Biochemical and pharmacological properties of a new thrombin-like serine protease (Russelobin) from the venom of Russell's Viper (Daboia russelii russelii) and assessment of its therapeutic potential

2013 ◽  
Vol 1830 (6) ◽  
pp. 3476-3488 ◽  
Author(s):  
Ashis K. Mukherjee ◽  
Stephen P. Mackessy
Keyword(s):  
Serine Protease ◽  
Therapeutic Potential ◽  
Pharmacological Properties ◽  
Russell’S Viper

Exploring the Chemistry and Therapeutic Potential of Triazoles: A Comprehensive Literature Review

2019 ◽  
Vol 19 (16) ◽  
pp. 1298-1368 ◽  
Author(s):  
Ankit Jain ◽  
Poonam Piplani
Keyword(s):  
Oxidative Stress ◽  
Drug Discovery ◽  
Literature Review ◽  
Structural Modification ◽  
Therapeutic Potential ◽  
Pharmacological Properties ◽  
Pharmacological Activities ◽  
Triazole Derivatives ◽  
Comprehensive Literature Review ◽  
The Common

: Triazole is a valuable platform in medicinal chemistry, possessing assorted pharmacological properties, which could play a major role in the common mechanisms associated with various disorders like cancer, infections, inflammation, convulsions, oxidative stress and neurodegeneration. Structural modification of this scaffold could be helpful in the generation of new therapeutically useful agents. Although research endeavors are moving towards the growth of synthetic analogs of triazole, there is still a lot of scope to achieve drug discovery break-through in this area. Upcoming therapeutic prospective of this moiety has captured the attention of medicinal chemists to synthesize novel triazole derivatives. The authors amalgamated the chemistry, synthetic strategies and detailed pharmacological activities of the triazole nucleus in the present review. Information regarding the marketed triazole derivatives has also been incorporated. The objective of the review is to provide insights to designing and synthesizing novel triazole derivatives with advanced and unexplored pharmacological implications.

Therapeutic perspectives of the black cumin component thymoquinone: A review

2021 ◽  
Author(s):  
Chandan Sarkar ◽  
Sarmin Jamaddar ◽  
Tawhida Islam ◽  
Milon Mondal ◽  
Muhammad Torequl Islam ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Nigella Sativa ◽  
Pharmacological Properties ◽  
Black Cumin

The dietary phytochemical thymoquinone, obtained from the black and angular seeds of Nigella sativa, is a promising monoterpenoid hydrocarbons, which has been receiving massive attention for its therapeutic potential and pharmacological properties.

scholarly journals Irreversible Inhibition of BoNT/A Protease: Unique Warhead Reactivity and Function Contingent upon a Bifunctional Approach

2021 ◽  
Author(s):  
Lewis Turner ◽  
Alexander Lund Nielsen ◽  
Lucy Lin ◽  
Sabine Pellett ◽  
Takashi Sugane ◽  
...  
Keyword(s):  
Enzyme Kinetics ◽  
Therapeutic Potential ◽  
Covalent Bond ◽  
Pharmacological Properties ◽  
Irreversible Inhibition ◽  
And Function ◽  
Chelating Compounds

We describe a comprehensive screening campaign of warheads, linked to a hydroxamate chelating anchor, for the modification of Cys165 within the BoNT/A protease. <div>Engaging thorough enzyme kinetics, we detail a remarkable proximity-driven covalent bond with an epoxide warhead, a weak electrophile; yet, one that possessed superior irreversible inhibition, and pharmacological properties, when compared to intrinsically higher reactive warheads. This directed, selective covalent bond was contingent upon the crucial hydroxamate-Zn<sup>2+ </sup>chelating interaction as exemplified by examining non-chelating compounds. </div><div>We discuss previous approaches using non-target selective cysteine-reactive warheads to modify the BoNT/A protease of which none present any therapeutic potential – our bifunctional strategy allows the use of intrinsically less reactive warheads to intercept the cysteine, which will allow for less off-target modifications of such inhibitors. Moreover, we also broach that this bifunctional approach is not a one-off strategy that we believe can be broadly translated to other metalloproteases that possess non-catalytic, yet, nucleophilic residues within the enzymes catalytic sphere. </div>

