ChemInform Abstract: NATURALLY OCCURRING SUBSTANCES WITH CYTOSTATIC ACTIVITY, STRUCTURE, MECHANISM OF ACTION, AND BIOLOGICAL EFFECTS

1975 ◽  
Vol 6 (22) ◽  
pp. no-no
Author(s):  
A. CIHAK
Keyword(s):  
Mechanism Of Action ◽  
Biological Effects ◽  
Cytostatic Activity ◽  
Naturally Occurring ◽  
Activity Structure

Synthesis and Biological Activity of Embelin and its Derivatives: An Overview

2020 ◽  
Vol 20 (5) ◽  
pp. 396-407 ◽  
Author(s):  
Zhaojun Sheng ◽  
Siyuan Ge ◽  
Min Gao ◽  
Rongchao Jian ◽  
Xiaole Chen ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Effects ◽  
New Drugs ◽  
Hydroxyl Groups ◽  
Carbonyl Groups ◽  
Cellular Mechanisms ◽  
Embelia Ribes ◽  
Naturally Occurring ◽  
Ic50 Value ◽  
Apoptosis Protein

Embelin is a naturally occurring para-benzoquinone isolated from Embelia ribes (Burm. f.) of the Myrsinaceae family, and contains two carbonyl groups, a methine group and two hydroxyl groups. With embelin as the lead compound, more than one hundred derivatives have been reported. Embelin is well known for its ability to antagonize the X-linked inhibitor of apoptosis protein (XIAP) with an IC50 value of 4.1 μM. The potential of embelin and its derivatives in the treatment of various cancers has been extensively studied. In addition, these compounds display a variety of other biological effects: antimicrobial, antioxidant, analgesic, anti-inflammatory, anxiolytic and antifertility activity. This paper reviews the recent progress in the synthesis and biological activity of embelin and its derivatives. Their cellular mechanisms of action and prospects in the research and development of new drugs are also discussed.

Role of Flavonoids in Neurodegenerative Disorders with Special Emphasis on Tangeritin

2019 ◽  
Vol 18 (8) ◽  
pp. 581-597 ◽  
Author(s):  
Ambreen Fatima ◽  
Yasir Hasan Siddique
Keyword(s):  
Medicinal Plants ◽  
Mechanism Of Action ◽  
Neurodegenerative Disorders ◽  
Treatment Strategies ◽  
Dietary Supplementation ◽  
Plant Polyphenols ◽  
Promising Candidate ◽  
Naturally Occurring ◽  
The Brain

Flavonoids are naturally occurring plant polyphenols found universally in all fruits, vegetables and medicinal plants. They have emerged as a promising candidate in the formulation of treatment strategies for various neurodegenerative disorders. The use of flavonoid rich plant extracts and food in dietary supplementation have shown favourable outcomes. The present review describes the types, properties and metabolism of flavonoids. Neuroprotective role of various flavonoids and the possible mechanism of action in the brain against the neurodegeneration have been described in detail with special emphasis on the tangeritin.

Screening of Synthetic Heterocyclic Compounds as Antiplatelet Drugs

2021 ◽  
Vol 17 ◽  
Author(s):  
Marcel Hrubša ◽  
Khondekar Nurjamal ◽  
Alejandro Carazo ◽  
Nayana Nayek ◽  
Jana Karlíčková ◽  
...  
Keyword(s):  
Mechanism Of Action ◽  
Biological Effects ◽  
Antiplatelet Drugs ◽  
Antiplatelet Drug ◽  
Breast Adenocarcinoma ◽  
Antiplatelet Activity ◽  
Major Mechanism ◽  
Treatment And Prevention ◽  
Impedance Aggregometry ◽  
Thromboxane Receptors

