ChemInform Abstract: 1-METHYLISOGUANOSINE, A PHARMACOLOGICALLY ACTIVE AGENT FROM A MARINE SPONGE

1981 ◽  
Vol 12 (4) ◽  
Author(s):  
A. F. COOK ◽  
R. T. BARTLETT ◽  
R. P. GREGSON ◽  
R. J. QUINN
1980 ◽  
Vol 45 (20) ◽  
pp. 4020-4025 ◽  
Author(s):  
Alan F. Cook ◽  
Robert T. Bartlett ◽  
Richard P. Gregson ◽  
Ronald J. Quinn

2020 ◽  
Vol 8 (3) ◽  
pp. 163-190
Author(s):  
Benjamin Steinborn ◽  
Ulrich Lächelt

: Coordinative interactions between multivalent metal ions and drug derivatives with Lewis base functions give rise to nanoscale coordination polymers (NCPs) as delivery systems. As the pharmacologically active agent constitutes a main building block of the nanomaterial, the resulting drug loadings are typically very high. By additionally selecting metal ions with favorable pharmacological or physicochemical properties, the obtained NCPs are predominantly composed of active components which serve individual purposes, such as pharmacotherapy, photosensitization, multimodal imaging, chemodynamic therapy or radiosensitization. By this approach, the assembly of drug molecules into NCPs modulates pharmacokinetics, combines pharmacological drug action with specific characteristics of metal components and provides a strategy to generate tailorable multifunctional nanoparticles. This article reviews different applications and recent examples of such highly functional nanopharmaceuticals with a high ‘material economy’. : Lay Summary: Nanoparticles, that are small enough to circulate in the bloodstream and can carry cargo molecules, such as drugs, imaging or contrast agents, are attractive materials for pharmaceutical applications. A high loading capacity is a generally aspired parameter of nanopharmaceuticals to minimize patient exposure to unnecessary nanomaterial. Pharmaceutical agents containing Lewis base functions in their molecular structure can directly be assembled into metal-organic nanopharmaceuticals by coordinative interaction with metal ions. Such coordination polymers generally feature extraordinarily high loading capacities and the flexibility to encapsulate different agents for a simultaneous delivery in combination therapy or ‘theranostic’ applications.


1980 ◽  
Vol 21 (6) ◽  
pp. 567-568 ◽  
Author(s):  
Ronald J. Quiann ◽  
Richard P. Gregson ◽  
Alan F. Cook ◽  
Robert T. Bartlett

2020 ◽  
Vol 2 (1) ◽  
pp. 52-66
Author(s):  
Wendy Alexander Tanod ◽  
Muliadin ◽  
Yeldi S. Adel ◽  
Didit Kustantio Dewanto

Marine organisms are a source of natural products and produce compounds with a molecular structure that is unique and useful. Thousands of new compounds have biological activitity for anticancer, antiviral, and antimicrobial. This compounds isolated from various marine organism, including from marine-derived fungi. Investigation of chemical compounds from marine-derived fungi isolated from sponge has increased steadily, indicating the important role of marine-derived fungi in the discovery of drug compounds. The sponge has produced various kinds of fungi, which have reported to provide a variety of pharmacologically active metabolites and structurally diverse. Study literature showed that many fungal genera isolated from the marine sponge dominated the genus Acremonium, Aspergillus, Penicillium, Phoma, and Fusarium. The high proportion of genera and new compounds showed that the fungi isolated from the sponge could develop.


