Pharmacological Properties Research Articles

Finerenone in patients with heart failure with mildly reduced or preserved ejection fraction: Rationale and design of the FINEARTS-HF trial.

Steroidal mineralocorticoid receptor antagonists (MRAs), spironolactone and eplerenone, are strongly recommended in the treatment of patients with chronic heart failure (HF) with reduced left ventricular ejection fraction (LVEF), but the balance of efficacy and safety in those with higher LVEF has not been well established. Broad use of steroidal MRAs has further been limited in part due to safety concerns around risks of hyperkalaemia, gynecomastia, and kidney dysfunction. These risks may be mitigated by the unique pharmacological properties of the non-steroidal MRA finerenone. The FINEARTS-HF trial is designed to evaluate the long-term efficacy and safety of the selective non-steroidal MRA finerenone among patients with HF with mildly reduced or preserved ejection fraction. FINEARTS-HF is a global, multicentre, event-driven randomized trial evaluating oral finerenone versus matching placebo in symptomatic patients with HF with LVEF ≥40%. Adults (≥40 years) with HF with New York Heart Association class II-IV symptoms, LVEF ≥40%, evidence of structural heart disease, and diuretic use for at least the previous 30 days were eligible. All patients required elevated natriuretic peptide levels: for patients in sinus rhythm, N-terminal pro-B-type natriuretic peptide (NT-proBNP) ≥300 pg/ml (or B-type natriuretic peptide [BNP] ≥100 pg/ml) were required, measured within 30 days (in those without a recent worsening HF event) or within 90 days (in those with a recent worsening HF event). Qualifying levels of NT-proBNP or BNP were tripled if a patient was in atrial fibrillation at screening. Estimated glomerular filtration rate <25 ml/min/1.73 m2 or serum potassium >5.0 mmol/L were key exclusion criteria. Patients were enrolled irrespective of clinical care setting (whether hospitalized, recently hospitalized, or ambulatory). The primary endpoint is the composite of cardiovascular death and total (first and recurrent) HF events. The trial started on 14 September 2020 and has validly randomized 6001 participants across 37 countries. Approximately 2375 total primary composite events are targeted. The FINEARTS-HF trial will determine the efficacy and safety of the non-steroidal MRA finerenone in a broad population of hospitalized and ambulatory patients with HF with mildly reduced or preserved ejection fraction. ClinicalTrials.gov NCT04435626 and EudraCT 2020-000306-29.

Inhibition of the morphological transition of Candida spp. by riparins I-IV.

Candida spp. is an opportunistic pathogen capable of causing superficial to invasive infections. Morphological transition is one of the main virulence factors of this genus and, therefore, is an important variable to be considered in pharmacological interventions. Riparins I, II, III, and IV are alkamide-type alkaloids extracted from the unripe fruit of Aniba riparia, whose remarkable pharmacological properties were previously demonstrated. This work aimed to evaluate in silico and in vitro the inhibitory effects of Riparins on the morphological transition of Candida albicans, Candida tropicalis, and Candida krusei. Molecular docking was applied to analyze the inhibitory effects of riparins against proteins such as N-acetylglucosamine, CYP-51, and protein kinase A (PKA) using the Ramachandran plot. The ligands were prepared by MarvinSketch and Spartan software version 14.0, and MolDock Score and Rerank Score were used to analyze the affinity of the compounds. In vitro analyses were performed by culturing the strains in humid chambers in the presence of riparins or fluconazole (FCZ). The morphology was observed through optical microscopy, and the size of the hyphae was determined using the ToupView software. In silico analysis demonstrated that all riparins are likely to interact with the molecular targets: GlcNAc (>50%), PKA (>60%), and CYP-51 (>70%). Accordingly, in vitro analysis showed that these compounds significantly inhibited the morphological transition of all Candida strains. In conclusion, this study demonstrated that riparins inhibit Candida morphological transition and, therefore, can be used to overcome the pathogenicity of this genus.

