Potential Biological Activity Research Articles

The Synthesis of Australine and its Stereoisomers as Naturally Pyrrolizidine Alkaloids

Abstract: Natural products are important from researchers’ perspectives due to their importance and applicability. Polyhydroxylated pyrrolizidine alkaloids are sugar mimics and received a growing interest in the last few years. Australine is a naturally polyhydroxylated pyrrolizidine, which was isolated from the seeds of Castanospermum austral, and exhibits potent biological activities such as inhibited glycosidases, as well as anti-virus, and anti-HIV activities. Thus, there is a considerable deal of interest in the synthesis of these classes of compounds. Different synthetic strategies and methodologies for the preparation of Australine and its stereoisomers were considered.

Study on fermentation preparation, physicochemical properties and biological activity of carboxymethylpachymaran with different degrees of substitution.

Carboxymethylpachymaran (CMP) is created by carboxymethylating pachyman (PM), which increases its water solubility and enhances a number of biological activities. Traditional polysaccharides modified by carboxymethylation employ strong chemical techniques. Carboxymethylcellulose (CMC) has been used previously for liquid fermentation to carboxymethyl modify bacterial polysaccharides. This theory can be applied to fungal polysaccharides because Poria cocos has the ability to naturally utilize cellulose. CMC with different degrees of substitution (DS) (0.7, 0.9 and 1.2) were added to P. cocos fermentation medium, and CMPs with different DS (0.38, 0.56 and 0.78, respectively) were prepared by liquid fermentation. The physical and chemical properties and biological activities of the CMPs were determined. Their structures were confirmed by Fourier transform infrared (FTIR) spectroscopy and monosaccharide composition. With the increase of DS, the viscosity and viscosity-average molecular weight of CMPs decreased, whereas polysaccharide content and water solubility increased, although the triple helix structure was not affected. The results of bioactivity assay showed that the higher the DS of CMPs, the higher the 2,2-diphenyl-1-picrylhydrazyl radical scavenging ability, and the stronger the bacterial inhibition ability. The present study has developed a method for producing CMPs by P. cocos liquid fermentation. The results of the study confirm that enhancing the DS of CMP could effectively enhance its potential biological activity. The findings provide safe and reliable raw materials for creating CMP-related foods and encourage CMP application in the functional food industry. © 2024 Society of Chemical Industry.

Carvacrol and Thymol Content Affects the Antioxidant and Antibacterial Activity of Origanum compactum and Thymus zygis Essential Oils.

Essential oils are of great interest due to their potent pharmaceutical and biological activities. In this study, essential oils extracted from Origanum compactum and Thymus zygis originating from the Middle Atlas of Morocco were investigated. Their chemical compositions were analyzed using gas chromatography and mass spectrometry, while the assessment of the trapping power of the radical (DPPH: 1,1-diphenyl-2-picrylhydrazyl) and the reducing antioxidant potential of ferric ions (FRAP: Ferric Reducing Antioxidant Power) were performed in order to evaluate the antioxidant activity. Their antibacterial potency was tested against six bacterial strains through the disk diffusion method. The chromatography analyses of the extracted essential oils highlighted the presence of two main components, namely carvacrol at 75.70% in O. compactum and thymol at 40.67% in T. zygis. The antioxidant activity tests showed that both essential oils demonstrated a significant antioxidant activity comparable to the positive control (e.g., ascorbic acid). The antibacterial activity results showed a strong antimicrobial effect for both essential oils, compared to synthetic antibiotics. This study affirms the presence of bioactive components with interesting antioxidant and antibacterial activities in the essential oils extracted from Origanum compactum and Thymus zygis, which could find several applications in the food and pharmaceutical industries through the substitution of synthetic antioxidants and antibiotics.

Approach to synthesis and study of pharmacological effects of new 1,3,5-triazine derivatives

