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In 2021, the World Health Organization released the fifth edition of the central nervous system (CNS) tumor classification. This classification uses histopathology and molecular pathogenesis to group tumors into more biologically and molecularly defined entities. The prognosis of brain cancer, particularly malignant tumors, has remained poor worldwide, approximately 308,102 new cases of brain and other CNS tumors were diagnosed in the year 2020, with an estimated 251,329 deaths. The cost and time-consuming nature of studies to find new anticancer agents makes it necessary to have well-designed studies. In the present study, the pathways that can be targeted for drug development are discussed in detail. Some of the important cellular origins, signaling, and pathways involved in the efficacy of bioactive molecules against CNS tumorigenesis or progression, as well as prognosis and common approaches for treatment of different types of brain tumors, are reviewed. Moreover, different study tools, including cell lines, in vitro, in vivo, and clinical trial challenges, are discussed. In addition, in this article, natural products as one of the most important sources for finding new chemotherapeutics were reviewed and over 700 reported molecules with efficacy against CNS cancer cells are gathered and classified according to their structure. Based on the clinical trials that have been registered, very few of these natural or semi-synthetic derivatives have been studied in humans. The review can help researchers understand the involved mechanisms and design new goal-oriented studies for drug development against CNS malignancies.
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Antineoplásicos , Produtos Biológicos , Neoplasias do Sistema Nervoso Central , Desenvolvimento de Medicamentos , Humanos , Produtos Biológicos/uso terapêutico , Produtos Biológicos/farmacologia , Neoplasias do Sistema Nervoso Central/tratamento farmacológico , Antineoplásicos/uso terapêutico , Antineoplásicos/farmacologia , Animais , Ensaios Clínicos como AssuntoRESUMO
PURPOSE: Pyrus boissieriana is a rich source of arbutin and has been used in herbal medicine to treat infectious diseases. This study aimed to investigate the effect of the arbutin-rich fraction of Pyrus boissieriana aerial parts on Toxoplasma gondii In Vitro and In Vivo. METHODS: An arbutin-rich fraction of P. boissieriana was prepared beforehand. Flow cytometry was used to evaluate the effect of different concentrations (1-512 µg/ml) of the P. boissieriana arbutin-rich fraction on Toxoplasma tachyzoites (RH strain). The cytotoxicity of the concentrations on the macrophage J774 cell line was also investigated by MTT assay. For In Vivo investigation, 4-6-week-old female mice infected with the RH strain of T. gondii were treated with different doses (16, 32, 64, 256, and 512 mg/kg) of the fraction using gavage. RESULTS: The highest and lowest lethality of the tachyzoites were 89.6% and 25.9% related to the concentrations of 512 µg/ml and 1 µg/ml, respectively, with an IC50 value of 18.1 µg/ml ± 0.37. The cytotoxicity test showed an IC50 value of 984.3 µg/ml ± 0.76 after 48 h incubation. The mean survival of mice at the lowest treated dose (16 mg/kg) was 6.6 days, and it was 15 days at the highest dose (512 mg/kg). The concentrations of 512, 256, 128, and 64 mg/kg of the fraction compared to the negative control (6.2 days mean survival) significantly increased the survival time of mice (P < 0.001, P = 0.009, P = 0.018, and P = 0.021, respectively). CONCLUSION: The results showed that the arbutin-rich fraction of P. boissieriana is effective against T. gondii In Vitro and In Vivo and may be a reliable alternative to conventional treatment for toxoplasmosis, although further studies are necessary.