Chamaecyparis lawsoniana and Its Active Compound Quercetin as Ca2+ Inhibitors in the Contraction of Airway Smooth Muscle

The Cupressaceae family includes species considered to be medicinal. Their essential oil is used for headaches, colds, cough, and bronchitis. Cedar trees like Chamaecyparis lawsoniana (C. lawsoniana) are commonly found in urban areas. We investigated whether C. lawsoniana exerts some of its effects by modifying airway smooth muscle (ASM) contractility. The leaves of C. lawsoniana (363 g) were pulverized mechanically, and extracts were obtained by successive maceration 1:10 (w:w) with methanol/CHCl3. Guinea pig tracheal rings were contracted with KCl, tetraethylammonium (TEA), histamine (HIS), or carbachol (Cch) in organ baths. In the Cch experiments, tissues were pre-incubated with D-600, an antagonist of L-type voltage-dependent Ca2+ channels (L-VDCC) before the addition of C. lawsoniana. Interestingly, at different concentrations, C. lawsoniana diminished the tracheal contractions induced by KCl, TEA, HIS, and Cch. In ASM cells, C. lawsoniana significantly diminished L-type Ca2+ currents. ASM cells stimulated with Cch produced a transient Ca2+ peak followed by a sustained plateau maintained by L-VDCC and store-operated Ca2+ channels (SOCC). C. lawsoniana almost abolished this last response. These results show that C. lawsoniana, and its active metabolite quercetin, relax the ASM by inhibiting the L-VDCC and SOCC; further studies must be performed to obtain the complete set of metabolites of the extract and study at length their pharmacological properties.

Recent Advances in Manganese(III)-Assisted Radical Cyclization for the Synthesis of Natural Products: A Comprehensive Review

Natural products play an important part in synthetic chemistry since they have many pharmacological properties and are used as active drug compounds in pharmaceutical chemistry. However, synthesis of these complex molecules is difficult due to the requirement of various synthetic steps, which include highly regio- and stereoselectivity. Therefore, oxidative radical cyclization assisted by manganese(III) acetate serves as an important step in obtaining spiro-, tricyclic, tetracyclic, and polycyclic derivatives of these compounds. Manganese(III)-based reactions offer a single-step regio- and stereoselective cyclizations and α-acetoxidations, reducing the number of synthetic steps. Also, the manganese(III)-mediated oxidative free radical cyclization method has been successfully applied for the synthesis of cyclic structures found in many natural products. This article presents a broad overview of manganese(III)-based radical reactions of natural products as a key step in overall synthesis. The authors have classified natural product synthesis processes assisted by manganese(III) acetate as intermolecular, intramolecular, oxidation, acetoxidation, aromatization, and polymerization reactions, respectively.

The Effects of Fingolimod (FTY720) on Leukocyte Subset Circulation cannot be Behaviourally Conditioned in Rats

Suppression of immune functions can be elicited by behavioural conditioning using drugs such as cyclosporin A or rapamycin. Nevertheless, little is known about the underlying mechanisms and generalisability of this phenomenon. Against this background, the present study investigated whether the pharmacological properties of fingolimod (FTY720), an immunosuppressive drug widely applied to treat multiple sclerosis, can be conditioned in rats by means of taste-immune associative learning. For this purpose, a conditioned taste avoidance paradigm was used, pairing the presentation of a novel sweet drinking solution (saccharin or sucrose) as conditioned stimulus (CS) with therapeutically effective doses of FTY720 as unconditioned stimulus (US). Subsequent re-exposure to the CS at a later time point revealed that conditioning with FTY720 induced a mild conditioned taste avoidance only when saccharin was employed as CS. However, on an immunological level, neither re-exposure with saccharin nor sucrose altered blood immune cell subsets or splenic cytokine production. Despite the fact that intraperitonally administered FTY720 could be detected in brain regions known to mediate neuro-immune interactions, the present findings show that the physiological action of FTY720 is not inducible by mere taste-immune associative learning. Whether conditioning generalises across all small-molecule drugs with immunosuppressive properties still needs to be investigated with modified paradigms probably using distinct sensory CS. Moreover, these findings emphasize the need to further investigate the underlying mechanisms of conditioned immunomodulation to assess the generalisability and usability of associative learning protocols as supportive therapies in clinical contexts.Graphical To assess the potential of taste-immune associative learning mediated by specific brain regions (e.g., insular cortex, amygdala), the presentation of a novel taste (saccharin or sucrose) as conditioned stimulus was paired with injections of fingolimod (FTY720) as unconditioned stimulus. However, re-exposure to the conditioned stimulus did not elicit behaviourally conditioned immunosuppressive effects. Created with BioRender.com.

