Broad Range Of Biological Properties Research Articles

Genus Pelargonium: General Aspects, Potential Pharmacological Applications, Extraction Methods and Applications in Industry

Pelargonium is a genus belonging to the Geraniaceae family, found within the Angiospermae division, the Dicotyledoneae class, and the Geraniales order. It is the second biggest genus of the family; it has about 280 taxa. In the past, Pelargonium species were characterized by presenting large and red roots, from which preparations were used in the treatment of diarrhea, dysentery, anemia, and weakness. This article is a bibliographic search carried out in different databases that focus on chemical and physical features of Pelargonium and also some of the extraction methods. Currently, there are a variety of studies that affirm the different properties of the species of the genus Pelargonium, among which the activities stand out: antituberculous, antioxidant, antitumor, antibacterial, antifungal, antiviral, and immunomodulatory. Therefore, they are used in both the pharmaceutical and food industries. The most relevant species of this genus is Pelargonium sidoides, which has a broad range of biological properties, from which a standardized hydroalcoholic root extract was formulated, known as EPs® 7630, which has been authorized by the EMA and is listed in the European Pharmacopoeia. It is important to continue with the clinical studies to be able to analyze the other properties that Pelargonium has in order to contribute to the pharmaceutical industry.

Screening and characterization of bioactive compounds from two epiphytic microlichen and evaluation of their in vitro antioxidant activity

BackgroundLichens in symbiosis produce a wide range of primary and secondary fine compounds in extreme environmental conditions that have a broad range of biological properties as well as antioxidant potential and can be used in future pharmaceuticals as a natural source of antioxidant molecules.ResultsThe two microlichen species collected are identified based on morphological and molecular techniques; further studies are carried out by analyzing phytochemicals (FTIR, GC MS), and antioxidant assays are evaluated. The non-enzymatic antioxidant activity is evaluated by DPPH and FRAP assays. The methanol extract of both lichens showed virtuous DPPH scavenge with IC50 of P. nitida (125.76 ± 0.023 µg/ml) and G. scripta IC50 (176.90 ± 0.058 µg/ml). FRAP activity was prominent in the methalonic extract. The enzymatic antioxidant activity is observed by SOD and catalase activity. The cytosolic (Cu–Zn-SOD and Fe-SOD) and mitochondrial SOD (Mn-SOD) are detected in lichens, though P. nitida shows mitochondrial Mn-SOD and cytosolic Cu–Zn-SOD and Fe-SOD, whereas G. scripta has a single cytosolic Cu–Zn-SOD; however, two isoforms of catalase were reported. GC–MS analysis screened bioactive metabolites such as phenols, Quinons, heterocyclic compounds, benzofurans, fatty acids, pyrans, carboxylic acid, aliphatic aldehydes, organic alcohol, fluorinated aliphatic substances, ketones, terpenes and fatty alcohols in P. nitida, whereas, in G. scripta screened fatty acids, alcohols, hydrocarbons, carbonyl compounds, polyols, terpenes, glycosides, phenols, and sugar alcohols detected in the chromatogram peak. FTIR analysis revealed functional groups like Alcohols, Amines, Amides, Alkanes, Aldehydes, Carboxylic acid, Alkynes, Esters, Ketones, Anhydrides, Acid chlorides, Alkenes, Aromatic compounds, Nitro compounds, Alkyl and Aryl Halides in both lichens.ConclusionsThe results obtained in the present study proved that P. nitida and G. scripta have promising antioxidant activity owing to the presence of polyphenols and terpenes, as evidenced by DPPH and FRAP assay along with enzymatic analysis (SOD and CAT). Thus both the lichens may be used as natural sources of new bioactive molecules having pharmaceutical interest.