Author(s):  
HANADY S AL-SHMGANI ◽  
RAIED MUSTAFA SHAKIR ◽  
AHMED W NASER ◽  
OLUSOLA OLALEKAN ELEKOFEHINTI

Objective: Hesperidin (HSP) is a pharmacologically active organic compound found in citrus fruits and peppermint. We synthesized a new HSP derivative by reacting it with 5-Amino-1,3,4-thiadiazole-2-thiol in acetic acid. Methods: This compound was characterized by Fourier-transform infrared, proton nuclear magnetic resonance, and electron impact mass spectra. A molecular docking study explores the predicted binding of the compound and its possible mode of action. Bioavailability, site of absorption, drug mimic, and topological polar surface was predicted using absorption, distribution, metabolism, and excretion (ADME) studies. Results: The docking study predicts that the new compound binds to the active sites of Aurora-B and the MST3 pocket and has good ADME properties. Moreover, the thiazole ring and the presence of the electron releasing groups and hydrogen bond interaction with amino acid residues within the active sites play an important role in enhancing the antioxidant activity. Conclusion: In the present study, a new HSP derivative has been synthesized and characterized successfully and a theoretically promising antioxidant and anticytotoxic active agent introduced. We have shown the detailed binding analysis of 1,3,4-thiadiazol and hydrogen bonds with the inhibitor binding cavity of Aurora B and MST3. This could provide the development of some effective compounds against different diseases.


1960 ◽  
Vol 38 (1) ◽  
pp. 39-45 ◽  
Author(s):  
K. G. Davey

The opaque accessory secretion from the male reproductive system of insects has been characterized in various ways. It exerts a melanophorotropic effect on the melanocytes in the skin of the frog, Rana pipiens, a property which, among naturally occurring compounds, is shared only by the indolalkylamines. The secretion also increases the rate of beating of the heart of the cockroach Periplaneta americana; its activity in this respect is unaffected by heating or by incubating with the enzyme trypsin, but it is destroyed by the action of the enzymes monoamine oxidase, tyrosinase, and o-diphenol oxidase. The active principle is associated with particles from which it is slowly released into solution. It is tentatively concluded that the material is an o-dihydroxyindolalkylamine.


1982 ◽  
Vol 30 (10) ◽  
pp. 3544-3547 ◽  
Author(s):  
HIROYUKI KIKUCHI ◽  
YASUMASA TSUKITANI ◽  
TOSHITAKA MANDA ◽  
TAKASHI FUJII ◽  
HAJIME NAKANISHI ◽  
...  

1988 ◽  
Vol 22 (12) ◽  
pp. 953-959 ◽  
Author(s):  
Robert W. Pfeifer ◽  
Robert E. Notari

Multiple dosage regimens for therapeutic agents are commonly comprised of a constant dosing interval and a constant dose size. This is not true for the ingestion of a pharmacologically active agent that is a component in a dietary source. Caffeine is contained in foods and beverages that are regular components of the diet for many people. Because daily intake is unsystematic, a computer program was written to simulate caffeine plasma concentration-time courses following ingestion of variable amounts on irregular schedules. Literature values for caffeine pharmacokinetics, for the caffeine content in various foods and beverages, and for consumer habits were employed to simulate various caffeine plasma concentration-time courses. By searching for predictable traits in a wide variety of plasma concentration-time courses representing normal adults, a simple noncomputer method was developed to allow individuals to estimate caffeine plasma concentrations based on personal intake habits. Changes in the time courses due to smoking, oral contraceptive use, and liver disease, all of which alter caffeine pharmacokinetics, were also examined.


Author(s):  
Dusica Ilic ◽  
Vesna Nikolic ◽  
Ljubisa Nikolic ◽  
Mihajlo Stankovic ◽  
Ljiljana Stanojevic ◽  
...  

In this review, the biosynthesis of allicin (allyl thiosulfinate) by enzymatic transformation of alliin and various methods of its synthesis with detailed investigation of mechanisms and kinetics are summarized. A convenient method is also described for determination of allicin stability and the utility of the inclusion complexes of this pharmacologically active agent with ?-cyclodextrins in increasing its stability. Allicin is the initial precursor for the production of ajoene ((E)- and (Z)-4,5,9-trithiadodeca- 1,6,11-triene 9-oxides) and vinyldithiin (2-vinyl-4H-1,3-dithiin, and 3-vinyl-4H-1,2- dithiin), which are more stable and show various pharmacological effects. The mechanisms of allicin transformations to these compounds are given in detail. Finally, the data on the pharmacological effects of allicin and its transformation products, ajoene and vinyldithiin, are presented.


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