Central Neuromodulators in Irritable Bowel Syndrome: Why, How, and When.

Irritable bowel syndrome (IBS) is responsive to treatments using central neuromodulators. Central neuromodulators work by enhancing the synaptic transmission of 5-hydroxytryptamine, noradrenalin, and dopamine, achieving a slower regulation or desensitization of their postsynaptic receptors. Central neuromodulators act on receptors along the brain-gut axis, so they are useful in treating psychiatric comorbidities, modifying gut motility, improving central downregulation of visceral signals, and enhancing neurogenesis in patients with IBS. Choosing a central neuromodulator for treating IBS should be according to the pharmacological properties and predominant symptoms. The first-line treatment for pain management in IBS is using tricyclic antidepressants. An alternative for pain management is the serotonin and noradrenaline reuptake inhibitors. Selective serotonin reuptake inhibitors are useful when symptoms of anxiety and hypervigilance are dominant but are not helpful for treating abdominal pain. The predominant bowel habit is helpful when choosing a neuromodulator to treat IBS; selective serotonin reuptake inhibitors help constipation, not pain, but may cause diarrhea; tricyclic antidepressants help diarrhea but may cause constipation. A clinical response may occur in 6-8 weeks, but long-term treatment (usually 6-12 months) is required after the initial response to prevent relapse. Augmentation therapy may be beneficial when the therapeutic effect of the first agent is incomplete or associated with side effects. It is recommended to reduce the dose of the first agent and add a second complementary treatment. This may include an atypical antipsychotic or brain-gut behavioral treatment. When tapering central neuromodulators, the dose should be reduced slowly over 4 weeks but may take longer when discontinuation effects occur.

Genetic diversity, clinical uses, and phytochemical and pharmacological properties of safflower (Carthamus tinctorius L.): an important medicinal plant

Safflower (Carthamus tinctorius L.), a member of the Asteraceae family, is widely used in traditional herbal medicine. This review summarized agronomic conditions, genetic diversity, clinical application, and phytochemicals and pharmacological properties of safflower. The genetic diversity of the plant is rich. Abundant in secondary metabolites like flavonoids, phenols, alkaloids, polysaccharides, fatty acids, polyacetylene, and other bioactive components, the medicinal plant is effective for treating cardiovascular diseases, neurodegenerative diseases, and respiratory diseases. Especially, Hydroxysafflor yellow A (HYSA) has a variety of pharmacological effects. In terms of treatment and prevention of some space sickness in space travel, safflower could be a potential therapeutic agent. Further studies are still required to support the development of safflower in medicine. Our review indicates that safflower is an important medicinal plant and research prospects regarding safflower are very broad and worthy of further investigation.

Chemistry, Biological Activities, and Pharmacological Properties of Gastrodin: Mechanism Insights.

Gastrodin, a bioactive compound derived from the rhizome of the orchid Gastrodia elata, exhibits a diverse range of biological activities. With documented neuroprotective, anti-inflammatory, antioxidant, anti-apoptotic, and anti-tumor effects, gastrodin stands out as a multifaceted therapeutic agent. Notably, it has demonstrated efficacy in protecting against neuronal damage and enhancing cognitive function in animal models of Alzheimer's disease, Parkinson's disease, and cerebral ischemia. Additionally, gastrodin showcases immunomodulatory effects by mitigating inflammation and suppressing the expression of inflammatory cytokines. Its cytotoxic activity involves the inhibition of angiogenesis, suppression of tumor growth, and induction of apoptosis. This comprehensive review seeks to elucidate the myriad potential effects of Gastrodin, delving into the intricate molecular mechanisms underpinning its pharmacological properties. The findings underscore the therapeutic potential of gastrodin in addressing various conditions linked to neuroinflammation and cancer.

