Traditional uses, biological activities, and phytochemicals of Lecaniodiscus cupanioides: a review

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Olusesan Ojo ◽  
Derek T. Ndinteh
Keyword(s):  
Skin Infection ◽  
Biological Activities ◽  
Therapeutic Agents ◽  
Mechanisms Of Action ◽  
Active Components ◽  
Active Constituents ◽  
Medicinal Tree ◽  
Drug Candidates ◽  
Solid Foundation ◽  
Ethnomedicinal Uses

Abstract Medicinal plants are indispensable source of therapeutic agents, and have proved to be “warehouse” of lead drug candidates. Lecaniodiscus cupanioides Planch. ex Benth is a medicinal tree plant that is extensively distributed in both Asia and Africa. The species has many ethnomedicinal uses in the treatment of fever, cough, typhoid, wound, skin infection, measles, jaundice, diabetes, sexual dysfunction, cancer, bone fracture, and as galactogogues. In the recent decades, the extracts and phytochemicals of L. cupanioides have been investigated to possess antibacterial, anticancer, aphrodisiac, antifungal, cytotoxic, antidiabetic, antiprotozoal, antioxidant, antidiarrhoeal, analgesic and ameliorative properties. However, triterpenoids which have been linked to its anticancer and antifungal actions, are the only isolated active constituents identified from the species despite the results of the phytochemical screenings and reported biological activities. Moreover, the mechanisms of action of the extracts and active components are yet to be fully elucidated. This paper provides a general review on the ethnomedicinal, phytochemicals, and biological activities of L. cupanioides, and lays a solid foundation for future investigations on the plant.

P1 Receptor Agonists/Antagonists in Clinical Trials - Potential Drug Candidates of the Future

2019 ◽  
Vol 25 (26) ◽  
pp. 2792-2807 ◽  
Author(s):  
Pobitra Borah ◽  
Satyendra Deka ◽  
Raghu Prasad Mailavaram ◽  
Pran Kishore Deb
Keyword(s):  
Clinical Trials ◽  
Biological Activities ◽  
Therapeutic Agents ◽  
Current Status ◽  
Preclinical Studies ◽  
P1 Receptors ◽  
Drug Candidates ◽  
Wide Range ◽  
P1 Receptor ◽  
Novel Therapeutic

Background: Adenosine mediates various physiological and pathological conditions by acting on its four P1 receptors (A1, A2A, A2B and A3 receptors). Omnipresence of P1 receptors and their activation, exert a wide range of biological activities. Thus, its modulation is implicated in various disorders like Parkinson’s disease, asthma, cardiovascular disorders, cancer etc. Hence these receptors have become an interesting target for the researchers to develop potential therapeutic agents. Number of molecules were designed and developed in the past few years and evaluated for their efficacy in various disease conditions. Objective: The main objective is to provide an overview of new chemical entities which have crossed preclinical studies and reached clinical trials stage following their current status and future prospective. Methods: In this review we discuss current status of the drug candidates which have undergone clinical trials and their prospects. Results: Many chemical entities targeting various subtypes of P1 receptors are patented; twenty of them have crossed preclinical studies and reached clinical trials stage. Two of them viz adenosine and regadenoson are approved by the Food and Drug Administration. Conclusion: This review is an attempt to highlight the current status, progress and probable future of P1 receptor ligands which are under clinical trials as promising novel therapeutic agents and the direction in which research should proceed with a view to come out with novel therapeutic agents.

Phytochemistry and Pharmacology of Ferula hermonis Boiss. – A Review

Drug Research ◽  
2017 ◽  
Vol 67 (08) ◽  
pp. 437-446 ◽  
Author(s):  
Zohreh Sattar ◽  
Mehrdad Iranshahi
Keyword(s):  
Erectile Dysfunction ◽  
Estrogen Receptors ◽  
Biological Activities ◽  
Mechanisms Of Action ◽  
Active Constituents ◽  
Beneficial Effects ◽  
Clinical Investigations ◽  
Prevention Of Osteoporosis ◽  
Agonistic Activity ◽  
Underlying Mechanisms

AbstractFerula hermonis, a well-known species of the genus Ferula found in Lebanon and Syria, has a brilliant history in traditional medicine as it has been used for the treatment of erectile dysfunction in men and menopausal disturbances in women. Thanks to modern pharmacological and clinical investigations, F. hermonis is a valuable medicinal and condimental plant that may be used for the treatment of impotence and diabetes, the prevention of osteoporosis, and possesses anti-microbial and anti-inflammatory properties. Phytochemical investigations have shown that this plant contains daucane aryl esters such as ferutinin, which has exhibited various biological activities including hypoglycemic and estrogenic activities. Ferutinin is one of the strongest natural phytoestrogen which has agonistic activity on estrogen receptors, particularly α receptor. It seems that ferutinin and its derivatives play an important role in F. hermonis biological activities, mainly the beneficial effects of this plant on impotence, diabetes and osteoporosis. The present review discusses the available data on the active constituents and biological activities of F. hermonis and their possible underlying mechanisms of action.