Introduction. Among the derivatives of 1,3,5-triazine, compounds with different biological activity are known, but there are few drugs of this structure on the pharmaceutical market. Thus, the production of new medicines based on a triazine core, as well as the study of their biological activity is an urgent direction. Objective: synthesis of new 1,3,5-triazine derivatives using the reaction of recycling of 2,5-disubstituted-4-hydroxy-6H-1,3-oxazine-6-ones by 1,3-binucleophiles to obtain different substituents at positions 2,4,6 in one stage, as well as assessment of acute toxicity, diuretic activity in silico and in vivo for synthesized products. Material and methods. The target compounds were obtained as a result of the interaction of 2,5-disubstituted-4-hydroxy-6H-1,3-oxazine-6-ones and S-methylisothiourea of hemisulfate in the presence of an equimolar amount of sodium methylate in a methanol medium. Prediction of acute toxicity of the studied compound was carried out using the local version of the GUSAR software. Computer screening of biological activity was carried out using the PASS program. Acute toxicity in vivo was determined on white male mice. For experimental evaluation of the diuretic activity of the obtained compounds in vivo, the Taylor, Topliss model was included in the work. Results. 2-(methylsulfanyl)-4-(4-nitrophenyl)-6-ethyl-1,3,5-triazine, 2-(methylsulfanyl)-4-(4-nitrophenyl)-6-(pentane-1-yl)-1,3,5-triazine were obtained with a yield of 72% and 69%, respectively. The structure of the obtained compounds was proved using 1H and 13C NMR spectroscopy. The predicted and experimental data of acute toxicity correlate with each other, and the studied compounds belong to the class "low-toxic". During the screening of biological activity using the PASS program, data on the estimated diuretic activity were obtained. Studies of biological activity in vivo have shown that the target compounds have pronounced diuretic activity. Conclusion. New compounds have been synthesized, their structure has been proved using modern physico-chemical analysis methods. The results of computer prediction made it possible to determine the potential class of toxicity and identify potential biological activity. With the help of experimental pharmacological studies, it has been proved that the studied compounds have low toxicity and exhibit pronounced diuretic activity.

Volatile Compounds and Potential Biological Activities of Essential Oil of Citrus amblycarpa Hassk. Ochse

Volatile Compounds and Potential Biological Activities of Essential Oil of Citrus amblycarpa Hassk. Ochse

Phytochemical composition and biological activity of native Australian ginger (Alpinia caerulea)

The edible, endemic Australian species Alpinia caerulea belongs to the same family as ginger and turmeric. The rhizome and fruit have a mild ginger-like flavour, but there is very little information on its chemical composition or potential biological activities. This study found low levels of ascorbic acid in the fruit and fruit capsule (2.3–3.4 mg/100 g fresh weight), as well as detecting six polyphenols (rutin, quercetin-3-glucoside, quercetin, vanillic acid, kaempferol and chlorogenic acid) across all of the plant parts. The volatile profile of the rhizome was also explored for the first time. The volatiles were dominated (91.7%) by (E)-8(17),12-labdadiene-15,16-dial, but included 20 other minor constituents; mainly monoterpenes and sesquiterpenes. Extracts showed no inhibitory activity against tyrosinase or cyclooxygenase-2 (COX-2), but moderate anti-acetylcholinesterase was found for the rhizome and stem extracts. Further investigation into A. caerulea and other species from this genus will help to elucidate their full nutritional and bioactive potential.

Distribution, Diversity and Biochemical Analysis of Endophytic Fungi Associated with Chromolaena odorata

Chromolaena odorata is a medicinal plant that possesses several properties, including antibacterial, antifungal, anti-inflammatory, anticancer, antioxidant, etc., and has been used in traditional medicine in various parts of the world. Medicinal plants are associated with endophytic fungi that have potential biological activities as well as protect the plant from biotic and abiotic agents. In this study, endophytic fungi were isolated from the leaves, stems, roots, and inflorescence of C. odorata and identified morphologically. Nineteen sporulating endophytic fungi belonging to 9 genera, 8 families and 4 classes, and three sterile forms were obtained. The isolation data recorded were used to calculate Isolation rate, Colonization frequency, Infection rate and Relative occurrence of different groups of fungi. The highest Isolation rate was found in the stem part (34.75%); the highest overall Colonization frequency (%) was shown by Chaetomium globosum (8.51%); the maximum Infection rate was found in root segments (77.86%); and the maximum isolate belongs to Sordariomycetes, showing 43.50%. Simpson’s dominance index, Simpson’s diversity index, Species richness, Shannon-Wiener index and Evenness (E) index were calculated to reveal diversity indices. The maximum diversity was recorded in the leaf part (0.99), and the maximum number of endophytic fungal species was observed in stem segments. The production of biochemicals was analyzed qualitatively, and it was observed that all the isolates produce flavonoids and phenols. This indicates that endophytic fungi are a storehouse of natural compounds and can be applied in agriculture, medicine, and pharmaceutical industries.

Effect of tea polyphenols supplement on growth performance, antioxidation, and gut microbiota in squabs.

