s):  
Body Weight ◽  
Aromatic Compound ◽  
Therapeutic Potential ◽  
Antioxidant Properties ◽  
Biological Properties ◽  
Clove Oil ◽  
Current State ◽  
Potential Component ◽  
Anti Inflammatory ◽  
High Concentrations

Eugenol is a phenolic aromatic compound obtained mainly from clove oil. Due to its known antibacterial, antiviral, antifungal, anticancer, anti-inflammatory and antioxidant properties, it has long been used in various areas, such as cosmetology, medicine, and pharmacology. However, high concentrations can be toxic. A dose of 2.5 mg/kg body weight is regarded as safe. This paper reviews the current state of knowledge regarding the activities and application of eugenol and its derivatives and recent research of these compounds. This review is based on information concerning eugenol characteristics and recent research from articles in PubMed. Eugenol remains of great interest to researchers, since its multidirectional action allows it to be a potential component of drugs and other products with therapeutic potential against a range of diseases.

scholarly journals Dibenzoylthiamine Has Powerful Antioxidant and Anti-Inflammatory Properties in Cultured Cells and in Mouse Models of Stress and Neurodegeneration

Biomedicines ◽  
2020 ◽  
Vol 8 (9) ◽  
pp. 361
Author(s):  
Margaux Sambon ◽  
Anna Gorlova ◽  
Alice Demelenne ◽  
Judit Alhama-Riba ◽  
Bernard Coumans ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Neurodegenerative Diseases ◽  
Cell Line ◽  
Mouse Models ◽  
Cultured Cells ◽  
Therapeutic Potential ◽  
Motor Dysfunction ◽  
Oxidative Stress Marker ◽  
Bv2 Cells ◽  
Anti Inflammatory

Thiamine precursors, the most studied being benfotiamine (BFT), have protective effects in mouse models of neurodegenerative diseases. BFT decreased oxidative stress and inflammation, two major characteristics of neurodegenerative diseases, in a neuroblastoma cell line (Neuro2a) and an immortalized brain microglial cell line (BV2). Here, we tested the potential antioxidant and anti-inflammatory effects of the hitherto unexplored derivative O,S-dibenzoylthiamine (DBT) in these two cell lines. We show that DBT protects Neuro2a cells against paraquat (PQ) toxicity by counteracting oxidative stress at low concentrations and increases the synthesis of reduced glutathione and NADPH in a Nrf2-independent manner. In BV2 cells activated by lipopolysaccharides (LPS), DBT significantly decreased inflammation by suppressing translocation of NF-κB to the nucleus. Our results also demonstrate the superiority of DBT over thiamine and other thiamine precursors, including BFT, in all of the in vitro models. Finally, we show that the chronic administration of DBT arrested motor dysfunction in FUS transgenic mice, a model of amyotrophic lateral sclerosis, and it reduced depressive-like behavior in a mouse model of ultrasound-induced stress in which it normalized oxidative stress marker levels in the brain. Together, our data suggest that DBT may have therapeutic potential for brain pathology associated with oxidative stress and inflammation by novel, coenzyme-independent mechanisms.

scholarly journals In Vitro Evaluation of the Anti-Inflammatory Effect of KMUP-1 and in Vivo Analysis of Its Therapeutic Potential in Osteoarthritis

Biomedicines ◽  
2021 ◽  
Vol 9 (6) ◽  
pp. 615
Author(s):  
Shang-En Huang ◽  
Erna Sulistyowati ◽  
Yu-Ying Chao ◽  
Bin-Nan Wu ◽  
Zen-Kong Dai ◽  
...  
Keyword(s):  
Articular Cartilage ◽  
Inflammatory Responses ◽  
Therapeutic Potential ◽  
Antioxidant Properties ◽  
Serum Levels ◽  
Gene Expressions ◽  
Tnf Α ◽  
Anti Inflammatory