Extraction, isolation and characterization of Bauhinia variegata flower

2020 ◽  
pp. 9-12
Author(s):  
Akanksha Gupta ◽  
Abhishek K Tripathi ◽  
Pushpraj S Gupta
Keyword(s):  
Biological Activities ◽  
Molecular Formula ◽  
Native Plant ◽  
Compound A ◽  
Active Constituents ◽  
Chromatographic Techniques ◽  
Isolation And Characterization ◽  
Soxhlet Apparatus ◽  
Bauhinia Variegata

Background: Bauhinia variegata Linn. is a native plant of Asia and China. B. variegata is found in tropical regions of the world. It belongs to family Leguminosae. It is used for diarrhea, hemorrhoids, constipation, piles, edema, leprosy, wounds, tumors, etc.  Objective: The objective of the present study was to perform extraction of B. variegata flower and isolation of active constituents from the extract. Materials and Methods: The ethanolic extraction of B. variegata flower was performed using the Soxhlet apparatus. The isolation of active constituents from the extract was performed using chromatographic techniques. In column chromatographic studies, n-hexane- [dichloromethane (DCM)] (2:8) was used as an eluting system and further purified through thin layer chromatography (TLC). Compound A and B were isolated through chromatographic techniques, then the molecular formula and characterization of these compounds were carried out with mass and infrared (IR) spectral analysis. Results and Discussion: The percentage yield of B. variegata ethanolic extract (BVE) was found to be 20.8% w/w. The different fractions were F1 having 12.5 grams with n-hexane, F2 (17.1 grams) with CH2Cl2, F3 (21.2 grams) with EtOAc, and F4 (13.4 grams) with EtOH. Compound A and B were isolated from the solvent fractions of n-hexane-DCM (2:8) and EtOAc-DCM (1:9), respectively. The compound A was characterized as 3-hydroxy-6-methoxy-2-phenyl-4H-chromen-4-one. The compound B was characterized as 3-hydroxy-6-methyl-2-phenyl-4H-chromen-4-one. Conclusion: Thus, B. variegata flowers possess active components that need to identify their biological activities.

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.

Click Reactions in Chemistry of Triterpenes - Advances Towards Development of Potential Therapeutics

2018 ◽  
Vol 25 (5) ◽  
pp. 636-658 ◽  
Author(s):  
Jan Pokorny ◽  
Lucie Borkova ◽  
Milan Urban
Keyword(s):  
Biological Activities ◽  
Synthetic Approach ◽  
Clinical Use ◽  
New Approach ◽  
Click Reactions ◽  
Drug Candidates ◽  
The Past ◽  
Low Toxicity ◽  
New Compounds ◽  
Potential Therapeutics

Triterpenoids are natural compounds with a large variety of biological activities such as anticancer, antiviral, antibacterial, antifungal, antiparazitic, antiinflammatory and others. Despite their low toxicity and simple availability from the natural resources, their clinical use is still severely limited by their higher IC50 and worse pharmacological properties than in the currently used therapeutics. This fact encouraged a number of researchers to develop new terpenic derivatives more suitable for the potential clinical use. This review summarizes a new approach to improve both, the activity and ADME-Tox properties by connecting active terpenes to another modifying molecules using click reactions. Within the past few years, this synthetic approach was well explored yielding a lot of great improvements of the parent compounds along with some less successful attempts. A large quantity of the new compounds presented here are superior in both activity and ADME-Tox properties to their parents. This review should serve the researchers who need to promote their hit triterpenic structures towards their clinical use and it is intended as a guide for the chemical synthesis of better drug candidates.

Current Status in the Design and Development of Agonists and Antagonists of Adenosine A3 Receptor as Potential Therapeutic Agents

2019 ◽  
Vol 25 (25) ◽  
pp. 2772-2787 ◽  
Author(s):  
Raghu P. Mailavaram ◽  
Omar H.A. Al-Attraqchi ◽  
Supratik Kar ◽  
Shinjita Ghosh
Keyword(s):  
Drug Target ◽  
Therapeutic Agents ◽  
G Protein Coupled Receptors ◽  
Current Status ◽  
Renal Diseases ◽  
Adenosine A3 Receptor ◽  
Drug Candidates ◽  
Novel Drugs ◽  
The Family ◽  
G Protein Coupled

Adenosine receptors (ARs) belongs to the family of G-protein coupled receptors (GPCR) that are responsible for the modulation of a wide variety of physiological functions. The ARs are also implicated in many diseases such as cancer, arthritis, cardiovascular and renal diseases. The adenosine A3 receptor (A3AR) has emerged as a potential drug target for the progress of new and effective therapeutic agents for the treatment of various pathological conditions. This receptor’s involvement in many diseases and its validity as a target has been established by many studies. Both agonists and antagonists of A3AR have been extensively investigated in the last decade with the goal of developing novel drugs for treating diseases related to immune disorders, inflammation, cancer, and others. In this review, we shall focus on the medicinal chemistry of A3AR ligands, exploring the diverse chemical classes that have been projected as future leading drug candidates. Also, the recent advances in the therapeuetic applications of A3AR ligands are highlighted.

