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Toxicological studies are important to investigate the genotoxic effects of various substances. Allium cepa can be used as test model for this purpose. This review summarizes the scope and applications for this A. cepa test model. For this, an up-to-date (April 2023) literature search was made in the Science Direct, PubMed, and Web of Science databases to find published evidence on studies performed using A. cepa as a test model. Out of 3,748 studies, 74 fit the inclusion criteria. The results showed that the use of the test model A. cepa contributed considerably to measuring the toxicological potential of plant extracts, proving the efficacy of the test as a potent bioindicator of toxic effects. In addition, 27 studies used more than one test system to verify the toxicological potential of extracts and fractions. Studies have shown that the A. cepa model has the potential to replace other test systems that make use of animals and cell cultures, besides having other advantages such as low cost, ease of execution, and good conditions for the observation of chromosomes. In conclusion, the A. cepa test can be considered one of the potential biomonitoring systems in toxicological studies of crude extracts.
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Artemisia judica L. is a desert aromatic herb with a characteristic fragrance and taste belonging to the family Asteraceae. This study aimed to evaluate the chemical composition of essential oil isolated from A. judaica L. using GC-MS analysis, along with an investigation of its antioxidant properties and inhibitory activity against key enzymes involved in the pathogenesis of Alzheimer's, diabetes mellitus, and skin pigmentation. GC-MS analysis of the oil revealed the identification of fourteen compounds (97.89%), predominated by piperitone (51.40%), followed by ethyl (E)-cinnamate (20.44%), (+)-2-bornanone (5.63%), and ethyl-(Z)-cinnamate (4.78%). The oil demonstrated remarkable antioxidant activities in the following order: ABTS (66.81 ± 1.49 mgTE/g)< CUPRAC (66.24 ± 0.53mgTE/g)
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Thymol (THY), as the natural monoterpene phenol, acts against oxidative stress and inflammatory processes. This study aimed to evaluate the anti-inflammatory effects and possible molecular mechanisms of THY via formalin-induced mouse and egg albumin-induced chick models alongside molecular docking and molecular dynamic (MD) simulations. THY (7.5, 15, and 30 mg/kg) was investigated, compared to celecoxib and ketoprofen (42 mg/kg), as anti-inflammatory standards. THY dose-dependently and significantly (p < 0.05) decreased paw-licking and edema diameter parameters in formalin (phases I and II) and egg albumin-induced models. Moreover, THY (15 mg/kg) exerted better anti-inflammatory effects in combination with the standard drug ketoprofen than alone and with celecoxib. In silico studies demonstrated elevated binding affinities of THY with cyclooxygenase-2 (COX-2) than the COX-1 enzyme, and the ligand binds at a similar location where ketoprofen and celecoxib interact. The results of MD simulations confirmed the stability of the test ligand. THY exerted anti-inflammatory effects on Swiss mice and young chicks, possibly by interacting with COX-2. As a conclusion, THY might be a hopeful drug candidate for the management of inflammatory disorders.
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BACKGROUND: Sclareol (SCL), a labdane diterpene compound found in Salvia sclarea L., exhibited therapeutic effects. This study investigated the potential interaction between SCL and diazepam (DZP) in modulating sedation in the thiopental sodium-induced sleeping animal model, supported by in-silico molecular docking analysis. METHODS: The control, sclareol (5, 10 and 20â¯mg/kg), and the reference drugs [diazepam: 3â¯mg/kg and Caffeine (CAF): 10â¯mg/kg] were used in male albino mice. Then, sodium thiopental (40â¯mg/kg, i.p.) was administrated to induce sleep. The latent period, percentage of sleep incidence and modulation of latency were measured. Further, homology modeling of human γ-aminobutyric acid (GABA) was conducted examine the binding mode of GABA interaction with SCL, DZP, and CAF compounds RESULTS: SCL (low dose) slightly increased the sleep latency, while the higher dose significantly prolonged sleep latency. DZP, a GABAA receptor agonist, exhibited strong sleep-inducing properties, reducing sleep latency, and increasing sleeping time. Caffeine (CAF) administration prolonged sleep latency and reduced sleeping time, consistent with its stimulant effects. The combination treatments involving SCL, DZP, and CAF showed mixed effects on sleep parameters. The molecular docking revealed good binding affinities of SCL, DZP, and CAF for GABAA receptor subunits A2 and A5. CONCLUSIONS: Our findings highlighted the complex interplay between SCL, DZP, and CAF in regulating sleep behaviors and provided insights into potential combination therapies for sleep disorders.
