Biological Activity Of Compounds Research Articles

Antimicrobial and Cytotoxic Naphthoquinones from Microbial Origin: An Updated Review.

Naphthoquinones (NQs) are small molecules bearing two carbonyl groups. They have been the subject of much research due to their significant biological activities such as antiproliferative, antimicrobial, anti-inflammatory, antioxidant, and antimalarial effects. NQs are produced mainly by bacteria, fungi and higher plants. Among them, microorganisms are a treasure of NQs with diverse skeletons and pharmacological properties. The purpose of the present study is to provide a comprehensive update on the structural diversity and biological activities of 91 microbial naphthoquinones isolated from 2015 to 2022, with a special focus on antimicrobial and cytotoxic activities. During this period, potent cytotoxic NQs such as naphthablin B (46) and hygrocin C (30) against HeLa (IC50=0.23 μg/ml) and MDA-MB-431 (IC50=0.5 μg/ml) cell lines was reported, respectively. In addition, rubromycin CA1 (39), exhibited strong antibacterial activity against Staphylococcus aureus (MIC of 0.2 μg/ml). As importance bioactive compounds, NQs may open new horizon for treatment of cancer and drug resistant bacteria. As such, it is hoped that this review article may stimulates further research into the isolation of further NQs from microbial, and other sources as well as the screening of such compounds for biological activity and beneficial uses.

A NEW NATURAL FOOD DYE: MICROENCAPSULATED CORNELIAN CHERRY BIOACTIVE COMPOUNDS

Cornus mas (CM) is one of the four edible fruits of the Cornus genus, a rich source of biologically active compounds (BACs) such as vitamins (like vitamin C), carotenoids, iridoids, and phenolics (phenolic acids, anthocyanins, and other flavonoids). This study aimed to analyse the improvement of the stability of CM anthocyanins by microencapsulation, in order to propose a new natural food dye. Microencapsulation using a mixture of whey protein isolate (WPI) and chitosan (CH) as wall materials has been applied to protect anthocyanins against external factors (e.g., light, temperature, storage, etc.). Two experimental variants of microencapsulated powders, WPI:CH = 1:1 (CH1) and WPI:CH = 1:2 (CH2), were realised by varying the wall materials ratio. The cornelian cherry fruit concentrated extract was evaluated for its phytochemical, colourimetric, and antioxidant capacities. Due to the excellent anthocyanin encapsulation effectiveness (74.29 – 88.71%), the wall materials utilised for both powders can be considered effective choices to safeguard the anthocyanins. All tests performed on the microencapsulated powders demonstrated that both suggested experimental forms can serve as a healthy substitute for artificial food additives. The incorporation of cornelian cherry fruit extract and microencapsulated powders into a food matrix (jelly candies) allowed examination of their effectiveness. The colour analysis rigorously characterised all the colour parameters related to red nuances (due to anthocyanins content, such as cyanidin-3-glucoside) and yellow nuances (associated with carotenoids content).

The genus Cochlospermum Kunth: a comprehensive review of key species with a focus on botanical, pharmacological, and chemical atributes

The Cochlospermum genus plant species are commonly used in traditional medicine for its antimicrobial, antiparasitic, anti-inflammatory, and hypoglycemic properties. The objective of this review is to describe the mainly important medicinal plant species of the genus Cochlospermum Kunth in terms of its botanical aspects, popular use, biological activity (pharmacology), and chemical compounds, intending to identify potential areas for innovative studies. The study considered literature published between 2010 - 2024 on the ethnobotany, pharmacology, botanical aspects, biological activity, and chemical compounds. Excluded from this study were eBooks, book chapters, patents, review articles, course completion articles, theses, and abstracts published in the proceedings of the event. Chem Draw software was used to draw a total of sixty-one bioactive compounds. The results show that six species of the Cochlospermum genus are documented as vital sources of traditional medicine. Ten species of this genus have been identified to contain secondary metabolites, including Cocholospermin A and B, polysaccharides, polyphenols (such as gallic and ellagic acids), flavonoids, and tannins. These compounds, such as polyphenols, flavonoids, and tannins, contribute to the pharmacological activities of this genus. The compounds in the Cochlospermum genus have demonstrated various biological activities, such as anti-inflammatory, antioxidant, antimicrobial, and potential antidiabetic properties. The genus has demonstrated some of these activities both in vitro and in vivo, making it of great pharmacological importance. This work presents a comprehensive overview of the botanical aspects, ethnopharmacology, biological activities, and chemical properties of the Cochlospermum genus. Its abundant chemical molecules can serve as an alternative source for the treatment of various diseases. This work provides a new perspective for future studies.