Background: Antiplatelet drugs represent the keystone in the treatment and prevention of diseases of ischemic origin, including coronary artery disease. The current palette of drugs represents efficient modalities in most cases, but their effect can be limited in certain situations or associated with specific side effects. In this study, representatives of compounds selected from series having scaffolds with known or potential antiplatelet activity were tested. These compounds were previously synthetized by us, but their biological effects have not yet been reported. Objective: The aim of this study was to examine the antiplatelet and anticoagulation properties of selected compounds and determine their mechanism of action. Methods: Antiplatelet activity of compounds and their mechanisms of action were evaluated using human blood by impedance aggregometry and various aggregation inducers and inhibitors and compared to appropriate standards. Cytotoxicity was tested using breast adenocarcinoma cell cultures and potential anticoagulation activity was also determined. Results: In total, four of 34 compounds tested were equally or more active than the standard antiplatelet drug acetylsalicylic acid (ASA). In contrast to ASA, all 4 active compounds decreased platelet aggregation triggered not only by collagen, but also partly by ADP. The major mechanism of action is based on antagonism at thromboxane receptors. In higher concentrations, inhibition of thromboxane synthase was also noted. In contrast to ASA, the tested compounds did not block cyclooxygenase-1. Conclusion: The most active compound, 2-amino-4-(1H-indol-3-yl)-6-nitro-4H-chromene-3-carbonitrile (2-N), which is 4-5x times more potent than ASA, is a promising compound for the development of novel antiplatelet drugs.

scholarly journals A multi-target caffeine derived rhodium(i) N-heterocyclic carbene complex: evaluation of the mechanism of action

2016 ◽  
Vol 45 (33) ◽  
pp. 13161-13168 ◽  
Author(s):  
Jing-Jing Zhang ◽  
Julienne K. Muenzner ◽  
Mohamed A. Abu el Maaty ◽  
Bianka Karge ◽  
Rainer Schobert ◽  
...  
Keyword(s):  
Mechanism Of Action ◽  
Metal Center ◽  
Carbene Complex ◽  
Naturally Occurring ◽  
Complex Evaluation

A rhodium(i) and a ruthenium(ii) complex with a caffeine derived N-heterocyclic carbene (NHC) ligand were biologically investigated as organometallic conjugates consisting of a metal center and a naturally occurring moiety.

Lithium - Pharmacological and Toxicological Aspects: The Current State of the Art

2020 ◽  
Vol 27 (3) ◽  
pp. 337-351 ◽  
Author(s):  
Branislava Medić ◽  
Marko Stojanović ◽  
Bojan V. Stimec ◽  
Nevena Divac ◽  
Katarina Savić Vujović ◽  
...  
Keyword(s):  
Mechanism Of Action ◽  
Glycogen Synthase ◽  
Tissue Injury ◽  
Current Knowledge ◽  
Biological Effects ◽  
Therapeutic Index ◽  
Adjunctive Treatment ◽  
Renal Diseases ◽  
Protective Effects ◽  
Organ Systems

: Lithium is the smallest monovalent cation with many different biological effects. Although lithium is present in the pharmacotherapy of psychiatric illnesses for decades, its precise mechanism of action is still not clarified. Today lithium represents first-line therapy for bipolar disorders (because it possesses both antimanic and antidepressant properties) and the adjunctive treatment for major depression (due to its antisuicidal effects). Beside, lithium showed some protective effects in neurological diseases including acute neural injury, chronic degenerative conditions, Alzheimer's disease as well as in treating leucopenia, hepatitis and some renal diseases. Recent evidence suggested that lithium also possesses some anticancer properties due to its inhibition of Glycogen Synthase Kinase 3 beta (GSK3β) which is included in the regulation of a lot of important cellular processes such as: glycogen metabolism, inflammation, immunomodulation, apoptosis, tissue injury, regeneration etc. : Although recent evidence suggested a potential utility of lithium in different conditions, its broader use in clinical practice still trails. The reason for this is a narrow therapeutic index of lithium, numerous toxic effects in various organ systems and some clinically relevant interactions with other drugs. Additionally, it is necessary to perform more preclinical as well as clinical studies in order to a precise therapeutic range of lithium, as well as its detailed mechanism of action. The aim of this review is to summarize the current knowledge concerning the pharmacological and toxicological effects of lithium.

scholarly journals Snake Venom: Any Clue for Antibiotics and CAM?

2005 ◽  
Vol 2 (1) ◽  
pp. 39-47 ◽  
Author(s):  
Deivy Clementino de Lima ◽  
Paula Alvarez Abreu ◽  
Cícero Carlos de Freitas ◽  
Dilvani Oliveira Santos ◽  
Rodrigo Oliveira Borges ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Alternative Medicine ◽  
Complementary And Alternative Medicine ◽  
Snake Venom ◽  
Biological Effects ◽  
Mechanisms Of Action ◽  
Snake Venoms ◽  
Commercial Use ◽  
Naturally Occurring ◽  
Complementary And Alternative