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Diazepam , Hipnóticos e Sedativos , Simulação de Acoplamento Molecular , Sono , Tiopental , Animais , Masculino , Hipnóticos e Sedativos/farmacologia , Camundongos , Diazepam/farmacologia , Sono/efeitos dos fármacos , Tiopental/farmacologia , Diterpenos/farmacologia , Cafeína/farmacologia , Simulação por Computador , Receptores de GABA-A/metabolismo , Humanos , Relação Dose-Resposta a Droga , Latência do Sono/efeitos dos fármacosRESUMO
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.
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Cafeína , Purinas , Animais , Humanos , Cafeína/química , Cafeína/metabolismo , Cafeína/farmacologia , Café/química , Café/metabolismo , Purinas/química , Purinas/biossíntese , Purinas/farmacologia , Purinas/metabolismoRESUMO
Recently, nanotechnology has emerged as an extensively growing field. Several important fabricated products including Carbon nanotubes (CNTs) are of great importance and hold significance in several industrial sectors, mainly food industry. Recent developments have come up with methodologies for the prevention of health complications like lack of adequate nutrition in our diet. This review delves deeper into the details of the food supplementation techniques and how CNTs function in this regard. This review includes the challenges in using CNTs for food applications and their future prospects in the industry. Food shortage has become a global issue and limiting food resources put an additional burden on the farmers for growing crops. Apart from quantity, quality should also be taken into consideration and new ways should be developed for increasing nutritional value of food items. Food supplementation has several complications due to the biologically active compounds and reaction in the in vivo environment, CNTs can play a crucial role in countering this problem through the supplementation of food by various processes including; nanoencapsulation and nanobiofortification thus stimulating crop growth and seed germination rates. CNTs also hold a key position in biosensing and diagnostic application for either the quality control of the food supplements or the detection of contagions like toxins, chemicals, dyes, pesticides, pathogens, additives, and preservatives. Detection such pathogens can help in attaining global food security goal and better production and provision of food resources. The data used in the current review was collected up to date as of March 31, 2024 and contains the best of our knowledge. Data collection was performed from various reliable and authentic literatures comprising PubMed database, Springer Link, Scopus, Wiley Online, Web of Science, ScienceDirect, and Google Scholar. Research related to commercially available CNTs has been added for the readers seeking additional information on the use of CNTs in various economic sectors.
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Introduction: D-pinitol, a naturally occurring inositol, has diverse biological activities like antioxidant, antimicrobial and anticancer activities. This study aimed to evaluate anti-inflammatory effect of d-pinitol in a chick model. Additionally, in silico studies were performed to evaluate the molecular interactions with cyclooxygenase-2 (COX-2). Methods: The tested groups received d-pinitol (12.5, 25, and 50 mg/kg) and the standard drugs celecoxib and ketoprofen (42 mg/kg) via oral gavage prior to formalin injection. Then, the number of licks was counted for the first 10 min, and the paw edema diameter was measured at 60, 90, and 120 min. Results and Discussion: The d-pinitol groups significantly (p < 0.05) reduced the number of paw licks and paw edema diameters, compared to negative control. When d-pinitol was combined with celecoxib, it reduced inflammatory parameters more effectively than the individual groups. The in silico study showed a promising binding capacity of d-pinitol with COX-2. Taken together, d-pinitol exerted anti-inflammatory effects in a dose-dependent manner, possibly through COX-2 interaction pathway.