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Antiprotozoários , Arbutina , Extratos Vegetais , Toxoplasma , Animais , Toxoplasma/efeitos dos fármacos , Camundongos , Feminino , Extratos Vegetais/farmacologia , Linhagem Celular , Arbutina/farmacologia , Antiprotozoários/farmacologia , Macrófagos/parasitologia , Macrófagos/efeitos dos fármacos , Toxoplasmose Animal/tratamento farmacológico , Toxoplasmose Animal/parasitologia , Concentração Inibidora 50 , Toxoplasmose/tratamento farmacológico , Toxoplasmose/parasitologiaRESUMO
A comprehensive literature search was conducted in PubMed, Cochrane Library, Web of Science, Scopus, the National Library of Medicine (NLM) catalog, and Google Scholar from January 1980 up until October 2023 on plants in the Gundelia genus. Gundelia L. (Asteraceae) has been treated as a monospecific genus with Gundelia tournefortii L. (1753: 814) in most recent floras with wide variation in corolla color, but nowadays, the genus consists of 17 species. The unripe inflorescences of these species, especially G. tournefortii L., are consumed in many ways. 'Akkoub' or 'akko' in Arabic, "Kangar" in Persian, and "Silifa" in Greek are the common names of G. tournefortii L., also known as tumble thistle in English. They have been used in traditional medicine to treat bronchitis, kidney stones, diarrhea, stomach pain, inflammation, liver and blood diseases, bacterial and fungal infections, and mumps. Based on recent studies, their extracts have exhibited hepatoprotective, hypolipidemic, antioxidant, anti-inflammatory, and antimicrobial effects. Moreover, a variety of phytochemicals, including terpenoids, sterols, and fatty acids, as well as vitamins and minerals, have been identified in this genus. This study reviewed the ethnobotany, phytochemicals, and biological activities of the plants in the Gundelia genus as functional foods and herbal remedies.
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Asteraceae , Etnobotânica , Etnofarmacologia , Fitoterapia , Medicina Tradicional , Extratos Vegetais/farmacologia , Compostos Fitoquímicos/farmacologiaRESUMO
Ten sesquiterpene lactones isolated from Anvillea garcinii (Burm.f.) DC ethanolic extract were assessed for their anti-inflammatory potential by myeloperoxidase (MPO) activity assignment, and mice paw swelling model. 3α,4α-10ß-trihydroxy-8α-acetyloxyguaian-12,6α-olide (1), epi-vulgarin (3), 9a-hydroxyparthenolide (4), garcinamine C (7), garcinamine D (8), garcinamine E (9), and 4, 9-dihydroxyguaian-10(14)-en-12-olide (10) showed explicit anti-inflammatory activity in rodent paw edema and MPO assignment. The findings of this study showed that the α-methylene γ-lactone moiety does not always guarantee an anti-inflammatory effect, but the presence of proline at the C3 of the lactone ring improves the binding of sesquiterpene lactones with MPO isoenzymes, resulting in a more potent inhibition.
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Sesquiterpenos de Guaiano , Sesquiterpenos , Camundongos , Animais , Sesquiterpenos de Guaiano/farmacologia , Anti-Inflamatórios/farmacologia , Sesquiterpenos/farmacologia , Lactonas/farmacologiaRESUMO
Natural pigments are important sources for the screening of bioactive lead compounds. This article reviewed the chemistry and therapeutic potentials of over 570 colored molecules from plants, fungi, bacteria, insects, algae, and marine sources. Moreover, related biological activities, advanced extraction, and identification approaches were reviewed. A variety of biological activities, including cytotoxicity against cancer cells, antioxidant, anti-inflammatory, wound healing, anti-microbial, antiviral, and anti-protozoal activities, have been reported for different pigments. Considering their structural backbone, they were classified as naphthoquinones, carotenoids, flavonoids, xanthones, anthocyanins, benzotropolones, alkaloids, terpenoids, isoprenoids, and non-isoprenoids. Alkaloid pigments were mostly isolated from bacteria and marine sources, while flavonoids were mostly found in plants and mushrooms. Colored quinones and xanthones were mostly extracted from plants and fungi, while colored polyketides and terpenoids are often found in marine sources and fungi. Carotenoids are mostly distributed among bacteria, followed by fungi and plants. The pigments isolated from insects have different structures, but among them, carotenoids and quinone/xanthone are the most important. Considering good manufacturing practices, the current permitted natural colorants are: Carotenoids (canthaxanthin, ß-carotene, ß-apo-8'-carotenal, annatto, astaxanthin) and their sources, lycopene, anthocyanins, betanin, chlorophyllins, spirulina extract, carmine and cochineal extract, henna, riboflavin, pyrogallol, logwood extract, guaiazulene, turmeric, and soy leghemoglobin.