Na+ transport in normal and CF human bronchial epithelial cells is inhibited by BAY 39-9437

2001 ◽  
Vol 281 (1) ◽  
pp. L16-L23 ◽  
Author(s):  
Robert J. Bridges ◽  
Ben B. Newton ◽  
Joseph M. Pilewski ◽  
Daniel C. Devor ◽  
Christopher T. Poll ◽  
...  
Keyword(s):  
Serine Protease ◽  
Half Life ◽  
Inhibitory Concentration ◽  
Therapeutic Potential ◽  
Short Circuit ◽  
Short Circuit Current ◽  
Inhibitory Effect ◽  
Human Bronchial Epithelial Cells ◽  
Na Transport ◽  
Bronchial Epithelial

To test the hypothesis that Na+ transport in human bronchial epithelial (HBE) cells is regulated by a protease-mediated mechanism, we investigated the effects of BAY 39-9437, a recombinant Kunitz-type serine protease inhibitor, on amiloride-sensitive short-circuit current of normal [non-cystic fibrosis (CF) cells] and CF HBE cells. Mucosal treatment of non-CF and CF HBE cells with BAY 39-9437 decreased the short-circuit current, with a half-life of ∼45 min. At 90 min, BAY 39-9437 (470 nM) reduced Na+ transport by ∼70%. The inhibitory effect of BAY 39-9437 was concentration dependent, with a half-maximal inhibitory concentration of ∼25 nM. Na+ transport was restored to control levels, with a half-life of ∼15 min, on washout of BAY 39-9437. In addition, trypsin (1 μM) rapidly reversed the inhibitory effect of BAY 39-9437. These data indicate that Na+transport in HBE cells is activated by a BAY 39-9437-inhibitable, endogenously expressed serine protease. BAY 39-9437 inhibition of this serine protease maybe of therapeutic potential for the treatment of Na+ hyperabsorption in CF.

scholarly journals Pharmacological properties and therapeutic potential of saffron ( Crocus sativus L.) in osteosarcoma

2019 ◽  
Vol 72 (1) ◽  
pp. 56-67 ◽  
Author(s):  
Bilal Ege ◽  
Onder Yumrutas ◽  
Miray Ege ◽  
Mustafa Pehlivan ◽  
Ibrahim Bozgeyik
Keyword(s):  
Therapeutic Potential ◽  
Crocus Sativus ◽  
Pharmacological Properties ◽  
Crocus Sativus L

scholarly journals A Phytopharmacological Review on a Medicinal Plant: Cordia africana Lam.

2021 ◽  
Vol 5 (3) ◽  
Author(s):  
Gashaw Nigussie ◽  
Fozia Ibrahim ◽  
Sebsib Neway
Keyword(s):  
Medicinal Plant ◽  
Human Health ◽  
Soil Conservation ◽  
Therapeutic Potential ◽  
Future Research ◽  
Pharmacological Properties ◽  
Young Branch ◽  
Cordia Africana ◽  
Trees And Shrubs ◽  
Different Parts

The use of phytoconstituents single or combined with standard medicines has been utilized in cure of different diseases. Many plants of genus Cordia comprise of trees and shrubs are widely distributed in warmer regions and have been utilized in management of various diseases. Cordia africana Lam. (family- Boraginaceae) is a small to medium-sized evergreen tree, 4 to 15 (30) m high, heavily branched with a spreading, umbrella-shaped or rounded crown. Bole typically curved or crooked. Bark grayish-brown to dark brown, smooth in young trees, but soon becoming rough and longitudinally fissured with age; young branch lets with sparse long. Uses of C. africana: firewood, timber (furniture, beehives, boxes, mortars, church, drums), food (fruit), medicine (bark, roots), fodder (leaves), bee forage, mulch, soil conservation, ornamental, shade. Various phytoconstituents like flavonoids, alkaloids, tannins, terpenoids, saponins, steroids, anthraquinones, carbohydrates and protins having different activities were screened and isolated from different parts of Cordia africana. Various important Pharmacological properties including Antioxidant, Cytotoxicity, anti-inflammatory, anthelmintic, antimicrobial, anti-nociceptive, and others have been well documented for this plant. Therefore, we have briefly reviewed the various bioactivities of Cordia africana to improve our knowledge on plant phytochemicals as therapeutic entities. The present review describes the various phytoconstituents and therapeutic potential of Cordia africana that can be followed for future research on this plant for human health benefits.

scholarly journals Review of Ethnomedicinal, Phytochemical and Pharmacological Properties of Lannea schweinfurthii (Engl.) Engl.