Early life nutritional supplementation can significantly improve pigeon health. Both the nutritional crops of parental pigeons and the intestinal development of squabs play key roles in the growth rate of squabs. Tea polyphenols (TPs), as natural plant extracts, exhibit potential biological activities. However, the impact of TPs on the intestinal function of squabs is not known. This study evaluated the effects of TPs on growth performance, immunity, antioxidation, and intestinal function in squabs. A total of 432 young pigeons (1 day old) were divided into four groups: a control group (fed a basic diet) and three treatment groups (low, medium, and high dose groups; 100, 200, and 400 mg/kg TPs, respectively). On the 28th day, samples of serum, mucosal tissue, and digests from the ileum of squabs were collected for analysis. The results revealed that TP supplementation significantly reduced the feed-to-meat ratio and improved the feed utilization rate and serum biochemical indices in squabs. Additionally, it enhanced the intestinal barrier function of birds by promoting intestinal development and integrity of tight junctions and regulating digestive enzyme activities and intestinal flora. Mechanistically, TPs activated the Nrf2-ARE signaling pathway, which may be associated with improved antioxidant and immune responses, correlating with an increased abundance of Candida arthritis and Corynebacterium in the ileum.

New N-Terminal Fatty-Acid-Modified Melittin Analogs with Potent Biological Activity.

Melittin, a natural antimicrobial peptide, has broad-spectrum antimicrobial activity. This has resulted in it gaining increasing attention as a potential antibiotic alternative; however, its practical use has been limited by its weak antimicrobial activity, high hemolytic activity, and low proteolytic stability. In this study, N-terminal fatty acid conjugation was used to develop new melittin-derived lipopeptides (MDLs) to improve the characteristics of melittin. Our results showed that compared with native melittin, the antimicrobial activity of MDLs was increased by 2 to 16 times, and the stability of these MDLs against trypsin and pepsin degradation was increased by 50 to 80%. However, the hemolytic activity of the MDLs decreased when the length of the carbon chain of fatty acids exceeded 10. Among the MDLs, the newly designed analog Mel-C8 showed optimal antimicrobial activity and protease stability. The antimicrobial mechanism studied revealed that the MDLs showed a rapid bactericidal effect by interacting with lipopolysaccharide (LPS) or lipoteichoic acid (LTA) and penetrating the bacterial cell membrane. In conclusion, we designed and synthesized a new class of MDLs with potent antimicrobial activity, high proteolytic stability, and low hemolytic activity through N-terminal fatty acid conjugation.

Cyclohexene oxide CA, a derivative of zeylenone, exhibits anti-cancer activity in glioblastoma by inducing G0/G1 phase arrest through interference with EZH2.

Introduction: Due to its highly aggressiveness and malignancy, glioblastoma (GBM) urgently requires a safe and effective treatment strategy. Zeylenone, a natural polyoxygenated cyclohexenes compound isolated from Uvaria grandiflora, has exhibited potential biological activities in various human diseases, including tumors. Methods: We designed and synthesized a series of (+)-Zeylenone analogues and evaluated their anti-GBM roles through structural-activity analysis. Cell Counting Kit-8, TUNEL, transwell and flow cytometry were employed for investigating the anticancer effects of CA on GBM cells. Western blotting, molecular docking, qRT-PCR and ChIP assays were performed to reveal the underlying mechanisms by which CA regulates the GBM cell cycle. The nude mouse xenograft model, HE staining, immunohistochemistry and was used to evaluate the anticancer effect of CA in vivo. Results: We identified CA ((1R, 2R, 3S)-3-p-fluorobenzoyl-zeylenone) as having the lowest IC50 value in GBM cells. CA treatment significantly inhibited the malignant behaviors of GBM cells and induced G0/G1 phase arrest in vitro. Furthermore, we validated the molecular mechanism by which CA interferes with EZH2, attenuating the down-regulation of cyclin-dependent kinase inhibitors p27 and p16 by the PRC2 complex. By establishing orthotopic nude mice models, we further validated the inhibitory role of CA on tumorigenesis of GBM cells in vivo and its potential values to synergistically potentiate the anti-tumor effects of EZH2 inhibitors. Conclusion: Overall, this paper elucidated the anti-GBM effects and potential mechanisms of CA, and may provide a therapeutic drug candidate for GBM treatment.