Furan based synthetic chalcone derivative functions against gut inflammation and oxidative stress demonstrated in in-vivo zebrafish model

Inflammatory Bowel Disease (IBD) is a group of persistent intestinal illnesses resulting from bowel inflammation unrelated to infection. The prevalence of IBD is rising in industrialized countries, increasing healthcare costs. Whether naturally occurring or synthetic, chalcones possess a broad range of biological properties, including anti-inflammatory, anti-microbial, and antioxidant effects. This investigation focuses on DKO7 (E)-3-(4-(dimethylamino)phenyl)-1-(5-methylfuran-2-yl)prop-2-en-1-one, a synthesized chalcone with potential anti-inflammatory effects in a zebrafish model of intestinal inflammation induced by Dextran sodium sulfate (DSS). The in vitro study displayed dose-dependent anti-inflammatory as well as antioxidant properties of DKO7. Additionally, DKO7 protected zebrafish larvae against lipid peroxidation, reactive oxygen stress (ROS), and DSS-induced inflammation. Moreover, DKO7 reduced the expression of pro-inflammatory genes, including TNF-α, IL-1β, IL-6, and iNOS. Further, it reduced the levels of nitric oxide (NO) and lactate dehydrogenase (LDH) in the intestinal tissues of adult zebrafish and increased the levels of antioxidant enzymes such as Catalase (CAT) and superoxide dismutase (SOD). The protective effect of DKO7 against chemically (or DSS) induced intestinal inflammation was further verified using histopathological techniques in intestinal tissues. The furan-based chalcone derivative, DKO7, displayed antioxidant and anti-inflammatory properties. Also, DKO7 successfully reverses the DSS-induced intestinal damage in zebrafish. Overall, this study indicates the ability of DKO7 to alleviate DSS-induced gut inflammation in an in-vivo zebrafish.

Difluoroalkylation/Lactonization of Alkenes with BrCF2CO2K via Photoredox Catalysis: Access to α,α‐Difluoro‐γ‐lactones†

Comprehensive SummaryDue to its unique electronic properties, the difluoromethylene group (CF2) has served as a valuable unity in the design of biologically active molecules. Since γ‐lactones display a broad range of biological properties, α,α‐difluoro‐γ‐lactones may exhibit unexpected biological activities, and thus their synthesis has received increasing attention. Traditional synthetic methods suffer from tedious multi‐ step processes, and very few effective methods have been reported recently. Herein, we describe the difunctionalization of alkenes with BrCF2CO2K under photoredox catalysis with the use of a boron‐Lewis acid for the access to α,α‐difluoro‐γ‐lactones. In this transformation, the alkene substrates and the used reagents, including BrCF2CO2K and the boron‐Lewis acid, PhB(OH)2 or BF3·THF, are cheap and widely available. High efficiency and atom economy may make this protocol attractive.

The Outstanding Chemodiversity of Marine-Derived Talaromyces.

Fungi in the genus Talaromyces occur in every environment in both terrestrial and marine contexts, where they have been quite frequently found in association with plants and animals. The relationships of symbiotic fungi with their hosts are often mediated by bioactive secondary metabolites, and Talaromyces species represent a prolific source of these compounds. This review highlights the biosynthetic potential of marine-derived Talaromyces strains, using accounts from the literature published since 2016. Over 500 secondary metabolites were extracted from axenic cultures of these isolates and about 45% of them were identified as new products, representing a various assortment of chemical classes such as alkaloids, meroterpenoids, isocoumarins, anthraquinones, xanthones, phenalenones, benzofurans, azaphilones, and other polyketides. This impressive chemodiversity and the broad range of biological properties that have been disclosed in preliminary assays qualify these fungi as a valuable source of products to be exploited for manifold biotechnological applications.

Indole Alkaloids from Psychoactive Mushrooms: Chemical and Pharmacological Potential as Psychotherapeutic Agents.