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Cosméticos , Xantonas , Antocianinas/farmacologia , Corantes , Carotenoides/farmacologia , Carotenoides/química , Plantas/química , Terpenos , Fungos/química , Bactérias , Pigmentos Biológicos/farmacologia , Pigmentos Biológicos/químicaRESUMO
The Latin word lupus, meaning wolf, was in the medical literature prior to the 1200s to describe skin lesions that devour flesh, and the resources available to physicians to help people were limited. The present text reviews the ethnobotanical and pharmacological aspects of medicinal plants and purified molecules from natural sources with efficacy against lupus conditions. Among these molecules are artemisinin and its derivatives, antroquinonol, baicalin, curcumin, emodin, mangiferin, salvianolic acid A, triptolide, the total glycosides of paeony (TGP), and other supplements such as fatty acids and vitamins. In addition, medicinal plants, herbal remedies, mushrooms, and fungi that have been investigated for their effects on different lupus conditions through clinical trials, in vivo, in vitro, or in silico studies are reviewed. A special emphasis was placed on clinical trials, active phytochemicals, and their mechanisms of action. This review can be helpful for researchers in designing new goal-oriented studies. It can also help practitioners gain insight into recent updates on supplements that might help patients suffering from lupus conditions.
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As a major public health issue, cutaneous leishmaniasis (CL) has a number of complications, including drug resistance and poor response to conventional treatments. Over the last decade, research on natural sources for finding new antileishmanial agents has been a critical part of tropical disease research. Natural products also should be regarded as one of the most valuable applications for CL infection drug development. In this study, we assessed the in vitro and in vivo antileishmanial potential of Carex pendula Huds. (hanging sedge) methanolic extract and its fractions against Leishmania major produced cutaneous infection. Although the methanolic extract and its fractions exhibited suitable activity, the ethyl acetate fraction showed the best activity (with the half maximal inhibitory concentration IC50 = 1.627 ± 0.211 mg/mL). The toxicity and selectivity indices (SI) of all samples were determined in murine peritoneal macrophage cells (J774A.1) using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) test. The flavonoid components of the ethyl acetate fraction were identified using liquid chromatography electrospray ionization mass spectrometry (LC-ESI MS/MS). Nine chemical compounds were identified in this fraction, including three flavonols, four flavanonols, and two flavan derivatives. L. major-infected mice were used as an in vivo model because the methanolic extract was effective against L. major promastigotes in the mammalian cell line J774A.1 with SI = 2.514 (tail lesion size model). In silico analysis of identified compounds also revealed a favorable interaction between compounds 2-5 and L. major protein targets (3UIB, 4JZX, 4JZB, 5L4N, and 5L42). According to the findings of this study, the ethyl acetate fraction (as flavonoid fraction) exhibited considerable in vitro antileishmanial activity.
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Antiprotozoários , Leishmaniose Cutânea , Animais , Camundongos , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Flavonoides/farmacologia , Espectrometria de Massas em Tandem , Antiprotozoários/farmacologia , Antiprotozoários/uso terapêutico , Leishmaniose Cutânea/tratamento farmacológico , Metanol/uso terapêutico , MamíferosRESUMO
Fruits, flowers, leaves, essential oils, hydrosols, and juices of citrus spp. Are utilized to prepare various forms of food products. Along with their nutritional values, in the health industry, different parts of the plants of the citrus genus have been used as supplements or remedies to prevent or control diseases. This review focused on reported meta-analyses and clinical trials on the health benefits of citrus plants as functional foods. Also, chemical compounds of various citrus species were reviewed. The following information sources were used for data collection: Google Scholar, the Web of Science, Scopus, and PubMed. Various keywords, including "citrus AND chemical compounds," "citrus AND phytochemicals," "citrus species," "citrus AND meta-analysis," "nutritional and therapeutical values of citrus spp.," "clinical trials AND citrus," "clinical trials AND Rutaceae," "health benefits of citrus spp.," "citrus edible or non-edible applications," and scientific names of the citrus plants were utilized to collect data for the review. The scientific name and common name of all twenty-eight citrus species, along with any of the above keywords, were also searched in the mentioned databases. Scientific papers and data sources were sought to review and discuss the citrus plant's nutritional and therapeutic importance. Several meta-analyses and clinical trials have reported beneficial effects of citrus spices on a variety of cancer risks, cardiovascular risk factors, neurologic disorders, urinary tract conditions, and gastrointestinal tract conditions. They have shown anxiolytic, antimicrobial, and pain-alleviating effects. Some of them can be helpful in managing obesity and cardiovascular risk factors.