Eco friendly, green route method for the preparation of poly ethylene glycol (PEG) mediated surface modified iron oxide nanoparticles (PEG‐IONps) with potential biological activities

AbstractAmong the various nanoparticles, excessively paramagnetic iron oxide nanoparticles assume an outstanding job in biomedicine, mostly as Nano clinical imaging and treatment. These nanoparticles’ effective working relies on superficial alteration utilizing different specialists. Among them, polyethylene glycol (PEG)—biocompatible polymer is primarily used attributable to its unmistakable qualities. In this examination, the impact of PEG covering on the counter bacterial and against proliferative properties of iron oxide nanoparticles has been considered. PEG‐covered nanoparticles were incorporated by co‐precipitation technique portrayed by UV–visible spectroscopy, Fourier change infrared spectroscopy, electron microscopy, X‐ray diffraction, and vibrating test magnetometer thinks about which uncovers exceptionally stable crystalline, circular, nanoparticles with high polarization impact. Hostile to the bacterial movement was examined against Staphylococcus aureus, and Pseudomonas aeruginosa uncovers PEGlated IONps displayed upgraded action against both tried endure lower fixations. A higher zone of restraint was construed from PEGlated IONps treatment. Hostile to proliferative activity was contemplated against the PC3 cell line (Prostate cancer). PEGlated IONps prompted the most extreme decrease in cell suitability and changed the cell design by chronicle fracture and build‐up of atomic material. PEGlated IONps treatment uncovered a high rate of receptive oxygen species (ROS), which brought about apoptosis or necrotic cell demise. The present discoveries suggest that PEGlated IONps synthesized in this examination could be utilized as potential bioactive operators against medication‐safe pathogenic bacterial strains and malignant growth cells.

The Relationship between Preparation and Biological Activities of Animal-Derived Polysaccharides: A Comprehensive Review.

Polysaccharides are biomolecules found in microorganisms, plants, and animals that constitute living organisms. Glycosaminoglycans, unique acidic polysaccharides in animal connective tissue, are often combined with proteins in the form of covalent bonds due to their potent biological activity, low toxicity, and minimal side effects, which have the potential to be utilized as nutrition healthcare and dietary supplements. Existing studies have demonstrated that the bioactivity of polysaccharides is closely dependent on their structure and chain conformation. The characteristic functional groups and primary structure directly determine the strength of activity. However, the relationship between structure and function is still unclear, and the target and mechanism of action are not fully understood, resulting in limited clinical applications. As a result, the clinical applications of these polysaccharides are currently limited. This review provides a comprehensive summary of the extraction methods, structures, and biological activities of animal-derived polysaccharides that have been discovered so far. The aim is to promote developments in animal active polysaccharide science and provide theoretical support for exploring other unknown natural products.

Biogenic zinc selenide nanoparticles fabricated using Rosmarinus officinalis leaf extract with potential biological activity

Zinc selenide nanoparticles (ZnSe) are semiconductor metals of zinc and selenium. ZnSe NPs are advantageous for biomedical and bio-imaging applications due to their low toxicity. ZnSe NPs can be used as a therapeutic agent by synthesizing those using biologically safe methods. As a novel facet of these NPs, plant-based ZnSe NPs were fabricated from an aqueous extract of Rosmarinus officinalis L. (RO extract). Physiochemical analyses such as UV-visible and FTIR spectroscopy, SEM-EDX and TEM Imaging, XRD and DLS-Zeta potential analyses confirmed the biological fabrication of RO-ZnSe NPs. Additionally, Ro-ZnSe NPs were investigated for their bioactivity. There was an apparent peak in the UV-visible spectrum at 398 nm to confirm the presence of ZnSe NPs. FTIR analysis confirmed RO-extract participation in ZnSe NPs synthesis by identifying putative functional groups associated with biomolecules. TEM and SEM analyses revealed that RO-ZnSe NPs have spherical shapes in the range of 90–100 nm. According to XRD and EDX analysis, RO-ZnSe NPs had a crystallite size of 42.13 nm and contain Se and Zn (1:2 ratio). These NPs demonstrated approximately 90.6% antioxidant and antibacterial activity against a range of bacterial strains at 100 µg/ml. Antibiofilm activity was greatest against Candida glabrata and Pseudomonas aeruginosa at 100 g/ml. Accordingly, the IC50 values for anticancer activity against HTB-9, SW742, and HF cell lines were 14.16, 8.03, and 35.35 g/ml, respectively. In light of the multiple applications for ZnSe NPs, our research indicates they may be an excellent option for biological and therapeutic purposes in treating cancers and infections. Therefore, additional research is required to determine their efficacy.

Comparative metabolomic analysis reveals nutritional properties and pigmentation mechanism of tea-scented rosehips.

