Embelin: A potential Benzoquinone

2017 ◽  
Vol 8 (03) ◽  
Author(s):  
Shyam Baboo Prasad
Keyword(s):  
Wound Healing ◽  
Drug Development ◽  
Anxiolytic Activity ◽  
Present Review ◽  
Pharmacological Activities ◽  
Wide Range ◽  
Myrsine Africana

Embelin is a benzoquinone compound, present mainly in Embelia species. Embelin is also reported in Lysimachia punctate, Ardisia humilis, Rapanea umbellate, Cannarus richiei, Myrsine Africana and Myrsine capitellata. Embelin has demonstrated wide range of pharmacological activities including; antidepressant, anticancer, antifertility, antidiabetic, antioxidant and analgesic. Embelin shown other activities also such as antihyperlipidemic, antifungal, antihyperhomocysteinemic, anthelminthic, anticonvulsant, antibacterial, hepatoprotective, wound healing and anxiolytic activity. Recent studies, have thrown light on anti-arthritis and antiulcer activities of the benzoquinone. The present review, discusses pharmacological investigations on embelin, with potential for drug-development.

Novel GABAA Agonist Entities: Pharmacological Investigation and Molecular Modeling Study of Thiazolo- and Thiadiazolo-[3,2-a][1,3] diazepine Analogs

2020 ◽  
Vol 21 ◽  
Author(s):  
Hussein I. El-Subbagh
Keyword(s):  
Molecular Modeling ◽  
Drug Development ◽  
Biological Evaluation ◽  
Neuromuscular Blocking ◽  
Present Review ◽  
Pharmacological Investigation ◽  
Important Class ◽  
Pharmacological Activities ◽  
Short Acting ◽  
New Drug Development

Abstract:: Thiazolo- and thiadiazolo-[3,2-a][1,3]diazepines and their patented derivatives, tested with diverse CNS pharmacological activities, constitute an important class of compounds for new drug development. Therefore, research efforts were continued to design, synthesize, and evaluate compounds for their ultra-short, short-acting hypnotic, anticonvulsant, and neuromuscular blocking activities. The present review provides a summary of the work accomplished by these heterocycles and their biological evaluation.

scholarly journals New Pharmacological Opportunities for Betulinic Acid

Planta Medica ◽  
2017 ◽  
Vol 84 (01) ◽  
pp. 8-19 ◽  
Author(s):  
José Ríos ◽  
Salvador Máñez
Keyword(s):  
Metabolic Syndrome ◽  
Natural Product ◽  
Betulinic Acid ◽  
Therapeutic Potential ◽  
Present Review ◽  
Antitumor Effects ◽  
Pharmacological Activities ◽  
Naturally Occurring ◽  
Wide Range ◽  
Birch Trees

AbstractBetulinic acid is a naturally occurring pentacyclic lupane-type triterpenoid usually isolated from birch trees, but present in many other botanical sources. It is found in different plant organs, both as a free aglycon and as glycosyl derivatives. A wide range of pharmacological activities has been described for this triterpenoid, including antiviral and antitumor effects. In addition, several other interesting properties have been identified in the fields of immunity and metabolism, namely antidiabetic, antihyperlipidemic, and anti-inflammatory activities. Taken together, these latter three properties make betulinic acid a highly interesting prospect for treating metabolic syndrome. The present review focuses on the therapeutic potential of this agent, along with several of its semisynthetic derivatives, which could open new frontiers in the use of natural product-based medicines.

scholarly journals EXTRACTION, ISOLATION OF ACTIVE PRINCIPLES, ANTI-BACTERIAL AND WOUND HEALING ACTIVITY OF THE MARINE ALGAL SPECIES OEDOGONIUM GLOBOSUM AND OEDOGONIUM INTERMEDIUM

2021 ◽  
pp. 72-77
Author(s):  
KARPAKAVALLI MEENAKSHISUNDARAM ◽  
PRAKASH GOVINDARAJ ◽  
SIVASUBRAMANIAM P. ◽  
RANJITHKUMAR DHANARAJ ◽  
MOHAN SELLAPPAN
Keyword(s):  
Wound Healing ◽  
Research Work ◽  
Algal Species ◽  
Raw Material ◽  
Spectral Studies ◽  
Pharmacological Activities ◽  
Methanolic Extracts ◽  
Wide Range ◽  
Marine Algal ◽  
Wound Healing Activity