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Citrus , Alimento Funcional , Humanos , Alimento Funcional/análise , Citrus/química , Suplementos Nutricionais , Frutas/químicaRESUMO
BACKGROUND AND AIMS: Coronary artery bypass graft surgery (CABG) is a primary treatment in coronary artery disease (CAD). Patients experience pain after CABG. Pain may increase postoperative complications and decrease quality of life (QoL). This study aims to determine the lavandula aromatherapy effect on patients' pain after CABG. METHODS: 98 patients undergoing CABG were randomly assigned to intervention and placebo groups. The intervention group inhaled 5-drops of 20 % lavandula essential oil (LEO) and the placebo group was exposed to 5-drop of distilled water. LEO or distilled water were dropped into a sterile gauze converted to the form of a necklace. The subjects wore necklace for three consecutive days and intervention was performed each 24 h. The pain intensity, systolic blood pressure (SBP), and diastolic blood pressure (DBP) were measured before each intervention and 30 min after it. Also, the mean analgesic intake was recorded. SPSS version 16 was used to analyze the data. RESULTS: The mean pain score measured in the intervention group showed a more decrease than that obtained in the placebo group after the first and second interventions. Additionally, the mean pain score in the intervention group demonstrated a significant decrease than the placebo group after the second intervention (P=0.008). Moreover, mean SBP after the second intervention (P=0.046) and mean DBP after the first intervention (P=0.029) revealed a significant difference between two groups. Moreover, the intervention group received less analgesic than the placebo group. CONCLUSIONS: Lavandula aromatherapy can reduce pain and received analgesic dose after CABG.
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Manejo da Dor , Qualidade de Vida , Humanos , Ponte de Artéria Coronária , Dor , ÁguaRESUMO
Different gentian preparations are used as traditional remedies for internal pain control in: Persian traditional medicine (PTM), Chinese traditional medicine (CTM) and Ancient Greek medicine (AGM) from the time of the Roman Empire. Objective: To present a survey of the ethnopharmacological applications of gentians recorded as being used in Eastern and Western traditional medical systems (PTM, CTM and AGM) and their pharmacological effects, chemical composition as well as an in silico investigation of the possible active component/s for the alleviation of internal pain via molecular docking studies. Major traditional medicine literature (PTM, CTM and AGM, 50 AD- 1770) and ethnobotanical studies for the application of gentians were reviewed. Nine European species representing 5 of the 13 sections currently attributed to Gentiana were selected. Chemical compounds and pharmacological activity data of these species were gathered from different databases including Google Scholar, PubChem, PubMed and Web of Science (between 1972 and 2020). The possible active constituents of gentians on visceral pain receptors were investigated, in silico. In all investigated literature, traditional uses of gentian were indicated to have anti-nociceptive effects on visceral pain and possess diuretic action. According to our computational study, acylated flavonoid glycosides, viz. trans-feruloyl-2"-isovitexin (33), trans-feruloyl-2"-isovitexin-4'-O-ß-D-glucoside (34), iso-orientin-4'-O-glucoside (38), trans-caffeoyl-2"-iso-orientin-4'-O-ß-D-glucoside (39), iso-orientin-2"-O-ß-D-glucoside (40) and isoscoparin (41), might be responsible for visceral pain reduction by interacting with the purinergic receptor (P2X3) and vanilloid receptor 1 (TrpV1). This finding shows a good correlation with different traditional gentian uses in Persian, Chinese and European ethnomedicine for visceral pain control.
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Gentiana , Dor Visceral , Glucosídeos , Simulação de Acoplamento Molecular , FitoterapiaRESUMO
INTRODUCTION: Fibroblasts and fibroblast-like cells (FLCs) are highly distributed in the dermis layer of the skin and gastrointestinal tract. A few studies have investigated the effects of color additives of cosmetic products on human fibroblasts. Therefore, this in vitro study was conducted to investigate the effects of 9 synthetic and natural dyes (indigo carmine, carmine, sunset yellow, tropaeolin, acid green 25, chlorophyllin, tartrazine, lissamine, and amaranth) on human foreskin fibroblast cells. METHODS: MTT assay was applied to investigate the effects of dyes on human normal fibroblast cells. For investigating the possible mechanism of cytotoxicity, the effect of dyes was evaluated on parameters of cellular oxidative stress including lipid peroxidation and reactive oxygen species (ROS) as well as lactate dehydrogenase. RESULTS: In the MTT assay, a significant reduction (p ≤ 0.05) was observed in the viability of fibroblast cells by chlorophyllin and indigo carmine at concentrations higher than 10 and 100 (µg/ml), respectively. Acid green 25 caused a significant reduction at very high concentrations (1000 and 2000 µg/ml), which was not toxic. The effect of other investigated dyes was not significant on the fibroblasts. A trend in increased cell proliferation by amaranth and carmine was observed, but this enhancement was not statistically significant. No significant changes were observed in lipid peroxidation or lactate dehydrogenase. Chlorophyllin caused a significant increase in the production of cellular ROS. CONCLUSIONS: Indigo carmine and chlorophyllin had cytotoxicity on human fibroblasts, and thus, further studies are required on their safety of use in cosmetics and pharmaceuticals.