Optimization of ultrasonic-assisted extraction of polyphenols from Salvia deserta Schang flowers based on response surface methodology and deep neural network and analysis of its in vitro antioxidant activities

This study aims to establish the optimization of ultrasound-assisted extraction for active compounds from Salvia deserta Schang flowers. The effect of ultrasonic time, ratio of liquid to material, ethanol concentration, and ultrasonic power on the extraction efficiency of total polyphenols and three phenolic compounds (e.g., rosmarinic acid, caffeic acid, and protocatechuic acid was investigated. Response surface methodology (RSM) and deep neural network (DNN) model was performed to find out the optimum extraction conditions to maximize the output using a comprehensive evaluation score in parallel. Compared with the DNN model, the optimal working conditions of the extraction procedures based on the RSM model achieves the maximum yield of active components in S. deserta Schang flowers while requiring a shorter extraction time, lower energy consumption, and greater cost effectiveness. The optimal extraction process for the active components of S. deserta Schang flowers was determined as follows: 39 min of ultrasonic time, 1:37 (g/mL) ratio of liquid to material, 55% ethanol concentration, and 200 W of ultrasonic power. Additionally, S. deserta Schang flowers exhibited promising antioxidative activity, which was verified through several in vitro antioxidant trials, including DPPH, ABTS, ·OH, and phosphomolybdate method, suggesting their remarkable antioxidant capacity. This findings contribute effective, sustainable and valuable insights into the ultrasonic-assisted extraction of valuable compounds from S. deserta Schang flower, and the more biological activity of compounds from S. deserta Schang flower remains to be further investigated.

Technology for obtaining a dry complex of basfrom a plant of the from species Rosa beggeriana Schrenk

The study of medicinal plant raw materials as a source for the creation of unique and highly effective medicines based on it is of great importance for the development of pharmacy and medicine in Kazakhstan. Various types of rosehip contain a valuable complex of biologically active compounds (BAC), which causes their widespread use in folk medicine due to antioxidant, antiinflammatory, choleretic and body-strengthening effects, as well as pharmacopoeial objects of both the plants themselves and the medicines obtained on their basis. The object of this study – Rosa beggeriana Schrenk, which grows only in Asia, in particular Kazakhstan, Iran, and some parts of China, and has an almost unexplored valuable arsenal of compounds with biological activity, can increase the share of domestic medicines in the pharmaceutical market of the country. Goals and objectives. The purpose is to identify the suitability of raw material for further use in medicine. Research methods. The research object was collected during the fruiting season along the Ili River in the Almaty region and dried in accordance with recommendations for this type of raw material. In this study, chemical and physicochemical research methods were used. The article presents data on the establishment of the goodness of the studied Rosa beggeriana Schrenk plants and the dry complex of BAC obtained on a comparative context with the wellknown pharmacopoeia species of this plant family of Rosa canina plants, the mineral composition of macro- and microelements and the development of an optimal technology for obtaining a complex of biologically active substances from Rosa beggeriana Schrenk in the form of a dry extract. Conclusion. It has been established that this type of rose hip can be used for medical purposes and is not inferior in quality to the widespread type of rose hip Rosa canina. Parameters were also established under which the highest yield of raw materials can be obtained.

Synthesis, Antiproliferative Evaluation, and Molecular Docking of Thieno[3,2-e]indazole Derivatives