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Natural approach became a high demand for the prevention and treatment of such diseases for their proven safety and efficacy. This study is aimed to perform comparative phytochemical analysis of white pitaya (Hylocereus undatus) peel, pulp and seed extracts via determination of total flavonoid content, phenolic content, and antioxidant capacity, coupled with HPLC-ESI/MS-MS analysis. Further, we evaluated the synergistic cytotoxic potential with Cisplatin against cervical cancer cells with investigation of underlying mechanism. The highest content of phenolics and antioxidants were found in both seed and peel extracts. The HPLC-ESI/MS-MS revealed identification of flavonoids, phenolic acids, anthocyanin glycosides, lignans, stilbenes, and coumarins. The cytotoxicity effects were evaluated by MTT assay against prostate, breast and cervical (HeLa) and Vero cell lines. The seed and peel extracts showed remarkable cytotoxic effect against all tested cell lines. Moreover, the selectivity index confirmed high selectivity of pitaya extracts to cancer cells and safety on normal cells. The combined therapy with Cisplatin effectively enhanced its efficacy and optimized the treatment outcomes, through the apoptotic ability of pitaya extracts in HeLa cells, as evaluated by flow cytometry. Besides, RT-PCR and western blotting analysis showed downregulation of Bcl-2 and overexpression of P53, BAX among HeLa cells treated with pitaya extracts, which eventually activated apoptosis process. Thus, pitaya extract could be used as adjuvant therapy with cisplatin for treatment of cervical cancer. Furthermore, in-vivo extensive studies on the seed and peel extracts, and their compounds are recommended to gain more clarification about the required dose, and side effects.
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Apoptose , Cactaceae , Cisplatino , Sinergismo Farmacológico , Frutas , Extratos Vegetais , Espectrometria de Massas por Ionização por Electrospray , Espectrometria de Massas em Tandem , Neoplasias do Colo do Útero , Humanos , Neoplasias do Colo do Útero/tratamento farmacológico , Neoplasias do Colo do Útero/metabolismo , Frutas/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Cromatografia Líquida de Alta Pressão/métodos , Células HeLa , Espectrometria de Massas por Ionização por Electrospray/métodos , Espectrometria de Massas em Tandem/métodos , Feminino , Animais , Cactaceae/química , Apoptose/efeitos dos fármacos , Cisplatino/farmacologia , Células Vero , Chlorocebus aethiops , Sementes/química , Antineoplásicos Fitogênicos/farmacologia , Flavonoides/farmacologia , Flavonoides/análise , Antioxidantes/farmacologia , Fenóis/farmacologia , Fenóis/análise , Metabolômica/métodosRESUMO
St. John's Wort, commonly known as Hypericum perforatum L., is a flowering plant in the Clusiaceae family that traditionally been employed for treating anxiety, depression, wounds, burns, sunburn, irritation, and stomach ailments. This review provides a synopsis of H. perforatum L. phytoconstituents and their biological effects, highlighting its beneficial therapeutic properties for dermatological indications, as well as its antioxidant, antimicrobial, anti-inflammatory, and anti-angiogenic activity in various applications including wound healing and skin conditions such as eczema, sun burn and minor burns also spastic paralysis, stiff neck and mood disorders as anti-depressant and nerve pains such as neuralgia. The data were collected from several databases as Web of Science PubMed, ScienceDirect, Scopus and Google Scholar using the terms: "H. perforatum L.", "H. perforatum L. /phytochemistry," and "H. perforatum extracts/wound healing" collected from 1994 to 2023. The findings suggest H. perforatum L. acts through various mechanisms and plays a role in each phase of the wound healing process, including re-epithelialization, angiogenesis, wound contraction, and connective tissue regeneration. H. perforatum L. enhances collagen deposition, decreases inflammation, inhibits fibroblast migration, and promotes epithelialization by increasing the number of fibroblasts with polygonal shape and the number of collagen fibers within fibroblasts. H. Perforatum L. extracts modulate the immune response and reduce inflammation were found to accelerate the wound healing process via inhibition of inflammatory mediators' production like interleukin-6, tumor necrosis factor-α, cyclooxygenase-2 gene expression, and inducible nitric oxide synthase. Thus, H. perforatum L. represents a potential remedy for a wide range of dermatological problems, owing to its constituents with beneficial therapeutic properties. H. perforatum L. could be utilized in the development of novel wound healing therapies.