Synthesis and Biological Activity of Quaternary Quinolinium Salts: A Review

2020 ◽  
Vol 23 (21) ◽  
pp. 2271-2294 ◽  
Author(s):  
Divya Utreja ◽  
Shivali Sharma ◽  
Akhil Goyal ◽  
Komalpreet Kaur ◽  
Sonia Kaushal
Keyword(s):  
Tyrosine Kinases ◽  
Biological Activities ◽  
Polymeric Materials ◽  
Tubulin Polymerization ◽  
Quinoline Derivatives ◽  
Heterocyclic Chemistry ◽  
Biological Profile ◽  
Drug Candidates ◽  
Anti Hiv ◽  
Quinolinium Salts

Heterocyclic chemistry is the only branch of chemistry that has applications in varied areas such as dyes, photosensitizers, coordination compounds, polymeric materials, biological, and many other fields. Quinoline and its derivatives have always engrossed both synthetic chemists and biologists because of their diverse chemical and pharmacological properties as these ring systems can be easily found in various natural products, especially in alkaloids. Among alkaloids, quinoline derivatives i.e. quinolinium salts have attracted much attention nowadays owing to their diverse biological profile such as antimicrobial, antitumor, antifungal, hypotensive, anti-HIV, analgesics and anti-inflammatory, etc. Quinoline and its analogs have recently been examined for their modes of function in the inhibition of tyrosine kinases, proteasome, tubulin polymerization, topoisomerase, and DNA repair. These observations have been guiding scientists for the expansion of new quinoline derivatives with improved and varied biological activities. Quinolinium salts have immense possibilities and scope to investigate these compounds as potential drug candidates. Therefore, we shall present a concise compilation of this work to aid in present knowledge and to help researchers explore an interesting quinoline class having medicinal potential.

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 Modern Synthetic Methods for the Stereoselective Construction of 1,3-Dienes

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 249
Author(s):  
Raquel G. Soengas ◽  
Humberto Rodríguez-Solla
Keyword(s):  
Organic Chemistry ◽  
Natural Products ◽  
Functional Group ◽  
Biological Activities ◽  
Synthetic Methods ◽  
Bond Forming ◽  
Drug Candidates ◽  
The Past ◽  
Wide Range

The 1,3-butadiene motif is widely found in many natural products and drug candidates with relevant biological activities. Moreover, dienes are important targets for synthetic chemists, due to their ability to give access to a wide range of functional group transformations, including a broad range of C-C bond-forming processes. Therefore, the stereoselective preparation of dienes have attracted much attention over the past decades, and the search for new synthetic protocols continues unabated. The aim of this review is to give an overview of the diverse methodologies that have emerged in the last decade, with a focus on the synthetic processes that meet the requirements of efficiency and sustainability of modern organic chemistry.

scholarly journals Hepatoprotective Effect of Mixture of Dipropyl Polysulfides in Concanavalin A-Induced Hepatitis

Nutrients ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 1022
Author(s):  
Dragana Arsenijevic ◽  
Bojana Stojanovic ◽  
Jelena Milovanovic ◽  
Aleksandar Arsenijevic ◽  
Milos Simic ◽  
...  
Keyword(s):  
Concanavalin A ◽  
Messenger Rna ◽  
T Regulatory Cells ◽  
Mononuclear Cells ◽  
Biological Activities ◽  
Biologically Active ◽  
Organosulfur Compounds ◽  
Liver Inflammation ◽  
Regulatory Cells ◽  
Active Components

The main biologically active components of plants belonging to the genus Allium, responsible for their biological activities, including anti-inflammatory, antioxidant and immunomodulatory, are organosulfur compounds. The aim of this study was to synthetize the mixture of dipropyl polysulfides (DPPS) and to test their biological activity in acute hepatitis. C57BL/6 mice were administered orally with DPPS 6 h before intravenous injection of Concanavalin A (ConA). Liver inflammation, necrosis and hepatocytes apoptosis were determined by histological analyses. Cytokines in liver tissue were determined by ELISA, expression of adhesive molecules and enzymes by RT PCR, while liver mononuclear cells were analyzed by flow cytometry. DPPS pretreatment significantly attenuated liver inflammation and injury, as evidenced by biochemical and histopathological observations. In DPPS-pretreated mice, messenger RNA levels of adhesion molecules and NADPH oxidase complex were significantly reduced, while the expression of SOD enzymes was enhanced. DPPS pretreatment decreased protein level of inflammatory cytokines and increased percentage of T regulatory cells in the livers of ConA mice. DPPS showed hepatoprotective effects in ConA-induced hepatitis, characterized by attenuation of inflammation and affection of Th17/Treg balance in favor of T regulatory cells and implicating potential therapeutic usage of DPPS mixture in inflammatory liver diseases.

Sign in / Sign up

Export Citation Format

Share Document