Background: Although indazole derivatives are rare and may not be available easily in nature, there are many reports demonstrating their pharmaceutical and other applications. Objective: This study aimed to synthesize new indazole derivatives and evaluate their antiproliferative activity to produce new anti-cancer agents. Method: The 2-aryllidenecyclohexane-1,3-dione derivatives 3a-c were obtained through the reaction of cyclohexane-1,3-dione with aromatic aldehydes used for the synthesis of thieno-[3,2-e]indazole derivatives. These derivatives were characterized by extensive analytical and spectral studies and were further used as starting materials for some heterocyclic transformations to produce biologically active compounds. The antiproliferative activities of the newly synthesized compounds were evaluated against the six cancer cell lines, A549, HT-29, MKN-45, U87MG, SMMC-7721, and H460. Most of the tested compounds exhibited high cytotoxicity except a few compounds. Results: In this study, new compounds were synthesized, characterized, and evaluated toward the selected six cancer cell lines. All tested compounds displayed potent c-Met enzymatic activity with IC50 values ranging from 0.25 to 10.30 nM and potent prostate PC-3 cell line inhibition with IC50 values ranging from 0.17 to 9.31mM. Conclusion: The results obtained in this work demonstrated that the variations in substituents within the aryl moiety, together with the attached heterocyclic ring, have a notable influence on the antiproliferative activity. The results obtained in this work encourage further work in the future.

Pharmacological evaluation and phytochemical profiling of butanol extract of L. edodes with in- silico virtual screening

L. edodes (L. edodes) is the most consumed mushroom in the world and has been well known for its therapeutic potential as an edible and medicinal candidate, it contains dietary fibers, vitamins, proteins, minerals, and carbohydrates. In the current study butanolic extract of mushroom was used to form semisolid butanol extract. The current study aimed to explore biometabolites that might have biological activities in n-butanol extract of L. edodes using FT-IR and GC–MS and LC–MS. The synergistic properties of bioactive compounds were futher assessed by performing different biological assays such as antioxidant, anti-inflammatory and antidiabetic. FTIR spectra showed different functional groups including amide N–H group, Alkane (C-H stretching), and (C = C stretching) groups at different spectrum peaks in the range of 500 cm−1 to 5000 cm−1 respectively. GC–MS profiling of n-butanol extract depicted 34 potent biomolecules among those dimethyl; Morphine, 2TMS derivative; Benzoic acid, methyl ester 1-(2-methoxy-1-methylethoxy)-2-propanol were spotted at highest range. Results indicate that L. edodes n-butanol extract showed a maximum anti-inflammatory potential 91.4% at 300 mg/mL. Antioxidant activity was observed by measuring free radical scavenging activity which is 64.6% at optimized concentration along with good antidiabetic activity. In-silico study executed the biopotential of active ingredient morphine which proved the best docking score (− 7.0 kJ/mol) against aldose reductase. The in-silico drug design analysis was performed on biometabolites detected through GC–MS that might be a potential target for sulfatase-2 to treat ruminated arthritis. Morphine binds more strongly (− 7.9 kJ/mol) than other bioactive constituents indicated. QSAR and ADMET analysis shown that morphine is a good candidates against ruminated arthritis. The current study showed that L. edodes might be used as potent drug molecules to cure multiple ailments. As mushrooms have high bioactivity, they can be used against different diseases and to develop antibacterial drugs based on the current situation in the world in which drug resistance is going to increase due to misuse of antibiotics so new and noval biological active compounds are needed to overcome the situation.

Study on Extraction, Identification, and Biological Activity of Compounds in Leaves of <i>Corylus mandshurica</i>

Study on Extraction, Identification, and Biological Activity of Compounds in Leaves of <i>Corylus mandshurica</i>

Recent Advances in the Synthesis of Fused‐Cyclic Quinolines

AbstractFused quinolines have gained substantial attention due to their significant biological and wide‐spectrum synthetic applications. This review supplies an encyclopedic document regarding the approaches developed for the synthesis of fused‐cyclic quinolines based on ring volume size reported thus far. This collected information will be valuable for medicinal chemists to obtain knowledge regarding designing new approaches in order to access biological active compounds.

High-Power Ultrasound (HPU) and Pulsed Electric Field (PEF) in the Hurdle Concept for the Preservation of Antioxidant Bioactive Compounds in Strawberry Juice-A Chemometric Evaluation-Part II.