The fruits of the genus Rosa, commonly known as rosehips, have attracted significant attention owing to their rich content of various bioactive compounds. However, their utility is generally secondary to the ornamental appeal of their flowers. This study aimed to explore the quality differences among tea-scented rosehips found in Yunnan, China, including those of Rosa odorata var. odorata (RO), Rosa odorata var. gigantea (RG), and Rosa yangii (RY). Morphological characteristics, chemical composition, and antioxidant activity of their fruits were evaluated. The study revealed significant variability in composition and biological activities based on fruit color. RO exhibited the highest levels of polyphenols, flavonoids, anthocyanins, carotenoids, and vitamin C, with the strongest antioxidant activity (10.99 μmol Trolox·g-1 ), followed by RG (7.91 μmol Trolox·g-1 ) and RY (6.52 μmol Trolox·g-1 ). This supports RO's potential as a functional food source. Untargeted metabolomics identified and quantified 502 metabolites, with flavonoids (171) and phenolic acids (147) as the main metabolites. The differential metabolites among the fruits are primarily enriched for flavonoid biosynthesis and phenylpropanoid biosynthesis pathways. Insights into color formation supported the role of anthocyanins, flavones, and flavonols in fruit color variation. Tea-scented rosehips offer vibrant colors and high nutritional value with potent biological activities. Rosa odorata var. odorata stands out as a functional food source owing to its rich bioactive compounds. These findings lay the groundwork for utilizing rosehips in functional foods, health supplements, and food additives, emphasizing the practical and beneficial applications of Rosa spp. independent of their ornamental value. © 2023 Society of Chemical Industry.

An in silico analysis of the interaction of marine sponge-derived bioactive compounds with type 2 diabetes mellitus targets DPP-4 and PTP1B

Type 2 diabetes is a medical condition involving elevated blood glucose levels resulting from impaired or improper insulin utilization. As the number of type 2 diabetes cases increases each year, there is an urgent need to develop novel drugs having new targets and/or complementing existing therapeutic protocols. In this regard, marine sponge-derived compounds hold great potential due to their potent biological activity and structural diversity. In this study, a small library of 50 marine sponge-derived compounds were examined for their activity towards type 2 diabetes targets, namely dipeptidyl peptidase-4 (DPP-4) and protein tyrosine phosphatase 1B (PTP1B). The compounds were first subjected to molecular docking on protein models based on their respective co-crystal structures to assess binding free energies (BFE) and conformations. Clustering analysis yielded BFE that ranged from 24.54 kcal/mol to −9.97 kcal/mol for DPP-4, and from −4.98 kcal/mol to −8.67 kcal/mol for PTP1B. Interaction analysis on the top ten compounds with the most negative BFE towards each protein target showed similar intermolecular interactions and key interacting residues as in the previously solved co-crystal structure. These compounds were subjected to absorption, distribution, metabolism, excretion, and toxicity (ADMET) profiling to characterize drug-likeness and combining the results from these analyses, (S)-6’-debromohamacanthin B was identified as a potential multi-target inhibitor of DPP-4 and PTP1B, having favorable protein interaction, no Lipinski violations, good gastrointestinal (GI) tract absorption, blood-brain barrier (BBB) penetration, and no predicted toxicity. Finally, the interaction of (S)-6’-debromohamacanthin B with the two proteins was validated using molecular dynamics simulations over 100 ns through RMSD, radius of gyration, PCA, and molecular mechanics Poisson-Boltzmann surface area (MMPBSA) confirming favorable interactions with the respective proteins. Communicated by Ramaswamy H. Sarma

Optimization of silver nanoparticles synthesis via Plackett-Burman experimental design: in vitro assessment of their efficacy against oxidative stress-induced disorders.

Nanoparticles possess remarkable biological activities owing to their small size and large surface-to-volume ratio. Given the increasing adoption of environmentally sustainable practices in silver nanoparticle (AgNP) fabrication, this study presents a simple lab-scale green synthesis of AgNPs using banana peels. Large amounts of banana peels are disposed off in Pakistan every day. As the fruit is available throughout the year and contains many active components with potent biological activities, we aimed to synthesize silver nanoparticles using its peel, through an energy-efficient and inexpensive route. The synthesis was optimized according to the Plackett-Burman design (PDB) of experiments, which helped identify significant factors and saved time and resources. For characterization, UV-Vis spectroscopy and SEM-EDX analysis were performed, revealing spherical particles in the 45-65 nm size range. To investigate functional groups, FT-IR analysis was performed, revealing the presence of N-C[double bond, length as m-dash]O amide I bonds of proteins, C-H bonds of tannins and C-O bonds involved in the capping and stabilization of nanoparticles. The free radical scavenging property of banana peel-mediated silver nanoparticles (BP-AgNPs) was studied against 2,2-diphenyl-1-picrylhydrazyl (DPPH), and the antioxidant potential was found to be 79% at 500 μg mL-1 concentration. The efficacy of BP-AgNPs with respect to certain biological activities were studied through anti-inflammatory assays, which demonstrated better results compared to a standard drug, and an anti-glycation assay, wherein only 4% of AGEs were formed, demonstrating 96% of AGE inhibition in vitro. The findings not only demonstrated the effectiveness of the PBD approach but also highlighted the potent property of BP-AgNPs against disorders associated with oxidative stress.