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Índigo Carmim , Tartrazina , Corante Amaranto , Antraquinonas , Carmim , Proliferação de Células , Clorofilídeos , Corantes , Fibroblastos , Prepúcio do Pênis , Humanos , Lactato Desidrogenases , Masculino , Estresse Oxidativo , Preparações Farmacêuticas , Espécies Reativas de OxigênioRESUMO
A new guaianolide sesquiterpene lactone with cytotoxic properties was isolated from Euphorbia microsphaera Boiss. To determine the highest active fraction and isolate bioactive compounds, a bioassay guided fractionation approach was used. The general toxicity properties of the plant's extracts and fractions (fr1-10) were assessed against Artemia salina, Oryzeaphilus mercator, and Tribolium castaneum. Cytotoxic activities were investigated against normal human foreskin fibroblasts and two malignant cell lines, including human breast cancer (MCF-7) and human fibrosarcoma cells (HT1080) using the MTT assay at different time points of 24, 48, and 72 h. Single crystal X-ray diffraction (SC-XRD) and mass spectrometry data were used to determine the structure of the active guaianolide sesquiterpene lactone (3aR,4S,4aS,5R,7aS,9aS)-5-hydroxy-5,8-dimethyl-3-methylene-2-oxo-2,3,3a,4,4a,5,6,7,7a, 9a decahydroazuleno [6,5-b] furan-4-yl acetate (named aryanin). Chloroformic fraction 7 (fr7, LC50 = 93.50 µg/mL for general toxicity) had the highest toxicity result, with a mortality rate of more than 50% for both insect species after 12 h at 15 mg/mL. The highest cytotoxicity of aryanin was observed on 24 h treated MCF-7 with an IC50 of 13.81 µg/mL. After 24 h, the inhibition of MCF-7 cell proliferation was 92%-94% at concentrations of 25-50 µg/mL, respectively. On MCF-7, the IC50 was found to be 49.35 µg/mL after 72 h. This compound had a considerable cytotoxicity (IC50 ≤ 12.5 µg/mL, 24 h) on human foreskin fibroblasts. In contrast to the MCF-7 cell line, the proliferation of human foreskin fibroblasts was increased after 72 h.
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Antineoplásicos Fitogênicos , Neoplasias da Mama , Euphorbia , Fibrossarcoma , Sesquiterpenos , Neoplasias da Mama/tratamento farmacológico , Feminino , Humanos , Lactonas , Células MCF-7RESUMO
Monitoring of toxic heavy metals in fish samples is a matter of a great importance from the nutritional and toxicological points of view. A dispersive micro solid phase extraction (dµSPE) for preconcentration of trace Pb, Cd, Hg, Co, Ni ions using pectin coated magnetic graphene oxide (pectin/Fe3O4/GO) is presented. Inductively coupled plasma optical emission spectroscopy (ICP/OES) was utilized for analyzing the samples. The influence of parameters name as pH, extraction time, sample volume and amount of sorbent were optimized using central composite design (CCD) methodology. Detection and quantification limits were between 0.01 and 0.21 µg g-1 and 0.04-0.67 µg g-1 of fresh fish sample, respectively. Accuracy of the method verified using certified reference materials (NIST-SRM-1946). Concentration of the toxic heavy metals were successfully determined in 11 different fish samples using the proposed method.
