The experience of using cholelitin

According to the composition of the components, cholelithin is produced in the form of three complexes of phytochemicals, selected according to the principle of selectively and synergistically influencing substances; the pharmacological effect of each of the complexes is much superior to the effect of the substances used separately.

Paracelsus Paradox and Drug Repurposing for Cancer

Dose is one of the parameters that any pharmacologist seriously considers when studying the effects of a drug. If the necessary dose to achieve a desired pharmacological effect is in a toxic or very toxic range for human use, the drug will probably fall out from further research. The concentration that a drug can reach at its target organ or cell is a direct consequence of the administered dose and its pharmacodynamic properties. Basic researchers investigate at the cellular level or eventually with xenografts. They use different concentrations of the drug in order to determine its cellular effects. However, in many cases, these concentrations require doses that are in the toxic range or well beyond any clinically achievable level. Therefore, in these cases, research is in the realm of Toxicology rather than therapeutics. This paper will show some examples about this exercise in futility which is time and resource consuming but that pullulates the pages of many prestigious journals. Many seasoned researchers seem to have forgotten the Paracelsus Paradox.

ANTIMICROBIAL ACTIVITY STUDY OF NEW QUINAZOLIN-4(3H)-ONES AGAINST STAPHYLOCOCCUS AUREUS AND STREPTOCOCCUS PNEUMONIAE

Quinazolin-4(3H)-one derivatives exhibiting a wide spectrum of a pharmacological activity, represent a promising class of substances used to obtain antibacterial agents, which is especially important in the context of the emergence of pathogenic microorganisms’ resistance to drugs used in medicine. It has been proved that compounds having a naphthyl radical in the molecule, as well as an amide group bound to the benzene ring as quinazolinone substituents, are characterized by a pronounced antimicrobial activity against Staphylococcus aureus and Streptococcus pneumoniae.The aim of the research is a primary microbiological screening of the in vitro antimicrobial activity of new quinazolin-4(3H)-one derivatives against Staphylococcus aureus and Streptococcus pneumoniae, as well as the assessment of the relationship between the pharmacological effect and the structural transformation of the substance molecule, lipophilicity and the possibility of forming resistance to them.Materials and methods. The experimental studies have been carried out using well-known nosocomial pathogens of infectious and inflammatory diseases Staphylococcus aureus and Streptococcus pneumoniae by a serial dilution method.Results. A compound containing a naphthyl radical in its structure, which contributes to an increase in the hydrophobicity of the substance and its solubility in the membrane of a bacterial cell, has a bacteriostatic effect against both Staphylococcus aureus and Streptococcus pneumoniae. A similar pharmacological effect is exhibited by a derivative with an amide group as a substituent of the quinazolinone nucleus linked to a phenyl radical, which probably contributes to an increase in the degree of binding to active sites of enzymes involved in the DNA replication, and protein synthesis. Obviously, the increased lipophilicity, which promotes better binding to the efflux protein, cannot serve as objective characteristics of the emergence possibility of the pathogen’s resistance to this substance.Conclusion. Among the synthesized compounds, the leading substances that exhibit an antimicrobial activity against Staphylococcus aureus and Streptococcus pneumonia, have been identified. The assessment of the chemical structure made it possible to substantiate their pharmacological action and draw conclusions about the possibility of developing resistance to it in microbial cells.

Chocolate as Carrier to Deliver Bioactive Ingredients: Current Advances and Future Perspectives

Consumer demand for healthier foods with improved taste and convenience has urged the food industry to develop functional foods added with bioactive ingredients that can supplement basic nutrition (food supplement) or exert a pharmacological effect (nutraceuticals). Chocolate could be used as an ideal carrier to deliver bioactive ingredients, mainly due to its high acceptability by consumers. However, a drawback of using chocolate as functional food is its high sugar content, which impedes its commercialization with the diabetic population. Therefore, there is need to develop sugar-free chocolate formulations added with bioactive ingredients. Nevertheless, sugar replacement and bioactive ingredients addition is a major technological challenge that affects texture, rheology, and sensory properties of chocolate. This review is designed as a practical guide for researchers and food industries to develop the next generation of functional chocolates. Different functional chocolate formulations, including sugar-free, are reviewed as potential carriers for the delivery of bioactive compounds. The physicochemical properties and sensory acceptability of the functional chocolates presented are also highlighted. Finally, future perspectives, such as the use of nanotechnology to improve the bioaccessibility and bioavailability of active ingredients, as well as the need for clinical trials to validate the pharmacological effect of functional chocolates, are also discussed.

Phytochemical Screening, Chemical Constituents, Traditional Medicine Usage, Pharmacological Effect, Metabolism and Pharmacokinetics of Semen armeniacae

Semen armeniacae refers to the seeds of Prunus armeniaca L. (Rosaceae). The Prunus armeniaca L. plant is spreading in the Korean peninsula, China, India, Japan, North Africa, and the United States of America. The Prunus armeniaca contains 3% amygdalin, titratable acidity, sugars (saccharose, fructose, and glucose), and organic acids (citric and malic acids) in addition to prunasin and mandelonitrile. Semen armeniacae is used for the treatment of asthma and cough (with expectoration and fever). It is used in constipation therapy. It is also used as eardrops for inflammation and tinnitus and the treatment of skin diseases. The pharmacological effect of Semen armeniacae includes experimental and clinical pharmacology. Experimental pharmacology includes anti-cholinesterase, neuroprotective, analgesic, antipyretic, antitumor, antibacterial, antimicrobial, antifungal, and antitussive activities. Decoction of Semen armeniacae to 2275 patients with COVID-19 improves clinical parameters such as lung state, clinical cure rate, number of cough reduction cases, symptom score of cough, viral nucleic acid testing, and inflammatory biomarkers. Oral intake of Semen armeniacae extract for 28 days did not cause any hematological, biochemical, or histological changes in rats. The Prunus armeniaca plant declines oxidative stress, inflammation, fat degeneration, and necrosis in alcohol-induced in-vivo and in-vitro liver injury models. There is no effect on fertility in rats after eating Semen armeniacae for 5 weeks. The average daily dose= 3-9 g of Semen armeniacae rinsing in boiling water then adding to a decoction. In conclusion, Semen armeniacae has anti-cholinesterase, neuroprotective, analgesic, antipyretic, antitumor, antibacterial, antimicrobial, antifungal, and antitussive activities.

The Ethnopharmacology, Phytochemistry, Pharmacology Activities of Yellow Velvetleaf Plant (Limnocharis flava): A Review

Ethnopharmacology is a scientific study that connects a group of people, health, and the habits of the people who use traditional medicines and formulating traditional medication. The yellow velvetleaf plant is a type of plant that lives in water. This plant can be used as a vegetable for daily consumption by the community. The yellow velvetleaf plant is a plant of the Alismataceae family. This plant is ethnopharmacological, in which there is a pharmacological effect related to treatment and health maintenance for the community because it has chemical compounds such as saponins, steroids, phenol hydroquinone, and also mineral contents: Phosphorus (P), Calcium (Ca), Potassium (K), Sodium (Na), Iron (Fe), and Zinc (Zn). This review article discusses the chemical compounds in yellow velvetleaf plants and the pharmacological effects of yellow velvetleaf plants. In this review article, it is known that yellow velvetleaf plants, used by the community as a local vegetable, have chemical compounds that can produce pharmacological effects.