Neuropsychiatric diseases such as depression, anxiety, and post-traumatic stress represent a substantial long-term challenge for the global health systems because of their rising prevalence, uncertain neuropathology, and lack of effective pharmacological treatments. The approved existing studies constitute a piece of strong evidence whereby psychiatric drugs have shown to have unpleasant side effects and reduction of sustained tolerability, impacting patients' quality of life. Thus, the implementation of innovative strategies and alternative sources of bioactive molecules for the search for neuropsychiatric agents are required to guarantee the success of more effective drug candidates. Psychotherapeutic use of indole alkaloids derived from magic mushrooms has shown great interest and potential as an alternative to the synthetic drugs currently used on the market. The focus on indole alkaloids is linked to their rich history, their use as pharmaceuticals, and their broad range of biological properties, collectively underscoring the indole heterocycle as significant in drug discovery. In this review, we aim to report the physicochemical and pharmacological characteristics of indole alkaloids, particularly those derived from magic mushrooms, highlighting the promising application of such active ingredients as safe and effective therapeutic agents for the treatment of neuropsychiatric disorders.

The synthesis and development of poly(ε-caprolactone) conjugated polyoxyethylene sorbitan oleate-based micelles for curcumin drug release: an in vitro study on breast cancer cells.

it is now known that curcumin (Cur) has a broad range of biological properties; however, photosensitivity, as well as low bioavailability and short half-life, have limited its clinical application. To overcome these problems the synthesis of poly(ε-caprolactone)-Tween 80 (PCL-T) copolymers was performed. the copolymers of PCL-T were created using the solvent evaporation/extraction technique. Then Cur was loaded in PCL-T micelles (PCL-T-M) by a self-assembly method. The characterization of copolymer and micelles was assessed by gel permeation chromatography (GPC), Fourier transform infrared spectroscopy (FT-IR), proton nuclear magnetic resonance spectroscopy (1HNMR), differential scanning calorimetry (DSC), transmission electron microscopy (TEM), and dynamic light scattering (DLS) methods. The MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay was used to indicate the cytotoxicity of the free Cur, PCL-T-M, and Cur-loaded PCL-T-M. TEM analysis showed monodispersed and spherical shapes with a size of about 90 nm. Cur was released from PCL-T-M at pH 7.4 (45%) and 5.5 (90%) during 6 days. After 24 and 48 h, the IC50 of the free Cur, PCL-T-M, and Cur-loaded PCL-T-M on MCF-7 cells were 80.86 and 54.45 μg mL-1, 278.30 and 236.19 μg mL-1, 45.47 and 19.05 μg mL-1, respectively. this study showed that, in the same concentration, the effectiveness of the Cur-loaded PCL-T-M is more than the free Cur, and the nano-system has been able to overcome delivery obstacles of Cur drug. Thus, PCL-T-M can be a candidate as a drug carrier for the delivery of Cur and future therapeutic investigations on breast cancer.

Antileukemia Activity and Mechanism of Platinum(II)-Based Metal Complexes.

Transition metal complexes have continued to constitute an appealing class of medicinal compounds since the exceptional discovery of cisplatin in the late 1960s. Pt(II)-based complexes are endowed with a broad range of biological properties, which are mainly exerted by targeting DNA. In this study, we report a significant biological investigation into and computation analyses of four Pt(II)-complexes, namely, LDP-1-4, synthesized and characterized according to previously reported procedures. Molecular-modelling studies highlighted that the top two LDP compounds (i.e., LDP-1 and LDP-4) might bind to both matched and mismatched base pair sites of the oligonucleotide 5'-(dCGGAAATTACCG)2-3', supporting their anticancer potential. These two complexes displayed noteworthy cytotoxicity in vitro (sub-micromolar-micromolar range) against two leukaemia cell lines, i.e., CCRF-CEM and its multi-drug-resistant counterpart CEM/ADR5000, and remarkable anti-angiogenic properties (in the sub-micromolar range) evaluated in an in vivo model, i.e., a chick embryo chorioallantoic membrane (CAM) assay.