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Peixes/metabolismo , Metais Pesados/metabolismo , Microextração em Fase Sólida/métodos , Análise Espectral/métodos , Animais , Concentração de Íons de Hidrogênio , Limite de DetecçãoRESUMO
Aromatic herbal remedies, hydrosols, and essential oils are widely used for women's hormonal health. Scientific investigation of their major constituents may prevent unwanted infertility cases, fetal abnormalities, and drug-herb interactions. It also may lead to development of new medications. A list of 265 volatile molecules (mainly monoterpenes and sesquiterpenes) were prepared from a literature survey in Scopus and PubMed (2000-2019) on hydrosols and essential oils that are used for women's hormonal and reproductive health conditions. The PDB (protein data bank) files of the receptors (136 native PDB files) that involve with oxytocin, progesterone, estrogen, prolactin, acetyl choline, androgen, dopamine, human chorionic gonadotropin, luteinizing hormone, follicle-stimulating hormone, aromatase, and HER2 receptors were downloaded from Protein Data Bank. An in silico study using AutoDock 4.2 and Vina in parallel mode was performed to investigate possible interactions of the ligands with the receptors. Drug likeliness was investigated for the most active molecules using DruLiTo software. Aristola-1(10),8-diene, bergapten (5-methoxypsoralen), α-bergamotene, bicyclogermacrene, α-bisabolol oxide A, α-bisabolone oxide, p-cymen-8-ol, 10-epi elemol, α-elemol, ß-eudesmol, 7-epi-ß-eudesmol, ficusin, ß-humulene, methyl jasmonate, nerolidol, pinocarvone, (+)-spathulenol, and thujone had better interactions with some androgen, aromatase, estrogen, progesterone, HER2, AChR, and/or dopamine receptors. Most of these molecules had an acceptable drug likeliness except for α-bergamotene, bicyclogermacrene, ß-humulene, and aristola-1(10),8-diene. Some volatile natural molecules can be considered as lead compound for drug development to treat hormonal conditions.
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Doenças dos Genitais Femininos/tratamento farmacológico , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Receptores de Esteroides/efeitos dos fármacos , Sítios de Ligação , Feminino , Humanos , Ligantes , Simulação de Acoplamento Molecular , Estrutura MolecularRESUMO
The Scrophularia genus is a rich source of phenylethanoid glycosides, with diverse biological activities including anti-diabetic properties. This study investigated anti-type 2 diabetic potential and active component of Scrophularia flava Grau. A new phenylethanoid glycoside was isolated from aerial parts of the plant and identified as 2-(4-hydroxy-3-methoxyphenyl) ethyl 6-deoxy-3-O-[(2E)-3-(3 hydroxy-4-methoxyphenyl) prop-2-enoyl]-α-rhamnopyranosyl-(1 â 3)-[α-rhamnopyranosyl-(1 â 6)]-4-O-[(2E)-3-(4-hydroxy-3-methoxyphenyl) prop-2-enoyl]-ß-glucopyranoside. It was named flavaioside. The structure of flavaioside was identified based on 1H NMR, 13C NMR, DEPT-HSQC, COSY, HMBC, NOESY and LC-ESI-MS-MS. Total methanol extract, fractions (A-F) and specific main phenylethanoid glycoside (flavaioside), were assessed for inhibitory effects against the α-glucosidase enzyme (in vitro anti-type 2 diabetic assay). The antioxidant activities of methanol extracts, all fractions and isolated flavaioside were identified based on 2, 2'-diphenyl-1-picrylhydrazyl radical (DPPH) scavenging activity, 2, 2'-azino-bis (3-ethylbenzothiazoline)-6-sulphonic acid radical cation (ABTS+) scavenging activity, phosphomolybdenum method, and metal chelating activity. In comparison to the other fractions, the best antioxidant result was observed in fraction E and its main compound, flavaioside, in DPPH (IC50 = 4.26, 2.57 µg/mL) and ABTS+ (EC50 = 55.45, 6.34 µg/mL) scavenging activities. Flavaioside showed significantly stronger activities than α-tocopherol and ascorbic acid in DPPH and ABTS+ assays. Furthermore, flavaioside showed a potent inhibitory activity on the α-glucosidase enzyme which was comparable with the known anti-type 2 diabetic drug, acarbose (91.85%, and 92.87%, respectively). Fraction E and flavaioside showed α-glucosidase inhibitory activities with IC50 values, 65.05 and 6.50 µg/mL. The plant and its isolated flavaioside can possess acceptable anti-type 2 diabetic potential and anti-oxidant activity.