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Hypericum , Compostos Fitoquímicos , Extratos Vegetais , Cicatrização , Hypericum/química , Cicatrização/efeitos dos fármacos , Humanos , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/química , Extratos Vegetais/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologiaRESUMO
Breast cancer is the most prevalent type of cancer, the fifth leading cause of cancer-related deaths, and the second leading cause of cancer deaths among women globally. Recent research has provided increasing support for the significance of phytochemicals, both dietary and non-dietary, particularly triterpenoids, in the mitigation and management of breast cancer. Recent studies showed that triterpenoids are promising agents in the treatment and inhibition of breast cancer achieved through the implementation of several molecular modes of action on breast cancer cells. This review discusses recent innovations in plant triterpenoids and their underlying mechanisms of action in combating breast cancer within the timeframe spanning from 2017 to 2023. The present work is an overview of different plant triterpenoids with significant inhibition on proliferation, migration, apoptosis resistance, tumor angiogenesis, or metastasis in various breast cancer cells. The anticancer impact of triterpenoids may be attributed to their antiproliferative activity interfering with angiogenesis and differentiation, regulation of apoptosis, DNA polymerase inhibition, change in signal transductions, and impeding metastasis. The present review focuses on several targets, mechanisms, and pathways associated with pentacyclic triterpenoids, which are responsible for their anticancer effects. We could conclude that natural triterpenoids are considered promising agents to conquer breast cancer.
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Antineoplásicos Fitogênicos , Neoplasias da Mama , Triterpenos , Humanos , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/patologia , Neoplasias da Mama/metabolismo , Triterpenos/farmacologia , Triterpenos/uso terapêutico , Feminino , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/uso terapêutico , Animais , Apoptose/efeitos dos fármacos , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Proliferação de Células/efeitos dos fármacosRESUMO
Inflammation is a complex and necessary mechanism of an organ's response to biological, chemical and/or physical stimuli. In recent years, investigations on natural compounds with therapeutic actions for the treatment of different diseases have increased. Among these compounds, bromelain is highlighted, as a cysteine protease isolated from the Ananas comosus (pineapple) stem. This review aimed to evaluate the anti-inflammatory activity of bromelain, as well as its pathways on inflammatory mediators, through a systematic review with in vitro studies on different cell lines. The search was performed in PubMed, Science Direct, Scopus, Cochrane Library and Web of Science databases. Bromelain reduced IL-1ß, IL-6 and TNF-α secretion when immune cells were already stimulated in an overproduction condition by proinflammatory cytokines, generating a modulation in the inflammatory response through prostaglandins reduction and activation of a cascade reactions that trigger neutrophils and macrophages, in addition to accelerating the healing process.
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Gigantol, a bibenzyl compound extracted from various medicinal plants, has shown a number of biological activities, making it an attractive candidate for potential medical applications. This systematic review aims to shed light on gigantol's promising role in inflammation treatment and its underlying mechanisms. Gigantol exhibits potential anti-inflammatory properties in pre-clinical pharmacological test systems. It effectively reduced the levels of pro-inflammatory markers and arachidonic acid metabolites through various pathways, such as NF-κB, AKT, PI3K, and JNK/cPLA2/12-LOX. The in-silico investigations demonstrated that the MMP-13 enzyme served as the most promising target for gigantol with highest binding affinity (docking score = -8.8 kcal/mol). Encouragingly, the absorption, distribution, metabolism, excretion, and toxicity (ADMET) analysis of gigantol confirmed its compatibility with the necessary physiochemical, pharmacokinetic, and toxicity properties, bolstering its potential as a drug candidate. Gigantol, with its well-documented anti-inflammatory properties, could be a promising agent for treating inflammation in the near future.
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Introduction: Cheilanthes tenuifolia is an evergreen ornamental small fern, belonging to the family Pteridaceae, that grows in warm and rocky regions worldwide. Many species of Cheilanthes genus are evidently endowed with important phytochemicals and bioactivities. This study aimed to perform a preliminary phytochemical analysis of Cheilanthes tenuifolia leaves alongside an evaluation of free radical scavenging, anti-inflammatory, antimicrobial, and clot lysis activities of extract fractions. Materials and methods: A preliminary phytochemical analysis was done after fractionation of ethanolic extract (ECT) with n-hexane (HCT) and chloroform (CCT). Then, 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, egg albumin and RBC membrane stabilization tests, disc diffusion, and human blood clot lysis assays were performed. Results: Phytochemical investigations suggested that the plant is rich in alkaloids, glycosides, tannins, and flavonoids. All obtained fractions exhibited concentration-dependent radical scavenging, inhibition of egg protein denaturation and RBC membrane lysis capacities. Except for antifungal tests, ECT exhibited better DPPH radical scavenging, anti-inflammatory, antibacterial, and clot lysis capacities than HCT and CCT fractions. However, all fractions exhibited a mild anti-inflammatory activity. Conclusion: C. tenuifolia might be a good source of antioxidant, anti-microbial, and anti-atherothrombotic agents. Further studies are required to isolate and characterize the active principles liable for each bioactivity, along with possible molecular interactions.