Synthesis of Novel (bis‐)1,5‐Disubstituted‐1H‐tetrazole‐Decorated Monomers and Their Respective Polymers via Thiol‐ene Polymerization

AbstractOver the years, nitrogen‐rich functional groups like tetrazole and its derivatives have received increasing interest in the chemistry of small molecules. There is a continuously growing interest in polymers decorated with nitrogen for potential biomedical applications because of their broad range of biological properties, such as being antibacterial, anticarcinogenic, and anti‐inflammatory. On this premise, a new synthesis route is reported for nitrogen‐decorated polymers via the combination of Ugi‐azide four‐multicomponent reaction (UA‐4MCR) and thiol‐ene polymerization. Accordingly, α,ω‐diene monomers decorated with (bis‐)1,5‐disubstituted‐1H‐tetrazoles (bis‐1,5‐DS‐Ts) are synthesized by using the UA‐4MCR. Subsequently, the light‐induced thiol‐ene polymerization facilitates the efficient synthesis of novel tetrazole‐decorated polymers with apparent number average molecular mass (Mn) up to 62 000 g mol−1, which are characterized for their chemical, thermal, and optical properties. The comprehensive characterization of the synthesized polymers is paving the way toward a wealth of opportunities, ranging from biomaterials to energy storage−relevant materials.

Osthole: Synthesis, Structural Modifications, and Biological Properties.

Osthole, a naturally occurring coumarin-type compound, is isolated from the Chinese herbal medicine Cnidium monnieri (L.) and exhibits a broad range of biological properties. In this review, the total synthesis and structural modifications of osthole and its analogs are described. Additionally, the progress on bioactivities of osthole and its analogs has been outlined since 2016. Moreover, the structure-activity relationships and mechanisms of action of osthole and its derivatives are discussed. These can provide references for future design, development, and application of osthole and its analogs as drugs or pesticides in the fields of medicine and agriculture.

Nitrobenzamido substitution on thiophene-3-carboxylate: Electrochemical investigation, antioxidant activity, molecular docking, DFT calculations

A novel nitro containing thiophene derivatives containing have been synthesized. In pharmaceutical chemistry, thiophene derivatives show a biological effect. Due to the promising antimicrobial, analgesic and anti-inflammatory, and antitumor activity, alternative and different approaches have also been one of the main objectives in the field of chemical sciences. Based on the broad range of biological properties of thiophene derivatives, this study aimed to evaluate the antioxidant activity of novel thiophene derivatives and explore the electrochemical features using CV (cyclic voltammetry). The synthesis and characterization of novel benzo[b]thiophone derivatives were confirmed using spectroscopic methods with 1H-NMR, 13C-NMR, FT-IR, and UV-vis. The DFT and TD-DFT computations were conducted to compare the spectroscopic data and then confirm the molecular structures of the compounds 1-3. The FMO and NBO analyses were conducted to estimate the possible reactivity features and key intra-molecular interactions. Last, molecular docking investigations were performed to explore the possible interaction of each compound to human EGFR Kinase.

Phytochemistry, Pharmacological Properties, and Recent Applications of Ficus benghalensis and Ficus religiosa.

Ficus is one of the largest genera in the plant kingdom that belongs to the Moraceae family. This review aimed to summarize the medicinal uses, phytochemistry, and pharmacological actions of two major species from this genus, namely Ficus benghalensis and Ficus religiosa. These species can be found abundantly in most Asian countries, including Malaysia. The chemical analysis report has shown that Ficus species contained a wide range of phytoconstituents, including phenols, flavonoids, alkaloids, tannins, saponins, terpenoids, glycosides, sugar, protein, essential and volatile oils, and steroids. Existing studies on the pharmacological functions have revealed that the observed Ficus species possessed a broad range of biological properties, including antioxidants, antidiabetic, anti-inflammatory, anticancer, antitumor and antiproliferative, antimutagenic, antimicrobial, anti-helminthic, hepatoprotective, wound healing, anticoagulant, immunomodulatory activities, antistress, toxicity studies, and mosquitocidal effects. Apart from the plant parts and their extracts, the endophytes residing in these host plants were discussed as well. This study also includes the recent applications of the Ficus species and their plant parts, mainly in the nanotechnology field. Various search engines and databases were used to obtain the scientific findings, including Google Scholar, ScienceDirect, PMC, Research Gate, and Scopus. Overall, the review discusses the therapeutic potentials discovered in recent times and highlights the research gaps for prospective research work.