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Antioxidantes/farmacologia , Inibidores de Glicosídeo Hidrolases/farmacologia , Hipoglicemiantes/farmacologia , Scrophularia/química , alfa-Glucosidases/metabolismo , Antioxidantes/química , Antioxidantes/isolamento & purificação , Benzotiazóis/antagonistas & inibidores , Compostos de Bifenilo/antagonistas & inibidores , Relação Dose-Resposta a Droga , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Glicosídeos/química , Glicosídeos/isolamento & purificação , Glicosídeos/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Estrutura Molecular , Estresse Oxidativo/efeitos dos fármacos , Álcool Feniletílico/química , Álcool Feniletílico/isolamento & purificação , Álcool Feniletílico/farmacologia , Picratos/antagonistas & inibidores , Saccharomyces cerevisiae/enzimologia , Relação Estrutura-Atividade , Ácidos Sulfônicos/antagonistas & inibidores , Trissacarídeos/química , Trissacarídeos/isolamento & purificação , Trissacarídeos/farmacologiaRESUMO
Lately, it has been proved that yeast exopolysaccharides (EPS) are potentially applicable biopolymers, a fact that has led to incremental needs for their assessment. The current study is based on the biochemical and molecular level identification of the novel cold-adapted yeast Rhodotorula mucilaginosa sp. GUMS16. Possible antioxidant and antiproliferative activities, as well as extraction and characterization of the GUMS16-produced EPS, were assessed during the course of this study. The results indicated that the strain of GUMS16 is a cold-adapted yeast with growth capability at 4 °C and an approximate EPS production yield of 28.5 g/L which are characterized as highly branched beta-D-glucan having glucose and mannose residues (85:15 mol%, respectively) with an average molecular weight of 84 kDa. In comparison to hyaluronic acid, DPPH, and OH, the scavenging activity attributed to the GUMS16-produced EPS was higher alongside being dose-dependent. The biocompatibility profile of the EPS was well-recognized based on its zero-cytotoxicity rate on a normal cell model. Collectively, the favorable properties of the EPS accentuate their potential as biocompatible compound suitable for subsequent pharmaceutical and industrial applications.
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Adaptação Fisiológica , Temperatura Baixa , Polissacarídeos Fúngicos/biossíntese , Polissacarídeos Fúngicos/química , Polissacarídeos Fúngicos/farmacologia , Rhodotorula/química , Rhodotorula/metabolismo , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Fenômenos Químicos , Cromatografia Gasosa , Genótipo , Peso Molecular , Filogenia , Rhodotorula/classificação , Rhodotorula/genética , Solubilidade , Espectrometria de Massas por Ionização por ElectrosprayRESUMO
Halophytic plants growing in harsh desert environments are rich reservoirs of unique endophytic microorganisms. Here, healthy fresh plants of the families Tamaricaceae and Amarantaceae at three saline locations in Iran were investigated for their bioactive endophytic fungi. Among a vast number of isolates, eight isolates were identified as Humicola fuscoatra (Sordariomycetes, Pezizomycotina, Ascomycota) by microscopy and representative DNA sequences of the 5.8S rDNA (ITS) and partial ß-tubulin (TUB2). Those isolates were halotolerant, and highly bioactive, so that their intra- and extra-cellular metabolites possessed in vitro antifungal, antibacterial and antiproliferative activities, against a number of fungal and bacterial plant pathogens including the fungi Arthrobotrys conoides, Pyrenophora graminea, Pyricularia grisea and the bacteria Agrobacterium tumefaciens, Pseudomonas syringae and Xanthomonas oryzae. Chemical analyses of metabolites from the endophytes using HNMR, CNMR, NOESY, COSY, HMBC, HSQC, DEPT, TOCSY and EI MASS techniques identified 3,8-dihydroxy-1-methyl-9,10-anthracenedione (aloesaponarin II; an anthraquinone derivative), 1,8,9-anthracenetriol structure (chrysarobin; an anthranol derivative) and 2,4-di-tert-butylthiophenol in fungal extracts. To the best of our knowledge, this is the first report of endophytic association of halotolerant H. fuscoatra isolates with Tamaricaceae and Amarantaceae, and their bioactivity against plant pathogens. Also, the capability of chrysarobin and aloesaponarin II production is new to the fungal kingdom. These findings may find application in agriculture, pharmacology, and biotechnology.