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Herbal spices are widely consumed as food additives owing to their distinct aroma and taste as well as a myriad of economic and health value. The aroma profile of four major spices including bay leaf, black pepper, capsicum, and fennel was tested using HS-SPME/GC-MS and in response to the most widely used spices´ processing methods including autoclaving and γ-radiation at low and high doses. Additionally, the impact of processing on microbial contamination of spices was tested using total aerobic count. GC-MS analysis led to the identification of 22 volatiles in bay leaf, 34 in black pepper, 23 in capsicum, and 24 in fennel. All the identified volatiles belonged to oxides/phenols/ethers, esters, ketones, alcohols, sesquiterpene and monoterpene hydrocarbons. Oxides/phenol/ethers were detected at high levels in all tested spices at ca. 44, 28.2, 48.8, 61.1%, in bay leaves, black pepper, capsicum, and fennel, respectively of the total blend and signifying their typical use as spices. Total oxides/phenol/ethers showed an increase in bay leaf upon exposure to γ-radiation from 44 to 47.5%, while monoterpene hydrocarbons were enriched in black pepper upon autoclaving from 11.4 in control to reach 65.9 and 82.6% for high dose and low dose of autoclaving, respectively. Cineole was detected in bay leaf at 17.9% and upon exposure to autoclaving at high dose and γ-radiation (both doses) its level increased by 29-31%. Both autoclaving and γ-radiation distinctly affected aroma profiles in examined spices. Further, volatile variations in response to processing were assessed using multivariate data analysis (MVA) revealing distinct separation between autoclaved and γ-radiated samples compared to control. Both autoclaving at 115 °C for 15 min and radiation at 10 kGy eliminated detected bioburden in all tested spices i.e., reduced the microbial counts below the detection limit (< 10 cfu/g).
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Foeniculum , Piper nigrum , Compostos Orgânicos Voláteis , Cromatografia Gasosa-Espectrometria de Massas/métodos , Odorantes/análise , Fenol/análise , Microextração em Fase Sólida/métodos , Quimiometria , Especiarias , Monoterpenos/análise , Éteres , Óxidos , Compostos Orgânicos Voláteis/análiseRESUMO
This study focused to assess the efficacy of Gynura procumbens (GP) leaf extract against cisplatin (CP)-induced hepatorenal complications in Wister albino rats. Additionally, it aims to detect polyphenolic compounds using high-performance liquid chromatography with diode-array detection (HPLC-DAD). The rats were treated intraperitoneally with CP (7.5â mg/kg) to mediate hepatorenal damage. They were then treated with GP extract (75 and 150â mg/kg, P.O.) for 7 consecutive days. Although GP extract significantly ameliorated CP-mediated hepatorenal biomarkers like alkaline phosphatase (ALP), alanine aminotransferase (ALT), aspartate aminotransferase (AST), creatinine, and blood urea nitrogen (BUN) levels in a dose-dependent manner, GP extract at 150â mg/kg dose normalized hepatorenal biomarkers ALP (45.11â U/L), ALT (34â U/L), AST (29â U/L), creatinine (10.3â mg/dl) and BUN (11.19â mg/dl) while comparing to control and disease group. Similarly, though it significantly reduced CP-induced oxidative stress inducers, including nitric oxide (NO) and advanced oxidative protein products (AOPP), higher dose (150â mg/kg) exhibited better activity in reducing NO (281.54â mmol/gm tissue in liver and 52.73â mmol/gm tissue in the kidney) and AOPP (770.95â mmol/mg protein in liver and 651.90â mmol/mg protein in the kidney). Besides, it showed better enhancement in the antioxidant enzymes superoxide dismutase, and glutathione levels at a higher dose (150â mg/kg). Histopathological studies showed that CP caused collagen accumulation in the liver and kidney tissues. GP extract drained the collagen mass and acted against hepatorenal damage. Ellagic acid, gallic acid, quercetin hydrate, kaempferol, and rutin hydrate were revealed in GP extract. In-silico modelling showed good docking scores of the polyphenolic compounds with molecular targets including CYP4502E1, NF-κB, caspase-3, and TNF-α. GP could be an effective therapeutic option for management of anticancer drugs' complications like CP-induced organ damage, although clinical studies are required to establish herbal formulation.