Objective: Algae is the undisputed treasures of the sea and are a valuable raw material, providing unlimited opportunities for new drug discoveries. Marine algal products are in demand in the international market in the form of standardized algal extracts or semi-finished products. Methods: Aqueous and methanolic extracts of Oedogonium globosum and Oedogonium intermedium species were obtained maceration and hot percolation. The active principles from O. intermedium were isolated, purified by column chromatography, and characterized by spectral studies IR, λmax, 1HNMR and MS. The extracts of Oedogonium species were screened for their anti-microbial effects, acute dermal irritation and wound-healing activity studies. Results: Comparing to Oedogonium intermedium (45 %, 90 %, 87 %), very low extractive yields were obtained for Oedogonium globosum (10.80 %, 37 %, 28 %). At phytochemical screening, Terpenoids, Flavanoids and, Glycans were found to be present in a significant amount and upon their isolation, it was found that a collection of fractions from cold extract with Rf value in the range 0.32-0.34 as Glycans and those from the hot extract with 0.40-0.72 as Flavanoids and those from methanolic extracts with 0.23, 0.44 and 0.71 as for Terpenoids. Anti-bacterial study revealed out the fact of Oedogonium species could give higher inhibition to gram-positive than for gram-negative bacteria at (10 μg/10μl/disc) concentration. No symptoms of systemic toxicity and mortality were observed. Silver sulfadiazine, more potent in wound closure, the effect of methanolic extracts of O. intermedium (87 %) was almost at par to the standard (95 %) in action and significantly greater than O. globosum (72 %, P<0.05). Conclusion: Admittedly, Oedogonium type algal species can be known as medicinal algae with a plethora of a wide range of pharmacological activities. Thus, this research work may be considered further for extensive innovative discoveries of new lead molecules and any other pharmacological activities, in the future.

scholarly journals Bioactivity of Torch Ginger Umbut Extract (Etlingera elatior) Against Heal Wounds of Mice (Mus musculus)

2020 ◽  
Vol 21 (2) ◽  
pp. 124-130
Author(s):  
Mhd Zalil Efendi ◽  
Ramadhan Sumarmin ◽  
M. Syukri Fadil
Keyword(s):  
Wound Healing ◽  
Adult Male ◽  
Mus Musculus ◽  
Male Mice ◽  
Pharmacological Activities ◽  
Active Compounds ◽  
Randomized Design ◽  
Wide Range ◽  
Completely Randomized Design ◽  
Etlingera Elatior

Torch ginger has a wide range of good antimicrobial, antioxidant, anticancer, larvicidal and repellent activities. Active compounds in Torch ginger that affect pharmacological activities are phenols, polyphenols, flavonoids, and terpenoids. Based on these ingredients Torch ginger can be used to heal wounds. This study aims to observe the effect of Torch ginger Umbut extract on wound healing in mice. This study hopes to add information about the effect of Torch ginger umbut extract on the healing of cuts in mice so that it can be another alternative for wound healing and can be a reference for other researchers. This study used a completely randomized design with 5 treatments and 3 replications. Tests carried out on adult male mice. The results showed that the optimal wound healing in P2 is treatment with 10% Torch ginger umbut extract which requires a range of wound healing 7-8 days. Based on these results, Torch ginger umbut extract can heal wounds.

Ethnomedicinal Uses, Phytochemistry and Pharmacology of Carica papaya Plant: A Compendious Review

2019 ◽  
Vol 16 (5) ◽  
pp. 463-480 ◽  
Author(s):  
Manpreet Kaur ◽  
Naveen Chandra Talniya ◽  
Seema Sahrawat ◽  
Arvind Kumar ◽  
Elena E. Stashenko
Keyword(s):  
Carica Papaya ◽  
Therapeutic Potential ◽  
Industrial Applications ◽  
Present Review ◽  
Future Research ◽  
Pharmacological Activities ◽  
Traditional System ◽  
Wide Range ◽  
Microbial Infections ◽  
Ethnomedicinal Uses