Studies on Various Taxonomic, Pharmacognostic and Phytochemical Properties of Sanchezia speciosa Leonard Acanthaceae

Sanchezia speciosa Leonard, Acanthaceae is used as ornamental plant. It used in folklore medicine in the management of pain, anti-microbial and insecticide. An investigation was carried out to evaluate the various taxonomic, pharmacognostic and phytochemical standards to ensure the identity, purity, safety and efficacy of the medicinal plant, S. speciosa. Various observations were recorded which included microscopy, micromeritics, fluorescence, chemomicroscopy, soluble extractive values, moisture contents and phytochemical analysis. The results indicated that the epidermal shapes were both polygonal on the adaxial and abaxial surfaces. Stomatal distribution was amphistomatic with anisocytic and diacytic stomata on the adaxial and abaxial surface, respectively. Stomatal index was 21.47% on the adaxial surface and 15.43% on the abaxial surface. Micromeritics results for the leaf powder were bulk volume of 25.33± 0.408, tapped volume of 19.00± 0.00, bulk density of 0.40± 0.006, tapped density of 0.53± 0.021, Hausner’s ratio of 1.34± 0.037, Carr’s index of 25.00± 2.550 and angle of repose of 43.07°. The micromeritics indicated a passable flow. The chemo microscopy indicated presence of lignin, mucilage and starch. Fluorescence properties showed different colours under different ultraviolet lights. The water-soluble, methanol-soluble, ethanol-soluble extractive values were 14.7% w/w, 4.3% w/w and 5.0% w/w, respectively. Moisture content was 8.5% w/w. Total ash, acid-insoluble and water-soluble ash values were 20.0 % w/w, 2.0% w/w and 4.2% w/w, respectively. GC-MS of methanol extract revealed the total of 39 phytochemicals with over 5 prominent peaks having higher area% which include hexadecanoic acid methyl ester (2.64%), 9,12,15-octadecatrienoic acid methyl ester (4.77%), phytol (9.98%), 9,12,15 octadecatrienoic acid (12.97%), Stigmasterol (2.00%) and Squalene (28.16%). Other compounds are glycerin (5.83%), n-hexadecanoic acid (2.85%) and 9 octadecenamide (2.18%). Many of them possess good pharmacological properties. The data generated from the present study would help to authenticate S. speciosa and also affirm its folklore use in traditional medicine which has potential for further development into drug product.

Phytochemical and pharmacological properties of Xanthium species: a review

Phytochemical and pharmacological properties of Xanthium species: a review

A systematic literature review on the pharmacological applications of the carotenoid norbixin

Carotenoids play essential roles in human health and can fight and prevent diseases. One carotenoid that is currently attracting scientific interest, particularly for its antioxidant properties, is norbixin. Studies related to its use in the treatment of diseases have become increasingly present in the medical field. This systematic literature review aimed to investigate and gather studies on the pharmacological activity of norbixin for health benefits and the treatment of diseases. Four databases were consulted: Web of Science, PubMed, Scopus, and ScienceDirect. Articles were extracted using a combination of keywords such as 'norbixin', 'antioxidant', 'diseases', 'in vitro', 'in vivo', etc. A total of 173 articles were identified. After applying the inclusion and exclusion criteria, 21 were selected for inclusion in this review. Studies have shown that norbixin, alone or in combination with other treatments, may be effective in DNA protection, tissue engineering, bone repair, and the prevention and treatment of age-related macular degeneration and cardiovascular disease. These results provide a solid basis for further studies aimed at exploring the pharmacological properties of norbixin and enabling its use in therapeutic applications.

Xanthone Derivatives and Their Potential Usage in the Treatment of Telangiectasia and Rosacea

Xanthone derivatives, a class of natural compounds abundantly found in plants such as mangosteen (Garcinia mangostana) and certain herbs, have garnered substantial interest due to their diverse pharmacological properties, including antioxidant, anti-inflammatory, and anti-cancer activities. Recent investigations have unveiled their potential as modulators of enzymatic activity, prompting exploration into their effects on hyaluronidase-mediated hyaluronic acid (HA) degradation, and their effects in topical treatment of telangiectasia and rosacea. Telangiectasia and rosacea are common dermatological conditions characterized by chronic skin inflammation, vascular abnormalities, and visible blood vessels, resulting in significant cosmetic concerns and impaired quality of life for affected individuals. This review aims to provide a comprehensive overview of the current understanding regarding the interplay between the mechanisms of action by which xanthone derivatives exert their therapeutic effects, including the inhibition of pro-inflammatory cytokines, modulation of oxidative stress pathways, and regulation of vascular endothelial growth factors. Furthermore, we will discuss the implications of harnessing xanthone derivatives as therapeutic agents for mitigating vascular dysfunction and its associated pathologies, thereby offering insights into future research directions and therapeutic strategies in the field of vascular biology.