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Cisplatino , Estresse Oxidativo , Extratos Vegetais , Ratos Wistar , Animais , Estresse Oxidativo/efeitos dos fármacos , Ratos , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Masculino , Folhas de Planta/química , Mediadores da Inflamação/metabolismo , Mediadores da Inflamação/antagonistas & inibidores , Asteraceae/química , Antioxidantes/farmacologia , Antioxidantes/química , Relação Dose-Resposta a Droga , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Simulação de Acoplamento Molecular , Rim/efeitos dos fármacos , Rim/metabolismo , Rim/patologia , Antineoplásicos/farmacologia , Antineoplásicos/químicaRESUMO
Pistacia khinjuk is a species of flowering plants belonging to family Anacardiaceae, with promising pharmacological activities like antioxidants, anti-inflammatory, antiviral, and antimicrobial. This study aimed to investigate the GC-MS chemical composition of essential oil isolated from Pistacia khinjuk leaves and its inhibitory properties against aging-relevant enzymes such a collagenase and elastase. The isolated oil showed predominance of ß-cadinene (15.34 %), γ-amorphene (8.50 %), α-cadinol (8.14 %), τ-cadinol (7.57 %), (E)-ß-caryophyllene (5.77 %), α-pinene (4.70 %), phytol (4.57 %), α-muurolene (3.30 %), (+)-epi-bicyclosesquiphellandrene (3.21 %), and cubenene (3.16 %). Further, it showed remarkable inhibitory activities against collagenase and elastase with IC50 values of 15.61±0.69 and 41.12±2.09â µg/mL, respectively compared to epigallocatechin gallate (IC50=29.52±1.3â µg/mL and 26.86±1.37â µg/mL). as a conclusion, the leaf oil is recommended for topical cosmetic preparations to retard skin aging symptoms such as wrinkles. However, the bioavailability assessment and toxicological profile should be considered in the future studies.
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Colagenases , Cromatografia Gasosa-Espectrometria de Massas , Óleos Voláteis , Elastase Pancreática , Pistacia , Folhas de Planta , Envelhecimento da Pele , Folhas de Planta/química , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação , Elastase Pancreática/antagonistas & inibidores , Elastase Pancreática/metabolismo , Pistacia/química , Envelhecimento da Pele/efeitos dos fármacos , Colagenases/metabolismo , Inibidores Enzimáticos/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , HumanosRESUMO
Quercetin is the most common polyphenolic flavonoid present in fruits and vegetables demonstrating versatile health-promoting effects. This study aimed to examine the effects of quercetin (QR) and sclareol (SCL) on the thiopental sodium (TS)-induced sleeping and forced swimming test (FST) mouse models. SCL (1, 5, and 10 mg/kg, p.o.) or QR (50 mg/kg, p.o.) and/or diazepam (DZP) (3 mg/kg, i.p.) were employed. After 30 min of TS induction, individual or combined effects on the animals were checked. In the FST test, the animals were subjected to forced swimming after 30 min of administration of the test and/or controls for 5 min. In this case, immobility time was measured. In silico studies were conducted to evaluate the involvement of GABA receptors. SCL (5 and 10 mg/kg) significantly increased the latency and decreased sleeping time compared to the control in the TS-induced sleeping time study. DZP (3 mg/kg) showed a sedative-like effect in animals in both sleeping and FST studies. QR (50 mg/kg) exhibited a similar pattern of activity as SCL. However, its effects were more prominent than those of SCL groups. SCL (10 mg/kg) altered the DZP-3-mediated effects. SCL-10 co-treated with QR-50 significantly (p < 0.05) increased the latency and decreased sleep time and immobility time, suggesting possible synergistic antidepressant-like effects. In silico studies revealed that SCL and QR demonstrated better binding affinities with GABAA receptor, especially α2, α3, and α5 subunits. Both compounds also exhibited good ADMET and drug-like properties. In animal studies, the both compounds worked synergistically to provide antidepressant-like effects in a slightly different fashion. As a conclusion, the combined administration of SCL and QR may be used in upcoming neurological clinical trials, according to in vivo and in silico findings. However, additional investigation is necessary to verify this behavior and clarify the potential mechanism of action.
