German Journal of Pharmaceuticals and Biomaterials

ADMET Prediction of synthesized Heterocyclic derivatives to treat renal cancer

Tue, 11 Oct 2022 00:00:00 -0400

A library of 121 potent, synthesized, and characterized compounds from different heterocyclic derivatives such as pyrimidine, phthalazine, benzothiazole, benzpyrazoline, indoline, benzimidazole, phthalazine, indole, quinoline, quinazoline were selected based on their anti-renal cancer activity. The Drug likeness, Bioactivity, Absorption, Distribution, Metabolism, Excretion, and Toxicity of all the screened compounds were predicted through Molinspiration, PreADMET, and Osiris software. After screening 121 compounds, 19 compounds showed drug-like properties and an absorption percentage better than the standard drug Sorafenib. These compounds were further assessed based on their distribution parameter and the compounds that showed plasma protein binding equal to or below 90% and blood-brain barrier penetration below 1.000 were selected, i.e., compounds 3, 23, 64, 65 were then further assessed for the toxicity. Osiris property explorer was used to predict drug relevance and toxicity of the synthesized compounds. Compounds 3 and 23 were non-toxic similar to the standard drug Sorafenib. Compounds 3 and 23 were found to be active as Kinase Inhibitors, with a bioactivity score of 0.2 and 0.6 compared to standard drug sorafenib, which scored 0.44. Therefore Compound 3 N-(4-fluoro-2-methoxyphenyl)-7-methyl-5,6,7,8-tetrahydropyrido [4',3':4,5] thieno[2,3-d] pyrimidin-4-amine and compound 23 1-(4-fluorophenyl)-3-methyl-N-phenyl-3a,7a-dihydro-1H-pyrazolo[3,4-d] pyrimidin-4-amine belonging to pyrimidine derivatives were considered as best and suggested to be taken further for preclinical and clinical trials. The pyrimidine derivatives with anti-renal cancer activity can serve as a scaffold for the design of renal cancer targeting agents and motivates the further development of effective and safer compounds.

Effects of carboxymethylated gum obtained from Entandophragma angolense tree on the compressional and release properties of ibuprofen tablets

Oladapo A detunji, Olubunmi M Ajakore, Oludele A Itiola — Tue, 11 Oct 2022 00:00:00 -0400

The incorporation of modified polymers in drug formulations is primarily due to their low toxicity, affordability, availability, compatibility with biological membranes, economic feasibility and bio-degradability.This study investigated the compressional and release characteristics of ibuprofen tablet formulations containing natural and modified Entandophragma angolense gum. Entandophragma angolense gum (ENTA) was extracted and modified by carboxymethylation to yield CENTA. Ibuprofen tablets containing varying binder concentrations (2.5-10% w/w) of ENTA and CENTA (compared with gelatin BP) were formulated by wet granulation. Crushing strength (CS) and friability (FR) were used in assessing the mechanical properties of the tablets, while disintegration and dissolution times accounted for drug release parameters. Density measurements, Kawakita equations and Heckel plots were used to assess the compressional properties of the formulations. The results were analysed using ANOVA at ɑ0.05. Generally, there was a direct relationship between the concentration of the polymers and the CS of the tablets, while an inverse relationship was observed for FR. The CS ranked ENTA > CENTA > gelatin BP. Carboxymethylation of ENTA enhanced drug release (t_30% and t_80%). Formulations containing CENTA had a slower and faster onset of plastic deformation; mean yield pressure (P_y), ranked ENTA > CENTA > gelatin BP. A measure of the rearrangement phase at the early stages of compression (D_B) was highest for CENTA at all concentrations. CENTA compared favourably with gelatin BP and showed better mechanical and release characteristics than ENTA. Also, CENTA shows good potential as a binder in fast disintegrating ibuprofen tablets, especially when incorporated at low concentrations.

Editor

Editor — Tue, 11 Oct 2022 00:00:00 -0400

Front Matter

Saraca asoca: A scoping review on the phytoconstituents, bioactives and their therapeutic effects

Tue, 11 Oct 2022 00:00:00 -0400

Saraca asoca or S. asoca, belonging to the family Caesalpinaceae, is popularly known as Ashoka and is a valuable indigenous plant of traditional and pharmacological significance. With a growing number of people seeking treatments and health practices devoid of synthetic medicines' adverse effects, medicinal herbs are becoming more mainstream. Ashoka has traditionally been employed to treat dysentery, colic, piles, biliousness, dyspepsia, and ulcers and is also known to display CNS depressant activity and regulate irregular menstrual cycles. The qualitative phytoconstituents of Ashoka's leaves, flowers, fruits, and bark, such as glycosides, flavonoids, tannins, and saponins, carry vast potential in therapeutic and diagnostic techniques. Formulations containing these components can efficiently exert anti-microbial, anti-inflammatory, anti-menorrhagia, anti-diabetic, anthelmintic, and analgesic activity. This review focuses on research associated with the medicinal qualities, phytochemistry, and pharmacological profile of Saraca asoca (Roxb.), De. wild.

Conflicts of interest in scholarly communication: what is it and how to avoid it?

Paras Sharma — Tue, 11 Oct 2022 00:00:00 -0400

The journals often require disclosure of the conflicts of interest from all the stakeholders involved in the peer review and editorial process. The international committee of medical journal editors (ICMJE) defines conflicts of interest as "The potential for conflict of interest and bias exists when professional judgment concerning a primary interest (such as patients' welfare or the validity of research) may be influenced by a secondary interest (such as financial gain)" [1]. Another definition states, "A conflict of interest is a set of circumstances that creates a risk that professional judgment or actions regarding a primary interest will be unduly influenced by a secondary interest" [2]. It is a situation where the same individual is involved with two competing interests, one of which may involve unethical motivation or benefit or financial interest. Therefore, the COI involves a real, apparent, or potential violation of the trust that others have in the process being conducted or in the researchers participating in the research. Although conflicts of interest (COI) are not new in biomedical research, it was rarely reported until the late 90s, when serious reports of linkage between private companies and academic institutions [3]. It gained more attention with the increasing number of sponsored research on commercial applications leading to doubt about how sponsorship or partial financial support affects the research outcome. The COI is a significant concern for biomedical and pharmaceutical journals. The organizations such as the International Committee of Medical Journal Editors, the World Association of Medical Editors and the Committee on Publication Ethics (COPE) have launched initiatives to establish international standards for Conflict of Interest (COI) disclosure. COPE requires its member journals to comply with its Code of Conduct for Journal Editors. Although these initiatives helped a lot to improve the situation, there is still a lack of awareness and understanding of COI, especially among budding researchers.