In this work, the influence of high-power ultrasound (HPU) followed by pulsed electric field (PEF) in the hurdle concept (HPU + PEF) on the content of biologically active compounds (BACs) and antioxidant activity in strawberry juices stored at 4 °C/7 days was investigated. The HPU was performed with an amplitude of 25% and pulse of 50% during 2.5, 5.0 and 7.5 min, while the PEF was performed with an electric field strength of 30 kV cm-1 and frequency of 100 Hz during 1.5, 3 and 4.5 min. The results obtained indicate that the synergy of the mechanisms of action for technologies in the hurdle concept plays a critical role in the stability of BACs and antioxidant activity. Juices treated with HPU + PEF hurdle technology and kept at 4 °C for 7 days showed a statistically significant decrease in all BACs, antioxidant capacity and pH. Shorter HPU + PEF treatment times favored the preservation of BACs in juices. Regarding total phenolic compounds, flavonols, condensed tannins and antioxidant capacity, optimization of hurdle parameters showed that a shorter HPU treatment time of 2.5 min provided the best yield of these compounds. In summary, by optimizing and adjusting the parameters of the HPU/PEF technology, it is possible to produce functional strawberry juice.

Cobalt‐Catalyzed Enantioselective C−H Carbonylation towards Chiral Isoindolinones

AbstractTransition metal‐catalyzed enantioselective C−H carbonylation with carbon monoxide, an essential and easily available C1 feedstock, remains challenging. Here, we disclosed an unprecedented enantioselective C−H carbonylation catalyzed by inexpensive and readily available cobalt(II) salt. The reactions proceed efficiently through desymmetrization, kinetic resolution, and parallel kinetic resolution, affording a broad range of chiral isoindolinones in good yields with excellent enantioselectivities (up to 92 % yield and 99 % ee). The synthetic potential of this method was demonstrated by asymmetric synthesis of biological active compounds, such as (S)‐PD172938 and (S)‐Pazinaclone. The resulting chiral isoindolinones also serve as chiral ligands in cobalt‐catalyzed enantioselective C−H annulation with alkynes to construct phosphorus stereocenter.

Cobalt-Catalyzed Enantioselective C-H Carbonylation towards Chiral Isoindolinones.

Transition metal-catalyzed enantioselective C-H carbonylation with carbon monoxide, an essential and easily available C1 feedstock, remains challenging. Here, we disclosed an unprecedented enantioselective C-H carbonylation catalyzed by inexpensive and readily available cobalt(II) salt. The reactions proceed efficiently through desymmetrization, kinetic resolution, and parallel kinetic resolution, affording a broad range of chiral isoindolinones in good yields with excellent enantioselectivities (up to 92 % yield and 99 % ee). The synthetic potential of this method was demonstrated by asymmetric synthesis of biological active compounds, such as (S)-PD172938 and (S)-Pazinaclone. The resulting chiral isoindolinones also serve as chiral ligands in cobalt-catalyzed enantioselective C-H annulation with alkynes to construct phosphorus stereocenter.

Stability of Serotonin Transporter Essential Amino Acid Complex with Curcumin and Demethoxycurcumin Compounds as Antidepressant Candidates Based on In Silico Test

A Depression is a mental problem that is common in all communities, including teenagers. It is estimated that 10-20% of teenagers in the world experience mental health problems. Turmeric at a dose of 560mg/KgBW was shown to be effective as an antidepressant in Wistar rats (rattus norvegicus). Computers offer in silico test methods as a complement to in vitro and in vivo methods which are commonly used in the process of discovering and developing the biological activity of chemical compounds or natural materials as drug candidates. The research results show that MD simulations on the serotonin transporter complex protein with the ligand Demethoxycurcumin are more stable than curcumin and fluvoxamine. The results of identifying the molecular dynamics determinant of binding with the native ligand are amino acid SER336 and the reference ligand is amino acid SER438.

Phytochemical and pharmacological study of biologically active compounds and dry extracts of Populus rubrinervis Hort. Alb. buds of various polarities