In vitro study on anti-proliferative and anti-cancer activity of picrosides in triple-negative breast cancer.

Picrorhiza kurroa, an "Indian gentian," a known Himalayan medicinal herb with rich source of phytochemicals like picrosides I, II, and other glycosides, has been traditionally used for the treatment of liver and respiratory ailments. Picrosides anti-proliferative, anti-oxidant, anti-inflammatory and other pharmacological properties were evaluated in treating triple-negative breast cancer (TNBC). Picroside I and II were procured from Sigma-Aldrich and were analyzed for anti-cancer activity in triple-negative breast cancer (MDA-MB-231) cells. Cell viability was analyzed using MTT and trypan blue assays. Apoptosis was analyzed through DNA fragmentation and Annexin V/PI flow cytometric analysis. Wound healing and cell survival assays were employed to determine the inhibition of invasion capacity and anti-proliferative activity of picrosides in MDA-MB-231 cells. Measurement of intracellular ROS was studied through mitochondrial membrane potential assessment using DiOC6 staining for anti-oxidant activity of picrosides in MDA-MB-231 cells. Both Picroside I and II have shown decreased cell viability of MDA-MB-231 cells with increasing concentrations. IC50 values of 95.3µM and 130.8µM have been obtained for Picroside I and II in MDA-MB-231 cells. Early apoptotic phase have shown an increase of 20% (p < 0.05) with increasing concentrations (0, 50, 75, and 100µM) of Picroside I and 15% (p < 0.05) increase with Picroside II. Decrease in mitochondrial membrane potential of 2-2.5-fold (p < 0.05) was observed which indicated decreased reactive oxygen species (ROS) generation with increasing concentrations of Picroside I and II. An increasing percentage of 70-80% (p < 0.05) cell population was arrested in G0/G1 phase of cell cycle after Picroside I and II treatment in cancer cells. Our results suggest that Picroside I and II possess significant anti-proliferative and anti-cancer activity which is mediated by inhibition of cell growth, decreased mitochondrial membrane potential, DNA damage, apoptosis, and cell cycle arrest. Therefore, Picroside I and II can be developed as a potential anti-cancer drug of future and further mechanistic studies are underway to identify the mechanism of anti-cancer potential.

Exploring the potential of fennel (&lt;i&gt;Foeniculum vulgare&lt;/i&gt; Mill.) as a valuable medicinal plant: a comprehensive (review)

Introduction. Foeniculum vulgare Mill., commonly known as fennel or drugstore dill, is very common as one of the world's oldest spice plants, which has significant economic importance and wide application in the pharmaceutical industry. In medical practice, the fruits of this plant are mainly used, which are included in the State Pharmacopoeia of the XIV edition and are a source of essential oil. They are used as an antispasmodic and carminative agent in the form of an infusion. Fennel grass harvested before flowering is used for food, as well as fruits, stems and inflorescences of the plant as a seasoning.Text. The purpose of this study is to summarize scientific papers on the morphological characteristics, phytochemical compounds, therapeutic properties and basic mechanisms of pharmacological activity of F. vulgare. A systematic literature search was conducted using relevant keywords such as "fennel", "Foeniculum vulgare Mill.", "therapeutic" and "pharmacology" in well-known databases, including ScienceDirect, Scopus, EBSCO and Medline. The search covered articles published before April 25, 2023 in available journals. The results of the study showed that fennel has a wide range of pharmacological properties, including antioxidant, anti-cancer, anti-inflammatory, antifungal, antibacterial and estrogenic effects. These effects can be explained by the presence of aromatic compounds, in particular anethole, estragole and fenchone, which are abundantly present in fennel.Conclusion. The diverse pharmacological properties and rich chemical composition of fennel make it a promising raw material for the development of new medicines. Further study of the therapeutic potential of fennel through in vivo and in vitro studies will contribute to the establishment of mechanisms of pharmacological action of biologically active substances (BAS) of fennel.