Advances in the total synthesis of bis- and tris-indole alkaloids containing N-heterocyclic linker moieties.

The past several years have seen an increase in the discovery and isolation of natural products of the indole alkaloid class. Bis- and tris-indole alkaloids are classes of natural products that have been shown to display diverse, potent biological activities. Of particular interest are bis- and tris-indole alkaloids containing N-heterocyclic linker moieties. It has been reported that more than 85% of biologically active compounds contain one or more heterocyclic moieties; of these, N-heterocycles have been identified as the most prevalent. The goal of this review is to provide a detailed overview of the recent advances in isolation and total synthesis of bis- and tris-indole alkaloids that contain N-heterocyclic linker moieties. The known biological activities of these natural products will also be discussed.

Decarboxylative photoinduced ligand-to-metal charge transfer reaction: synthesis of 2-substituted chroman-4-ones.

In this manuscript, a photoinduced ligand-to-metal charge transfer (LMCT) approach, employing transition-metal-based photocatalysts, for the efficient alkylation of electron-poor olefin is described. The developed redox-neutral process benefits from mild reaction conditions and involves a wide range of chromone-3-carboxylic acids as well as nucleophiles amenable to selective C-H functionalization leading to the formation of 2-substituted chroman-4-one compounds with potential biological activity.

Antioxidant activity of chia flour as a food supplement in a cellular model: Repercussions of processing and in vitro digestion

Food processing and digestion can alter bioactive compound composition of food, affecting their potential biological activity. In this study, we evaluated the direct and protective antioxidant effects of polyphenols extracted from defatted chia flour (DCF) (salviaflaside, rosmarinic and fertaric acid as major compounds), sweet cookies supplemented with DCF (CFC) (same major compounds), and their digested fractions (rosmarinic acid, salviaflaside, fertaric and salvianolic E/B/L acid as major compounds) in HepG2 cells in basal and in oxidative stress conditions. DCF showed protective antioxidant effects by decreasing reactive oxygen species (ROS) and protein oxidation products (POP) while increasing reduced glutathione (GSH). Additionally, CFC revealed similar protective effects and even showed enhanced modulation of the antioxidant system due to the activation of antioxidant enzymes. However, the digested fractions only decreased ROS, indicating continued antioxidant effects. This study underscores the importance of evaluating manufacturing and digestion effects to confirm a food's antioxidant properties.

Effect of substituents on the 1O2 production and biological activity of (N^N^N)Pt(py) complexes.

Twelve (N^N^N)platinum pyridyl complexes, (N^N^N)Pt(pyF), were synthesised and investigated for their singlet oxygen generation and potential biological activities. They exhibited 1IL and 1MLCT absorption transitions at approximately 325 and 360 nm, identified through TD-DFT calculations. Luminescence was observed only in the L1-derived compounds in solution, with a dual emission with the main contribution of phosphorescence under deaerated conditions. Room temperature phosphorescence was detected in all solid-state cases. Electron-withdrawing substituents at specific positions (R1 and X) and the number of fluorine atoms in R2 were found to enhance the photosensitizing capabilities of these compounds. Biological assessments, including cytotoxicity and photocytotoxicity, were conducted to evaluate their potential as chemotherapeutic agents and photosensitizers. Complexes with chloro substitution in the N^N^N tridentate ligand of the central pyridine ring exhibited promising chemotherapeutic properties. Ancillary pyridine ring substitution became significant under irradiation conditions, with fluoromethylated substituents enhancing cytotoxicity. Complex 2-CF3 was the most efficient singlet oxygen producer and a highly effective photosensitizer. CHF2-substituted complexes also showed improved photosensitizing activity. DNA binding studies indicated moderate interactions with DNA, offering insights into potential biological applications.