The aim of the work was a phytochemical and pharmacological study of biologically active compounds (BACs) and Populus rubrinervis Hort. Alb. buds preparations of various polarities.Materials and methods. The object of the study was dry extracts of P. rubrinervis Hort. Alb. buds the samples of which were prepared in January–March 2023 in the Botanical Garden of Samara University (Samara, Russia). The separation of the amount of current substances was carried consecutively by the method of circulating extraction (chloroform), then, by the method of fractional percolation, a tincture was received on 70% ethyl alcohol (1:5). Pinostrobin was used as the standard sample (SS). The analysis of the substances was carried out by the TLC method. The electronic spectra registration was carried out with a spectrophotometer “Specord 40” (Analytik Jena, Germany). The study of the pharmacological (diuretic) activity of P. rubrinervis Hort. Alb. buds dried extracts was carried out on 60 white outbred rats of both sexes weighing 200–220 g in the experiments with aqueous diuresis.Results. P. rubrinervis Hort. Alb. buds dried extracts of various polarities (extract No. 1 (chloroform) and extract No. 2 (70% ethanol) were received. By the method of thin-layer chromatography, it was determined that the dominant complexes of the lipophilic nature with pinostrobin are isolated in extract No. 1, phenolic substances of the glycoside nature prevail in extract No. 2. Despite various polarities of the extragents, spectral characteristics of extract No. 2 have significant similarities with extract No. 1. When studying the diuretic activity, it was established that when SS pinostrobin was injected at a dose of 1 mg/kg, for 4 h of the experiment, an isolated increase in diuresis was noted (from 1.72±0.11 to 1.97±0.03 ml, p <0.05); at the same time, an isolated increase in creatininuresis (from 1.50±0.29 to 2.39±0.15 mg, p <0.05) was observed during 24 h of the experiment. When extract No. 2 was injected at a dose of 10 mg/kg, there was a moderate significant increase in diuresis (from 1.82±0.02 to 2.07±0.04 ml and from 2.38±0.39 to 3.02±0.11 ml, p <0.05) and a significant increase in creatininuresis (from 0.14±0.01 to 0.19±0.03 mg and from 2.31±0.42 to 2.79±0.51 mg, p <0.05) for 4 and 24 h of the experiment, respectively.Conclusion. The extraction separation of the amount of P. rubrinervis Hort. Alb. buds by the polarity degree was carried out. Pinostrobin SS at a dose of 1 mg/kg and extract No. 2 at a dose of 10 mg/kg had a diuretic activity, in connection with which they are promising in terms of the development of effective drugs.

Natural ten-membered lactones: sources, structural diversity, biological activity, and intriguing future.

Covering: 2012 to 2022Ten-membered lactones (TMLs) are an interesting and diverse group of natural polyketides that are abundant in fungi and, to a lesser extent, in bacteria, marine organisms, and insects. TMLs are known for their ability to exhibit a wide spectrum of biological activity, including phytotoxic, cytotoxic, antifungal, antibacterial, and others. However, the random discovery of these compounds by scientific groups with various interests worldwide has resulted in patchy information about their distribution among different organisms and their biological activity. Therefore, despite more than 60 years of research history, there is still no common understanding of the natural sources of TMLs, their structural type classification, and most characteristic biological activities. The controversial nomenclature, incorrect or erroneous structure elucidation, poor identification of producing organisms, and scattered information on the biological activity of compounds - all these factors have led to the problems with dereplication and the directed search for TMLs. This review consists of two parts: the first part (Section 2) covers 104 natural TMLs, published between 2012 and 2022 (after the publishing of the previous review), and the second part (Section 3) summarizes information about 214 TMLs described during 1964-2022 and as a result highlights the main problems and trends in the study of these intriguing natural products.

Suberoylanilide Hydroxamic Acid Analogs with Heteroaryl Amide Group and Different Chain Length: Synthesis and Effect on Histone Deacetylase.

This review covers the last 25 years of the literature on analogs of suberoylanilide hydroxamic acid (SAHA, known also as vorinostat) acting as an HDAC inhibitor. In particular, the topic has been focused on the synthesis and biological activity of compounds where the phenyl group (the surface recognition moiety, CAP) of SAHA has been replaced by an azaheterocycle through a direct bond with amide nitrogen atom, and the methylene chain in the linker region is of variable length. Most of the compounds displayed good to excellent inhibitory activity against HDACs and in many cases showed antiproliferative activity against human cancer cell lines.