Osteoarthritis is a degenerative arthropathy that is mainly characterized by dysregulation of inflammatory responses. KMUP-1, a derived chemical synthetic of xanthine, has been shown to have anti-inflammatory and antioxidant properties. Here, we aimed to investigate the in vitro anti-inflammatory and in vivo anti-osteoarthritis effects of KMUP-1. Protein and gene expressions of inflammation markers were determined by ELISA, Western blotting and microarray, respectively. RAW264.7 mouse macrophages were cultured and pretreated with KMUP-1 (1, 5, 10 μM). The productions of TNF-α, IL-6, MMP-2 and MMP- 9 were reduced by KMUP-1 pretreatment in LPS-induced inflammation of RAW264.7 cells. The expressions of iNOS, TNF-α, COX-2, MMP-2 and MMP-9 were also inhibited by KMUP-1 pretreatment. The gene expression levels of TNF and COX families were also downregulated. In addition, KMUP-1 suppressed the activations of ERK, JNK and p38 as well as phosphorylation of IκBα/NF-κB signaling pathways. Furthermore, SIRT1 inhibitor attenuated the inhibitory effect of KMUP-1 in LPS-induced NF-κB activation. In vivo study showed that KMUP-1 reduced mechanical hyperalgesia in monoiodoacetic acid (MIA)-induced rats OA. Additionally, KMUP-1 pretreatment reduced the serum levels of TNF-α and IL-6 in MIA-injected rats. Moreover, macroscopic and histological observation showed that KMUP-1 reduced articular cartilage erosion in rats. Our results demonstrated that KMUP-1 inhibited the inflammatory responses and restored SIRT1 in vitro, alleviated joint-related pain and cartilage destruction in vivo. Taken together, KMUP-1 has the potential to improve MIA-induced articular cartilage degradation by inhibiting the levels and expression of inflammatory mediators suggesting that KMUP-1 might be a potential therapeutic agent for OA.

MAPK/AP-1-Targeted Anti-Inflammatory Activities of Xanthium strumarium

2016 ◽  
Vol 44 (06) ◽  
pp. 1111-1125 ◽  
Author(s):  
Muhammad Jahangir Hossen ◽  
Mi-Yeon Kim ◽  
Jae Youl Cho
Keyword(s):  
Mouse Model ◽  
Therapeutic Potential ◽  
Inflammatory Diseases ◽  
Elevated Serum ◽  
Human Monocyte ◽  
Serum Levels ◽  
Mitogen Activated Protein Kinase ◽  
Xanthium Strumarium ◽  
U937 Cells ◽  
Anti Inflammatory

Xanthium strumarium L. (Asteraceae), a traditional Chinese medicine, is prescribed to treat arthritis, bronchitis, and rhinitis. Although the plant has been used for many years, the mechanism by which it ameliorates various inflammatory diseases is not yet fully understood. To explore the anti-inflammatory mechanism of methanol extracts of X. strumarium (Xs-ME) and its therapeutic potential, we used lipopolysaccharide (LPS)-stimulated murine macrophage-like RAW264.7 cells and human monocyte-like U937 cells as well as a LPS/D-galactosamine (GalN)-induced acute hepatitis mouse model. To find the target inflammatory pathway, we used holistic immunoblotting analysis, reporter gene assays, and mRNA analysis. Xs-ME significantly suppressed the up-regulation of both the activator protein (AP)-1-mediated luciferase activity and the production of LPS-induced proinflammatory cytokines, including interleukin (IL)-1[Formula: see text], IL-6, and tumor necrosis factor (TNF)-[Formula: see text]. Moreover, Xs-ME strongly inhibited the phosphorylation of mitogen-activated protein kinase (MAPK) in LPS-stimulated RAW264.7 and U937 cells. Additionally, these results highlighted the hepatoprotective and curative effects of Xs-ME in a mouse model of LPS/D-GalN-induced acute liver injury, as assessed by elevated serum levels of aspartate aminotransferase (AST) and alanine aminotransferase (ALT), and histological damage. Therefore, our results strongly suggest that the ethnopharmacological roles of Xs-ME in hepatitis and other inflammatory diseases might result from its inhibitory activities on the inflammatory signaling of MAPK and AP-1.

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