Medicinal properties of papaya (Carica papaya Linn.) fruit and other parts are wellknown in the traditional system of medicine. Papaya plant originated in Central America and now grown in tropical areas of worldwide, most particularly in Africa and Asia. Studies validate that, papaya has several pharmacological activities, such as antioxidant, antiulcer, antibacterial, woundhealing, anti-inflammatory and anti-sickling, just to name a few. The present review article provides the explicit and updated information on botanical aspects, ethnomedicinal uses, phytochemistry and pharmacological activities of C. papaya plant in order to explore their therapeutic potential. This review conducted a systematic search on C. papaya through electronic database search (Google Scholar, PubMed, SciFinder, Scopus, Science Direct, and Web of Science) and a library search for articles published in peer-reviewed journals, until January of 2018. Constituents of papaya plant belongs to different chemical classes that include alkaloids, flavonoids, terpenoids, saponins, steroids, tannin, vitamins, quinones, minerals and others. Experimental evidence confirmed that these classes of compounds cure the microbial infections, diabetes, inflammatory, cytotoxic and liver disorders. Conclusively, the present review aimed to summarize the information of ethnomedicinal uses, phytochemistry and pharmacological activities to prevent and treat the wide range of diseases and disorders. The future research draws the attention of the researcher for intensive investigations relating to phytochemicals, pharmacological activities and industrial applications.

Therapeutic Potential of Cinnoline Core: A Comprehensive Review

2020 ◽  
Vol 20 (3) ◽  
pp. 196-218
Author(s):  
Rajiv K. Tonk ◽  
Sandhya Bawa ◽  
Deepak Kumar
Keyword(s):  
Heterocyclic Compounds ◽  
Therapeutic Potential ◽  
Biological Properties ◽  
Present Review ◽  
Natural Occurrence ◽  
Pharmacological Activities ◽  
Comprehensive Review ◽  
Wide Range ◽  
The Family ◽  
Almost All

Cinnoline or Benzo-pyridazine has its place in the family of fairly well-known benzfuseddiazine heterocycles. Because of its natural occurrence and synthetic exploration, cinnoline compounds validated its thought-provoking bioactivity through a number of research publications and patents during last few decades. A creative consideration has been rewarded to the synthesis of cinnoline based heterocyclic compounds, mostly due to their wide range of diverse pharmacological activities. The present review covers the principle approaches to the synthesis of cinnoline nucleus and almost all biological properties of 115 cinnoline derivatives reported during the last 65 years from natural and synthetic origin with 140 references.

Extending the Applicability of the ANI Deep Learning Molecular Potential to Sulfur and Halogens

2020 ◽  
Author(s):  
Christian Devereux ◽  
Justin Smith ◽  
Kate Davis ◽  
Kipton Barros ◽  
Roman Zubatyuk ◽  
...  
Keyword(s):  
Drug Development ◽  
Autonomous Vehicles ◽  
Potential Energy Surfaces ◽  
Organic Molecules ◽  
Chemical Elements ◽  
Molecular Potential ◽  
Wide Range ◽  
Energy Surfaces ◽  
New Applications ◽  
Physical Phenomena

<p>Machine learning (ML) methods have become powerful, predictive tools in a wide range of applications, such as facial recognition and autonomous vehicles. In the sciences, computational chemists and physicists have been using ML for the prediction of physical phenomena, such as atomistic potential energy surfaces and reaction pathways. Transferable ML potentials, such as ANI-1x, have been developed with the goal of accurately simulating organic molecules containing the chemical elements H, C, N, and O. Here we provide an extension of the ANI-1x model. The new model, dubbed ANI-2x, is trained to three additional chemical elements: S, F, and Cl. Additionally, ANI-2x underwent torsional refinement training to better predict molecular torsion profiles. These new features open a wide range of new applications within organic chemistry and drug development. These seven elements (H, C, N, O, F, Cl, S) make up ~90% of drug like molecules. To show that these additions do not sacrifice accuracy, we have tested this model across a range of organic molecules and applications, including the COMP6 benchmark, dihedral rotations, conformer scoring, and non-bonded interactions. ANI-2x is shown to accurately predict molecular energies compared to DFT with a ~10<sup>6</sup> factor speedup and a negligible slowdown compared to ANI-1x. The resulting model is a valuable tool for drug development that can potentially replace both quantum calculations and classical force fields for myriad applications.</p>