Extracts from Four Species of Xylotrophic Basidiomycetes Growing in the Middle Urals (Russia) Revealed Cytotoxic Effects on Model Object Drosophila melanogaster

In our study, four species of wood-decaying fungi with perennial fruiting bodies were used as the source of biologically active compounds (BACs) - <i>Inonotus obliquus</i> (chaga), <i>Fomitopsis pinicola, Fomes fomentarius,</i> and <i>Ganoderma applanatum</i>. Fungi have a wide range of secondary metabolites but are used much less frequently than plants in both folk and official medicine. Fungotherapy could be considered a promising trend in the development of modern natural therapy. Therefore, qualitative and quantitative analyses of the extracts were carried out. The cytotoxic and genotoxic effects of aqueous-alcoholic extracts, obtained from fungal fruiting bodies were assessed after application on <i>Drosophila melanogaster</i>. The frequency of the larvae lethally, SMART mosaicism, the <i>GstD1</i> gene expression and the DNA damage were studied. The addition of 0.5% of fungal extracts to the food substrate did not cause a significant change in the lethality level in <i>D. melanogaster</i>. All extracts caused an increase in the degree of DNA damage. The greatest effect was caused by extract from <i>I. obliquus</i> and <i>G. applanatum</i>. Chaga extract caused a significant increase in the expression level of the <i>GstD1</i> gene. <i>F. fomentarius</i> extract exhibited the lowest level of DNA damage and reduced <i>GstD1</i> gene expression. The <i>F. fomentarius</i> extract showed a pronounced antiproliferative effect. So, <i>Drosophila melanogaster</i> could be used as the preliminary test object for early studies of biological activities from natural raw materials as it is much cheaper compared with cell lines and vertebrate models.

Indole-containing pharmaceuticals: targets, pharmacological activities, and SAR studies.

Indole is a prestigious heterocyclic skeleton widely found in both naturally-occurring and biologically-active compounds. Pharmaceutical agents containing an indole skeleton in their framework possess a wide range of pharmacological properties, including antiviral, antitumor, analgesic, and other therapeutic activities, and many indole-containing drugs have been proven to have excellent pharmacokinetic and pharmacological effects. Over the past few decades, the FDA has approved over 40 indole-containing drugs for the treatment of various clinical conditions, and the development of indole-related drugs has attracted significant attention from medicinal chemists. This review aims to provide an overview of all the approved drugs that contain an indole nucleus, focusing on their targets, pharmacological activities, and SAR studies.

The influence of conversion creatine and guanidinoacetic acid from zwitterionic to cationic form on their solubility in water - a thermodynamic study

In this work, the solubility of creatine, creatinine, guanidinoacetic acid and their hydrochlorides in water at atmospheric pressure and in the temperature range T 293.15?313.15 K was determined by the gravimetric method. The thermodynamic parameters of dissolution in water for the mentioned compounds were calculated. The solubility increases significantly by converting the zwitterionic structures of creatine and guanidinoacetic acid into a cationic form, i.e., hydrochloride salt. The effect of increasing solubility is more pronounced for guanidinoacetic acid and decreases with temperature for both compounds. A simple process of transforming the electrically neutral zwitterionic structures into cations represents a good way to increase the solubility in water and bioavailability of biologically active compounds.

On the origin of the electronic and magnetic circular dichroism of naphthyl C-glycosides: Anomeric configuration

Aryl C-glycosides, in which the glycosidic bond is changed to a carbon–carbon bond, are an important family of biologically-active compounds. They often serve as secondary metabolites or exhibit antibiotic and cytostatic activities. Their stability to hydrolysis has made them attractive targets for new drugs. Their conformational behavior often strongly influences the resulting function. Their detailed structural and conformational description is thus highly desirable.This work studies the structure of three different naphthyl C-glycosides using UV–vis absorption as well as electronic and magnetic circular dichroism. It also describes their conformational preferences using a combination of molecular dynamics and DFT calculations. The reliability of these preferences has been verified by simulations of spectral properties and a comparison with their measured spectra. In particular, ECD spectroscopy has been shown to distinguish easily between α- and β-pseudoanomers of aryl C-glycosides. Computer simulations and spectral decomposition have revealed how the resulting ECD patterns of the naphthyl glycosides studied are influenced by different conformer populations. In conclusion, reliable ECD patterns cannot be calculated by separating the naphthyl rotation from other conformational motions. MCD patterns have been similar for all the naphthyl C-glycosides studied. No clear diagnostic features have been found for either the pseudoanomeric configuration or the preferred hydroxymethyl rotamer. Nevertheless, the work has demonstrated the potential of MCD for the study of aryl glycosides interacting with proteins.