Caffeine and Purine Derivatives: A Comprehensive Review on The Chemistry, Biosynthetic Pathways, Synthesis-Related Reactions, Biomedical Prospectives and Clinical Applications.

Caffeine and purine derivatives represent interesting chemical moieties, which show various biological activities. Caffeine is an alkaloid that belongs to the family of methylxanthine alkaloids and it is present in food, beverages, and drugs. Coffee, tea, and some other beverages are a major source of caffeine in the human diet. Caffeine can be extracted from tea or coffee using hot water with dichloromethane or chloroform and the leftover is known as decaffeinated coffee or tea. Caffeine and its derivatives were synthesized via different procedures on small and large scales. It competitively antagonizes the adenosine receptors (ARs), which are G protein-coupled receptors largely distributed in the human body, including the heart, vessels, brain, and kidneys. Recently, many reports showed the effect of caffeine derivatives in the treatment of many diseases such as Alzheimer's, asthma, parkinsonism, and cancer. Also, it is used as an antioxidant, anti-inflammatory, analgesic, and hypocholesterolemic agent. The present review article discusses the synthesis, reactivity, and biological and pharmacological properties of caffeine and its derivatives. The biosynthesis and biotransformation of caffeine in coffee and tea leaves and the human body were summarized in the review.

Characterization, In Silico Antimalarial, Antiinflammatory, Antioxidant, and ADMET Assessment of Neonauclea excelsa Merr.

In our study, we identified the phytoconstituents and carried out antimalarial, anti-inflammatory, antioxidant, and ADMET assessments of Neonauclea excelsa. The phytochemicals were detected and quantified followed by identification via GC-MS. The antimalaria, anti-inflammatory, and antioxidant assessments were done by molecular docking (MD) and molecular dynamics simulation (MDS) while ADMET by ADMET predictions. Saponins (27.33% ±1.20) and terpenes (8.33% ±0.73) were detected while alkaloids, steroids, glycosides, and flavonoids were absent. Exactly 29 compounds were identified with squalene being the most abundant (32.41%). Compound II exhibited the lowest BA (-6.4 kcal/mol) and Ki (20.12 µM), interacting with dihydrofolate reductase-thymidylate synthase. IV exhibited the lowest respective BA and Ki interacting with Plasmodium falciparum hexose transporter protein 1 (-6.2 kcal/mol and 28.20 µM), cyclo-oxygenase-2 (-7.2 kcal/mol and 5.21 µM), and myeloperoxidase (-7.4 kcal/mol and 3.71 µM). Compound VII had the lowest respective BA and Ki interacting with inducible nitric oxide synthase (-8.0 kcal/mol and 1.35 µM), xanthine oxidase (-7.2 kcal/mol and 5.21 µM), and cytochrome p450 21A2 (-7.0 kcal/mol and 7.30 µM). The MDS showed various cluster mobilities and residue fluctuations up to 5.26, 2.96, 5.10, 3.51, 5.02, 4.65, and 6.18 Å for dihydrofolate reductase-thymidylate synthase, Plasmodium falciparum hexose transporter protein 1, inducible nitric oxide synthase (INOS), cyclo-oxygenase-2 (COX2), xanthine oxidase (XO), cytochrome p450 21A2, and myeloperoxidase, respectively. Additionally, these compounds demonstrated good pharmacological properties with minimal toxicity. Conclusively, the identified compounds might be significant contributors to the antimalarial, anti-inflammatory, and antioxidant activity of N. excelsa and are good sources of novel antimalarial, anti-inflammatory, and antioxidant drugs.