Nanoceria Can Inhibit the Reproduction of Transmissible Gastroenteritis Virus: Consideration for Use to Prevent and Treat Coronavirus Disease

Nanoceria (cerium dioxide nanoparticles, CeO2) has a broad range of biological properties including antiviral activity. The hypothesis was that nanoceria can efficacy against coronavirus (coronavirus of porcine transmissible gastroenteritis) and potentially can target SARS-CoV-2. Transmissible gastroenteritis coronavirus (TGEV) is the etiologic agent of porcine transmissible gastroenteritis (PTG), a highly contagious pig intestinal disease. The aim of the study was to determine the antiviral activity of CeO2 nanoparticles on the model of porcine coronavirus – TGEV. Methods. We used a highly pathogenic virus strain D52-5 (BRE79), of TGEV. We evaluated antiviral activity of CeO2 nanoparticles on the experimental model of porcine coronavirus (transmissible gastroenteritis virus) in transplantable line of porcine embryonic kidney cells (PEK) culture. Results. The criterion for evaluating the inhibitory activity of antiviral drugs in different in vitro systems is the selectivity index (SI) and the reduction of infectious titer by 1.5–2.0 lgTCD50. Nanoceria effectively inhibited the reproduction of porcine coronavirus with SI index of 83.3.

A novel indazole derivative, compound Cyy-272, attenuates LPS-induced acute lung injury by inhibiting JNK phosphorylation

Acute lung injury (ALI) is a diffuse lung dysfunction disease characterized by high prevalence and high mortality. Thus far, no effective pharmacological treatment has been made for ALI in clinics. Inflammation is critical to the development of ALI. Therefore, anti-inflammation may be a potential therapy strategy for ALI. Indazole-containing derivatives, representing one of the most important heterocycles in drug molecules, are endowed with a broad range of biological properties, such as anti-cancer and anti-inflammation. In the current study, we investigated the biological effects of Cyy-272, a newly synthesized indazole compound, on LPS-induced ALI both in vivo and in vitro. Results show that Cyy-272 can inhibit the release of inflammatory cytokines in LPS-stimulated macrophage and alleviate LPS induced ALI. Further experiment revealed that Cyy-272 exhibit anti-inflammation activity by inhibiting JNK phosphorylation. Overall, our studies show that an indazole derivative, Cyy-272, is effective in suppressing LPS-induced JNK activation and inflammatory signaling.

Indazole scaffold: a generalist for marketed and clinical drugs

More and more attention has been paid to the structurally diverse indazole analogs in recent years which are widely present in numerous commercially available drugs. Indazole-containing derivatives are endowed with a broad range of biological properties, such as anti-inflammatory, antibacterial, anti-HIV, antiarrhythmics, antifungal and antitumor activities. This review is a guide for pharmacologists who are in search of valid preclinical/clinical drug compounds where the progress, from 1966 to the present day, of approved marketed drugs containing indazole scaffold is examined.

Nanoencapsulation of Plant Volatile Organic Compounds to Improve Their Biological Activities.

Plant volatile organic compounds (volatiles) are secondary plant metabolites that play crucial roles in the reproduction, defence, and interactions with other vegetation. They have been shown to exhibit a broad range of biological properties and have been investigated for antimicrobial and anticancer activities. In addition, they are thought be more environmentally friendly than many other synthetic chemicals 1. Despite these facts, their applications in the medical, food, and agricultural fields are considerably restricted due to their volatilities, instabilities, and aqueous insolubilities. Nanoparticle encapsulation of plant volatile organic compounds is regarded as one of the best strategies that could lead to the enhancement of the bioavailability and biological activity of the volatile compounds by overcoming their physical limitations and promoting their controlled release and cellular absorption. In this review, we will discuss the biosynthesis and analysis of plant volatile organic compounds, their biological activities, and limitations. Furthermore, different types of nanoparticle platforms used to encapsulate the volatiles and the biological efficacies of nanoencapsulated volatile organic compounds will be covered.