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Antidepressivos , Diazepam , Quercetina , Sono , Tiopental , Animais , Camundongos , Antidepressivos/farmacologia , Masculino , Quercetina/farmacologia , Diazepam/farmacologia , Sono/efeitos dos fármacos , Tiopental/farmacologia , Natação , Modelos Animais de Doenças , Simulação de Acoplamento Molecular , Hipnóticos e Sedativos/farmacologia , Receptores de GABA-A/metabolismoRESUMO
This work aims to develop plant extract-loaded electrospun nanofiber as an effective wound dressing scaffolds for topical wound healing. Electrospun nanofibers were fabricated from Syzygium cumini leaf extract (SCLE), poly(lactic-co-glycolic acid) (PLGA), poly(methyl methacrylate) (PMMA), collagen and glycine. Electrospinning conditions were optimized to allow the formation of nanosized and uniform fibers that display smooth surface. Morphology and swelling behavior of the formed nanofibers were studied. In addition, the antibacterial activity of the nanofibers against multidrug-resistant and human pathogens was assessed by agar-well diffusion. Results showed that nanofibers containing Syzygium cumini extract at concentrations of 0.5 and 1% w/v exhibited greater antibacterial activity against the tested Gram-positive (i.e., Staphylococcus aureus, Candida albicans, Candida glabrata and Bacillus cereus) and Gram-negative (i.e., Salmonella paratyphi and Escherichia coli) pathogens compared to the same concentrations of the plain extract. Furthermore, in vivo wound healing was evaluated in Wistar rats over a period of 14 days. In vivo results demonstrated that nanofiber mats containing SCLE and collagen significantly improved wound healing within two weeks, compared to the control untreated group. These findings highlight the potential of fabricated nanofibers in accelerating wound healing and management of topical acute wounds.
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Diabetes mellitus is a globally metabolic endocrine syndrome marked by a deficiency of insulin secretion (type-1 DM) or glucose intolerance arising from insulin response impairment (type-2 DM) leading to abnormal glucose metabolism. With an increasing interest in natural dietary components for diabetes management, the identification of novel agents witnessed major discoveries. Plant-derived mucilage, pectin, and inulin are important non-starch polysaccharides that exhibit effective antidiabetic properties often termed soluble dietary fiber (SDF). SDF affects sugar metabolism through multiple mechanisms affecting glucose absorption and diffusion, modulation of carbohydrate metabolizing enzymes (α-amylase and α-glucosidase), ameliorating ß-pancreatic cell dysfunction, and improving insulin release or sensitivity. Certain SDFs inhibit dipeptidyl peptidase-4 and influence the expression levels of genes related to glucose metabolism. This review is designed to discuss holistically and critically the antidiabetic effects of major SDF and their underlying mechanisms of action. This review should aid drug discovery approaches in developing novel natural antidiabetic drugs from SDF.
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Diabetes Mellitus Tipo 2 , Hipoglicemiantes , Humanos , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Hipoglicemiantes/química , Inulina , Pectinas/farmacologia , Pectinas/uso terapêutico , Frutanos , Polissacarídeos , Insulina , Glucose , Diabetes Mellitus Tipo 2/tratamento farmacológicoRESUMO
This review aims to provide an in-depth analysis of the pharmacological properties of mangiferin, focusing primarily on its bioavailability and mechanisms of action, and its potential therapeutic applications, especially in the context of chronic diseases. We conducted a comprehensive examination of in vitro and in vivo studies, as well as clinical trials involving mangiferin or plant extracts containing mangiferin. The primary source of mangiferin is Mangifera indica, but it's also found in other plant species from the families Anacardiaceae, Gentianaceae, and Iridaceae. Mangiferin has exhibited a myriad of therapeutic properties, presenting itself as a promising candidate for treating various chronic conditions including neurodegenerative disorders, cardiovascular diseases, renal and pulmonary diseases, diabetes, and obesity. Despite the promising results showcased in many in vitro studies and certain animal studies, the application of mangiferin has been limited due to its poor solubility, absorption, and overall bioavailability. Mangiferin offers significant therapeutic potential in treating a spectrum of chronic diseases, as evidenced by both in vitro and clinical trials. However, the challenges concerning its bioavailability necessitate further research, particularly in optimizing its delivery and absorption, to harness its full medicinal potential. This review serves as a comprehensive update on the health-promoting and therapeutic activities of mangiferin.