Mechanism of tacrolimus in the treatment of lupus nephritis

Systemic lupus erythematosus (SLE) is a complex autoimmune disorder, with more than half of the patients developing lupus nephritis (LN), which significantly contributes to chronic kidney disease (CKD) and end-stage renal disease (ESRD). The treatment of lupus nephritis has always been challenging. Tacrolimus (TAC), an effective immunosuppressant, has been increasingly used in the treatment of LN in recent years. This review aims to explore the mechanisms of action of tacrolimus in treating LN. Firstly, we briefly introduce the pharmacological properties of tacrolimus, including its role as a calcineurin (CaN) inhibitor, exerting immunosuppressive effects by inhibiting T cell activation and cytokine production. Subsequently, we focus on various other immunomodulatory mechanisms of tacrolimus in LN therapy, including its effects on T cells, B cells, and immune cells in kidney. Particularly, we emphasize tacrolimus’ regulatory effect on inflammatory mediators and its importance in modulating the Th1/Th2 and Th17/Treg balance. Additionally, we review its effects on actin cytoskeleton, angiotensin II (Ang II)-specific vascular contraction, and P-glycoprotein activity, summarizing its impacts on non-immune mechanisms. Finally, we summarize the efficacy and safety of tacrolimus in clinical studies and trials. Although some studies have shown significant efficacy of tacrolimus in treating LN, its safety remains a challenge. We outline the potential adverse reactions of long-term tacrolimus use and provide suggestions on effectively monitoring and managing these adverse reactions in clinical practice. In general, tacrolimus, as a novel immunosuppressant, holds promising prospects for treating LN. Of course, further research is needed to better understand its therapeutic mechanisms and ensure its safety and efficacy in clinical practice.

Naturally Occurring Norsteroids and Their Design and Pharmaceutical Application

Naturally Occurring Norsteroids and Their Design and Pharmaceutical Application

Potential Role of Dietary Phenolic Compounds in the Prevention and Treatment of Rheumatoid Arthritis: Current Reports

Rheumatoid arthritis (RA) is a complex illness with both hereditary and environmental components. Globally, in 2019, 18 million people had RA. RA is characterized by persistent inflammation of the synovial membrane that lines the joints, cartilage loss, and bone erosion. Phenolic molecules are the most prevalent secondary metabolites in plants, with a diverse spectrum of biological actions that benefit functional meals and nutraceuticals. These compounds have received a lot of attention recently because they have antioxidant, anti-inflammatory, immunomodulatory, and anti-rheumatoid activity by modulating tumor necrosis factor, mitogen-activated protein kinase, nuclear factor kappa-light-chain-enhancer of activated B cells, and c-Jun N-terminal kinases, as well as other preventative properties. This article discusses dietary polyphenols, their pharmacological properties, and innovative delivery technologies for the treatment of RA, with a focus on their possible biological activities. Nonetheless, commercialization of polyphenols may be achievable only after confirming their safety profile and completing successful clinical trials.

Bioinspired synthesis of silver nanoparticles using Luffa aegyptiaca seed extract and assessment of pharmacological properties

This work used a cost-effective and eco-friendly green process to formulate silver nanoparticles (AgNPs) using Luffa aegyptiaca seed extract (AgNPs-LA). Extraction of L. aegyptiaca seed was done at three different time points [12 (S1), 24 (S2), and 48 (S3) hrs.] to see the effect of extraction on AgNPs-LA. The reaction process of AgNPs was accessed by UV–Vis spectroscopy. Fourier transform infrared (FTIR) spectroscopy, scanning electron microscopy (SEM), transmission electron microscopy (TEM), energy-dispersive X-ray (EDX), X-ray powder diffraction (XRD), dynamic light scattering (DLS), and zeta potential analyses were used to characterize greenly synthesized AgNPs using L. aegyptiaca seed extract. The pharmacological properties of AgNPs-LA were assessed by evaluating the in-vitro antioxidant (DPPH), antidiabetic (α-amylase inhibition), anti-inflammatory (protein denaturation assay), cytotoxicity, and antibacterial activity. The spherical and crystalline structure of AgNPs-LA was observed to have an average size of 168.08 nm for S1. All S1, S2, and S3 showed potent antioxidant activity. For antidiabetic activity, S2 showed the most significant α-amylase inhibitory properties. All AgNPs-LA exhibited the appropriate anti-inflammatory activity as compared to the standard. Only S3 nanoparticles have been shown to have potential cytotoxic effects against malignant human kidney cells. Compared to the standard, the antibacterial test confirmed a higher bactericidal activity of the resulting AgNPs-LA against the Gram-positive and Gram-negative bacteria. An appropriate antioxidant, antidiabetic, anti-inflammatory, cytotoxicity, and antibacterial activity have been demonstrated in the AgNPs derived from the L. aegyptiaca seed extract, which can be considered a promising candidate for various medical applications.