Molecules ◽  
2019 ◽  
Vol 24 (4) ◽  
pp. 732 ◽  
Author(s):  
Alfred Maroyi
Keyword(s):  
Animal Studies ◽  
Therapeutic Potential ◽  
American Chemical Society ◽  
Relevant Information ◽  
Chemical Society ◽  
Pharmacological Properties ◽  
Phytochemical Compounds ◽  
Cytotoxicity Activities ◽  
Ethnomedicinal Uses

Lannea schweinfurthii is a valuable medicinal plant species among different ethnic groups in tropical Africa. The aim of the current study was to review existing literature on the ethnomedicinal uses, phytochemistry and pharmacological properties of L. schweinfurthii in an effort to evaluate the therapeutic potential of the species. The relevant information on the ethnomedicinal uses, phytochemistry and pharmacological properties of L. schweinfurthii was generated from several sources including books, book chapters, theses, scientific reports and journal articles obtained from the library and internet sources such as SciFinder, Wiley, Web of Science, American Chemical Society publications, PubMed, BMC, Elsevier, Science Direct, Scielo and Scopus. Traditionally, L. schweinfurthii is used against reproductive system disorders, respiratory disorders, injuries, headache, blood system disorders, infections or infestations and gastro-intestinal disorders. The phytochemical compounds that have been isolated from L. schweinfurthii include alkaloids, anthocyanins, flavonoids, glycosides, phenols, saponins, steroids, tannins and terpenoids. The in vitro and animal studies carried out so far from the crude extracts and compounds isolated from the species exhibited acetylcholinesterase inhibitory, anti-apoptotic, antibacterial, antiviral, anti-giardial, anti-inflammatory, antioxidant, antiplasmodial, antitrypanosomal, hepatoprotective, larvicidal and cytotoxicity activities. Detailed ethnopharmacological studies emphasizing clinical and toxicological evaluations are needed to assess efficacy and safety of the species as herbal medicine.

Traditional knowledge to clinical trials: a review on nutritional and therapeutic potential of Pithecellobium dulce

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Suresh Sulekha Dhanisha ◽  
Sudarsanan Drishya ◽  
Chandrasekharan Guruvayoorappan
Keyword(s):  
Combinatorial Chemistry ◽  
Therapeutic Potential ◽  
New Drugs ◽  
Pharmacological Properties ◽  
Traditional System ◽  
The Past ◽  
Drug Of Choice ◽  
Anti Oxidant ◽  
Therapeutic Properties ◽  
Different Parts

Abstract The review describes botanical aspects, bioactive phytocompounds and pharmacological properties of different parts of Pithecellobium dulce, with special emphasis on the nutritional status of its fruits. The different parts of plant extract have been reported to possess anti-oxidant, anti-inflammatory, anti-microbial, anti-diabetic, cardio protective, anti-diarrhoeal, anti-ulcerogenic, larvicidal and ovicidal activities. Different parts of plant extracts were reported to contain several bioactive phytocompounds such as flavonoids, saponins, tannins, alkaloids etc. Natural products discovered so far served as a viable source for new drugs. Over the past few years, continued and perpetual attention of people has been paid to medicinal plants in connection with its remarkable importance in drug discovery. Plant products always remains a drug of choice for the identification of novel leads despite facing a tough competition from existing synthetic alternatives derived from combinatorial chemistry, owing to their efficacy, side effects, and safety. P. dulce is a highly acclaimed genus in traditional system of medicine because of its versatile nutraceutical and pharmacological properties. In this review we discuss in detail about nutritional and various therapeutic properties of P. dulce.

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