Assuntos
Amaranthaceae/metabolismo , Ascomicetos/metabolismo , Tamaricaceae/microbiologia , Amaranthaceae/genética , Amaranthaceae/fisiologia , Antracenos/metabolismo , Antralina/metabolismo , Antraquinonas/metabolismo , Ascomicetos/genética , Ascomicetos/fisiologia , DNA Bacteriano/genética , DNA Ribossômico/genética , Plantas Tolerantes a Sal/metabolismo , Plantas Tolerantes a Sal/microbiologia , Tamaricaceae/metabolismoRESUMO
A straightforward and efficient method was developed by ultrasound assisted emulsification microextraction (USAEME) combined with inductively coupled plasma optical emission spectroscopy (ICP/OES) to trace some toxic heavy metal ions in eight select farmed and four select imported rice samples. In this study, carbon tetrachloride (CCl4) and 1-(2-pyridylazo)2-naphthol (PAN) were used as the extraction solvent and complexing reagent, respectively. The extraction parameters were optimized by means of a central composite design (CCD). Detection and quantification limits were set to be between 0.02 and 0.08⯵g L-1 and 0.07-0.30⯵g L-1, respectively. The accuracy of our method was further verified against two certified reference materials namely NCS ZC73029 and NIES No 10-b. While no trace of contaminations was found in some rice samples (Tarom, Hashemi, Sadri, Khazar and one imported sample), others such as Kazemi, Jamshidi, Dom Siah, Guilanehand and three of the imported samples were considerably polluted.
Assuntos
Metais Pesados/análise , Oryza/química , Espectrofotometria Atômica/métodos , Tetracloreto de Carbono/química , Limite de Detecção , Microextração em Fase Líquida , Metais Pesados/isolamento & purificação , Naftóis/química , Oryza/metabolismo , SonicaçãoRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: As a significant health issue, Functional Constipation (FC) has a high prevalence of 0.7%-29% worldwide. In Persian ethnomedicine, several formulations of sugarcane extracts including faniz, shekar-e- sorkh and black strap molasses have been used to treat pediatric constipation. AIM OF THE STUDY: To evaluate efficacy and safety of oral intake of black strap molasses syrup (BSM) on FC in children. MATERIALS AND METHODS: A randomized controlled double blinded trial was performed on children aged 4-12 years diagnosed with FC according to ROMIII Constipation Measurement Questionnaire. Ninety-two patients were randomly divided in two groups of BSM or PEG syrups (40%) with a dose of 1â¯mL/kg body weight/day for 1 month. Symptoms were evaluated every two weeks. Possible serological side-effects and changes in children's body weight were investigated. BSM syrup constituents were determined by pharmacognostic methods. RESULTS: Treatment was successful with both interventions with no significant difference between the groups. Defecation per week was significantly improved in both groups. Symptoms including volitional stool retention, large diameter stool, painful or hard stool and large fecal mass in the rectum decreased significantly two and four weeks after intervention (Pâ¯<â¯0.05). There was no significant difference between groups except for the rate of large diameter stool. No side -effects were observed. The BSM naturally contained polyphenols (960⯵g/mL), potassium (12430⯵g/mL), iron (80⯵g/mL) and calcium (3320⯵g/mL). CONCLUSION: BSM and PEG syrups had similar efficacy on FC. Compared with PEG, BSM syrup contained different natural micronutrients.
Assuntos
Constipação Intestinal/tratamento farmacológico , Melaço , Extratos Vegetais/uso terapêutico , Polietilenoglicóis/uso terapêutico , Saccharum , Administração Oral , Criança , Pré-Escolar , Método Duplo-Cego , Feminino , Humanos , Masculino , Resultado do TratamentoRESUMO
INTRODUCTION: In addition to the development of analytical equipment, another movement has also appeared in the field of computer assisted techniques for metabolite assessment. Although, some studies can be found in the literature there is still not available reliable and user-friendly software which is coupled with a simple chromatography method for developing a database to identify medicinal plants. OBJECTIVES: Developing a novel similarity search approach for high-performance thin-layer chromatography (HPTLC) fingerprinting. METHODS: Combined HPTLC with image analysis approach was used for similarity assessment of 70 standard medicinal plants. Ethyl acetate-ethyl methyl ketone-formic acid 98%-water (50:30:10:10) were chosen among different examined mobile phases. Liebermann-Burchard and anisaldehyde reagents were chosen for HPTLC derivatisation for visualisation. Image analysis based on Cannys' method was used to determine the spot size of each HPTLC image. A similarity search algorithm based on colour (RGB, HSV and Lab) information alone or together with retardation factor (Rf ) and spot size information calculated with the software was built to assess the fingerprinting of medicinal plants. RESULTS: The software was capable of calculating spots size and Rf values. It authenticated unknown samples based on comparing images information, spots size and/or Rf in the built database. Similarity values were 75-96% for the selected plants chromatograms with those of the same plant in the database. It presents better results than principal components analysis (PCA), classification and regression trees (CART) and partial least squares discriminant analysis (PLS-DA). CONCLUSION: The procedure paves the way for constructing a database of HPTLC images of medicinal plants.