Lately several naturally occurring peptides presenting antimicrobial activity have been described in the literature. However, snake venoms, which are an enormous source of peptides, have not been fully explored for searching such molecules. The aim of this work is to review the basis of antimicrobial mechanisms revealing snake venom as a feasible source for searching an antibiotic prototype. Therefore, it includes (i) a description of the constituents of the snake venoms involved in their main biological effects during the envenomation process; (ii) examples of snake venom molecules of commercial use; (iii) mechanisms of action of known antibiotics; and (iv) how the microorganisms can be resistant to antibiotics. This review also shows that snake venoms are not totally unexplored sources for antibiotics and complementary and alternative medicine (CAM).

scholarly journals Escherichia coli S-adenosylhomocysteine/5′-methylthioadenosine nucleosidase. Purification, substrate specificity and mechanism of action

1985 ◽  
Vol 232 (2) ◽  
pp. 335-341 ◽  
Author(s):  
F Della Ragione ◽  
M Porcelli ◽  
M Cartenì-Farina ◽  
V Zappia ◽  
A E Pegg
Keyword(s):  
Escherichia Coli ◽  
Enzyme Activity ◽  
Mechanism Of Action ◽  
Specific Activity ◽  
Maximal Rate ◽  
Purification Procedure ◽  
Protein Affinity ◽  
Naturally Occurring ◽  
Purine Ring ◽  
Ribose Moiety

S-Adenosylhomocysteine/5′-methylthioadenosine nucleosidase (EC 3.2.2.9) was purified to homogeneity from Escherichia coli to a final specific activity of 373 mumol of 5′-methylthioadenosine cleaved/min per mg of protein. Affinity chromatography on S-formycinylhomocysteine-Sepharose is the key step of the purification procedure. The enzyme, responsible for the cleavage of the glycosidic bond of both S-adenosylhomocysteine and 5′-methylthioadenosine, was partially characterized. The apparent Km for 5′-methylthioadenosine is 0.4 microM, and that for S-adenosylhomocysteine is 4.3 microM. The maximal rate of cleavage of S-adenosylhomocysteine is approx. 40% of that of 5′-methylthioadenosine. Some 25 analogues of the two naturally occurring thioethers were studied as potential substrates or inhibitors of the enzyme. Except for the analogues modified in the 5′-position of the ribose moiety or the 2-position of the purine ring, none of the compounds tested was effective as a substrate. Moreover, 5′-methylthioformycin, 5′-chloroformycin, S-formycinylhomocysteine, 5′-methylthiotubercidin and S-tubercidinylhomocysteine were powerful inhibitors of the enzyme activity. The results obtained allow the hypothesis of a mechanism of enzymic catalysis requiring as a key step the protonation of N-7 of the purine ring.

BIOLOGICAL MONITORING OF THE FORTIES OILFIELD (NORTH SEA)

1983 ◽  
Vol 1983 (1) ◽  
pp. 405-414 ◽  
Author(s):  
J. P. Hartley ◽  
J. Ferbrache
Keyword(s):  
North Sea ◽  
Biological Effects ◽  
Monitoring Program ◽  
Benthic Fauna ◽  
Sediment Type ◽  
The North ◽  
Naturally Occurring ◽  
The North Sea ◽  
Similar Survey ◽  
Benthic Sediments

ABSTRACT The Forties Oilfield (the largest in the U.K. sector of the North Sea) has been in production since September 1975. In June 1975, a quantitative survey of the benthic sediments and fauna over the area was made at the start of an environmental monitoring program for the field. The results of a repeat survey carried out after three years of production have been reported by Hartley.13 This paper presents data from a third similar survey in June 1981 and compares the findings with those of the earlier surveys. The benthic fauna of the Forties Field is rich and diverse and qualitatively corresponded well in 1981 to previous descriptions. Naturally occurring gradients in both the sediment type and fauna are a feature of this area. Changes in the densities of certain species were noted at some sites in 1981, including increases in certain opportunistic forms. Although no areas of biological effect could be delineated around the four production platforms, the industrial activity in the field may be implicated in the changes found at several stations. The hydrocarbon content of the sediments was low and, with one possible exception, did not appear related to the biological changes noted. The results to date suggest that offshore oilfields in deep water, developed using water-based drill fluids, present relatively few biological problems in the short term. Since no major biological effects have been found after six years of drilling and production, a reduced program of monitoring is recommended to maintain biological surveillance during the life of the field.

Sign in / Sign up

Export Citation Format

Share Document