Indazole as a Privileged Scaffold: The Derivatives and their Therapeutic Applications.

Heterocyclic compounds, also called heterocycles, are a major class of organic chemical compound that plays a vital role in the metabolism of all living cells. The heterocyclic compound, indazole, has attracted more attention in recent years and is widely present in numerous commercially available drugs. Indazole-containing derivatives, representing one of the most important heterocycles in drug molecules, are endowed with a broad range of biological properties. A literature search was conducted in PubMed, Google Scholar and Web of Science regarding articles related to indazole and its therapeutic application. The mechanism and structure-activity relationship of indazole and its derivatives were described. Based on their versatile biological activities, the compounds were divided into six groups: anti-inflammatory, antibacterial, anti-HIV, antiarrhythmic, antifungal and antitumour. At least 43 indazole-based therapeutic agents were found to be used in clinical application or clinical trials. This review is a guide for pharmacologists who are in search of valid preclinical/clinical drug compounds where the progress of approved marketed drugs containing indazole scaffold is examined from 1966 to the present day. Future direction involves more diverse bioactive moieties with indazole scaffold and greater insights into its mechanism.

Advances in Research on the Preparation and Biological Activity of Maslinic Acid.

Maslinic acid, a pentacyclic triterpene acid, is mainly isolated from olives. Maslinic acid and its derivatives exhibit a broad range of biological properties, such as anti-inflammatory, anticancer, anti-diabetic, antimicrobial, neuroprotective and hepatoprotective activities. In this minireview, the progress of research on maslinic acid with regard to its bioactivities, extraction, semisynthetic preparation and patents is reported. The relationships between the structure and the activity of maslinic acid and its derivatives are also discussed.

Advances on the Bioactivities, Total Synthesis, Structural Modification, and Structure-Activity Relationships of Cytisine Derivatives.

Cytisine is a quinolizidine alkaloid isolated from various Leguminosae plants. Cytisine and its derivatives exhibit a broad range of biological properties, such as smoking cessation aid, antidepressant, neuroprotective, nootropic, anticancer, antiviral, antiparasitic, antidiabetic, insecticidal, and nematicidal activities. In this review, the progress of cytisine and its derivatives in regard to bioactivities, total synthesis, structural modifications focusing on their N-12 position and lactam ring is reported. Additionally, the structure-activity relationships of cytisine and its derivatives are also discussed.

Dihydroartemisinin inhibits the growth and invasion of gastric cancer cells by regulating cyclin D1-CDK4-Rb signaling

BackgroundDihydroartemisinin (DHA), a semisynthetic derivative of artemisinin, has a broad range of biological properties, including antitumor activity. However, the mechanisms by which DHA affects the tumorigenesis of gastric carcinoma (GC) are poorly understood. Material and methodsThe targets of DHA were identified by network pharmacology, and the association of CDK4 with clinicopathological characteristics and prognosis in patients with GC was analyzed by using TCGA data. CCK8, Transwell and flow cytometric analyses, as well as a tumor xenograft model, were used to assess the effects of DHA on the growth and migration of GC cells. qRT-PCR and Western blot analyses were used to determine the effects of DHA on the cyclin D1-CDK4-Rb signaling pathway. ResultsWe identified 13 DHA targets and measured their expression of whichCDK4 expression levels were substantially higher in GC tissues than those in adjacent normal tissues, and high CDK4 expression acted as an independent prognostic factor of poor survival in patients with GC. DHA suppressed cell proliferation, migration and invasion in vitro and in vivo and induced G1 phase cell cycle arrest in a dose-dependent manner by regulating cyclin D1-CDK4-Rb signaling. ConclusionsDHA inhibits the tumorigenesis and invasion of GC by regulating cyclin D1-CDK4-Rb signaling and may provide therapeutic strategies for the treatment of GC.