A Comprehensive Review on the Therapeutic Versatility of Imidazo [2,1-b]thiazoles

2020 ◽  
Vol 27 (40) ◽  
pp. 6864-6887 ◽  
Author(s):  
Mohd Adil Shareef ◽  
Irfan Khan ◽  
Bathini Nagendra Babu ◽  
Ahmed Kamal
Keyword(s):  
Literature Review ◽  
Medicinal Chemistry ◽  
Therapeutic Agents ◽  
Present Review ◽  
Thiazole Derivatives ◽  
Pharmacological Activities ◽  
Comprehensive Review ◽  
Derivatives Of

Background:: Imidazo[2,1-b]thiazole, a well-known fused five-membered hetrocycle is one of the most promising and versatile moieties in the area of medicinal chemistry. Derivatives of imidazo[2,1-b]thiazole have been investigated for the development of new derivatives that exhibit diverse pharmacological activities. This fused heterocycle is also a part of a number of therapeutic agents. Objective:: To review the extensive pharmacological activities of imidazo[2,1-b]thiazole derivatives and the new molecules developed between 2000-2018 and their usefulness. Method:: Thorough literature review of all relevant papers and patents was conducted. Conclusion:: The present review, covering a number of aspects, is expected to provide useful insights in the design of imidazo[2,1-b]thiazole-based compounds and would inspire the medicinal chemists for a comprehensive and target-oriented information to achieve a major breakthrough in the development of clinically viable candidates.

A Brief Review on the Development of Novel Potentially Active Azetidin-2-ones Against Cancer

2020 ◽  
Vol 24 (5) ◽  
pp. 473-486 ◽  
Author(s):  
Ligia S. da Silveira Pinto ◽  
Thatyana R. Alves Vasconcelos ◽  
Claudia Regina B. Gomes ◽  
Marcus Vinícius N. de Souza
Keyword(s):  
Side Effects ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Present Review ◽  
Pharmacological Properties ◽  
Important Group ◽  
Wide Range ◽  
Anti Inflammatory

Azetidin-2-ones (&#946;-lactams) and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antibacterial, anticancer, anti-diabetic, anti-inflammatory and anticonvulsant. Efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. The present review aimed to highlight some recent discoveries (2013-2019) on the development of novel azetidin-2-one-based compounds as potential anticancer agents.

Ethnomedicinal uses, Phytochemistry and Pharmacological Aspects of the Genus Berberis Linn: A Comprehensive Review

2020 ◽  
Vol 23 ◽  
Author(s):  
Roohi Mohi-ud-din ◽  
Reyaz Hassan Mir ◽  
Prince Ahad Mir ◽  
Saeema Farooq ◽  
Syed Naiem Raza ◽  
...  
Keyword(s):  
Chemical Constituents ◽  
Pharmacological Activities ◽  
Traditional Use ◽  
Comprehensive Review ◽  
Wide Range ◽  
Anti Cancer ◽  
Comprehensive Survey ◽  
Ethnomedicinal Uses

Background: Genus Berberis (family Berberidaceae), which contains about 650 species and 17 genera worldwide, has been used in folklore and various traditional medicine systems. Berberis Linn. is the most established group among genera with around 450-500 species across the world. This comprehensive review will not only help researchers for further evaluation but also provide substantial information for future exploitation of species to develop novel herbal formulations. Objective: The present review is focussed to summarize and collect the updated review of information of Genus Berberis species reported to date regarding their ethnomedicinal information, chemical constituents, traditional/folklore use, and reported pharmacological activities on more than 40 species of Berberis. Conclusion: A comprehensive survey of the literature reveals that various species of the genus possess various phytoconstituents mainly alkaloids, flavonoid based compounds isolated from different parts of a plant with a wide range of pharmacological activities. So far, many pharmacological activities like anti-cancer, anti-hyperlipidemic, hepatoprotective, immunomodulatory, anti-inflammatory both in vitro & in vivo and clinical study of different extracts/isolated compounds of different species of Berberis have been reported, proving their importance as a medicinal plant and claiming their traditional use.

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