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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
microRNAs (miRNAs) play a crucial role in brain growth and function. Hence, research on miRNA has the potential to reveal much about the etiology of neuropsychiatric diseases. Among these, schizophrenia (SZ) is a highly intricate and destructive neuropsychiatric ailment that has been thoroughly researched in the field of miRNA. Despite being a relatively recent area of study about miRNAs and SZ, this discipline has advanced enough to justify numerous reviews that summarize the findings from the past to the present. However, most reviews cannot cover all research, thus it is necessary to synthesize the large range of publications on this topic systematically and understandably. Consequently, this review aimed to provide evidence that miRNAs play a role in the pathophysiology and progression of SZ. They have also been investigated for their potential use as biomarkers and therapeutic targets.
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MicroRNAs , Esquizofrenia , Humanos , MicroRNAs/genética , MicroRNAs/metabolismo , Esquizofrenia/genética , Esquizofrenia/metabolismo , Biomarcadores , Encéfalo/metabolismo , Transdução de SinaisRESUMO
This study aims to investigate the phytoconstituents of the chloroform fraction of three Cystoseira spp. namely C. myrica, C. trinodis, and C. tamariscifolia using UPLC/ESI/MS technique. The results revealed the identification of 19, 20 and 11 metabolites in C. myrica, C. trinodis, and C. tamariscifolia, respectively mainly terpenoids, flavonoids, phenolic acids and fatty acids. Also, an in vitro antioxidant study using FRAP and DPPH assays was conducted where the chloroform fraction of C. trinodis displayed the highest antioxidant activity in both assays, which would be attributed to its highest total phenolics and total flavonoids. Besides, the investigation of COX-1, α-glucosidase and α-amylase inhibitory activities were performed. Regarding C. trinodis, it showed the strongest inhibitory activity towards COX-1. Moreover, it showed potent inhibitory activity towards α-glucosidase and α-amylase enzymes. According to the molecular docking studies, the major compounds characterised showed efficient binding to the active sites of the target enzymes.
Assuntos
Clorofórmio , alfa-Glucosidases , Simulação de Acoplamento Molecular , Cromatografia Líquida de Alta Pressão , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Antioxidantes/farmacologia , Antioxidantes/química , Flavonoides/química , alfa-AmilasesRESUMO
In this work, Tamarindus indica (T. indica)-loaded crosslinked poly(methyl methacrylate) (PMMA)/cellulose acetate (CA)/poly(ethylene oxide) (PEO) electrospun nanofibers were designed and fabricated for wound healing applications. T. indica is a plant extract that possesses antidiabetic, antimicrobial, antioxidant, antimalarial and wound healing properties. T. indica leaves extract of different concentrations were blended with a tuned composition of a matrix comprised of PMMA (10 %), CA (2 %) and PEO (1.5 %), and were electrospun to form smooth, dense and continuous nanofibers as illustrated by SEM investigation. In vitro evaluation of T. indica-loaded nanofibers on normal human skin fibroblasts (HBF4) revealed a high compatibility and low cytotoxicity. T. indica-loaded nanofibers significantly increased the healing activity of scratched HBF4 cells, as compared to the free plant extract, and the healing activity was significantly enhanced upon increasing the plant extract concentration. Moreover, T. indica-loaded nanofibers demonstrated significant antimicrobial activity in vitro against the tested microbes. In vivo, nanofibers resulted in a superior wound healing efficiency compared to the control untreated animals. Hence, engineered nanofibers loaded with potent phytochemicals could be exploited as an effective biocompatible and eco-friendly antimicrobial biomaterials and wound healing composites.
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Anti-Infecciosos , Celulose/análogos & derivados , Nanofibras , Tamarindus , Animais , Humanos , Polimetil Metacrilato/farmacologia , Nanofibras/química , Cicatrização , Anti-Infecciosos/farmacologia , Extratos Vegetais/química , Antibacterianos/farmacologiaRESUMO
BACKGROUND: The emergence of different viral infections calls for the development of new, effective, and safe antiviral drugs. Glycyrrhiza glabra is a well-known herbal remedy possessing antiviral properties. OBJECTIVE: The objective of our research was to evaluate the effectiveness of a newly developed combination of the probiotics Lactobacillus acidophilus and G. glabra root extract against two viral models, namely the DNA virus Herpes simplex virus-1 (HSV-1) and the RNA virus Vesicular Stomatitis Virus (VSV), with regards to their antiviral properties. METHODOLOGY: To examine the antiviral impacts of various treatments, we employed the MTT assay and real-time PCR methodology. RESULTS: The findings of our study indicate that the co-administration of L. acidophilus and G. glabra resulted in a significant improvement in the survival rate of Vero cells, while also leading to a reduction in the titers of Herpes Simplex Virus Type 1 (HSV-1) and Vesicular Stomatitis Virus (VSV) in comparison to cells that were not treated. Additionally, an investigation was conducted on glycyrrhizin, the primary constituent of G. glabra extract, utilizing molecular docking techniques. The results indicated that glycyrrhizin exhibited a greater binding energy score for HSV-1 polymerase (- 22.45 kcal/mol) and VSV nucleocapsid (- 19.77 kcal/mol) in comparison to the cocrystallized ligand (- 13.31 and - 11.44 kcal/mol, respectively). CONCLUSIONS: The combination of L. acidophilus and G. glabra extract can be used to develop a new, natural antiviral agent that is safe and effective.
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Glycyrrhiza , Herpes Simples , Herpesvirus Humano 1 , Probióticos , Estomatite Vesicular , Chlorocebus aethiops , Animais , Lactobacillus acidophilus , Antivirais/farmacologia , Ácido Glicirrízico , Simulação de Acoplamento Molecular , Células Vero , Extratos Vegetais/farmacologiaRESUMO
Glycyrrhiza glabra and Sophora japonica (Fabaceae) are well-known medicinal plants with valuable secondary metabolites and pharmacological properties. The flavonoid-rich fractions of G. glabra roots and S. japonica leaves were prepared using Diaion column chromatography, and the confirmation of flavonoid richness was confirmed using UPLC-ESI-MS profiling and total phenolics and flavonoids assays. UPLC-ESI-MS profiling of the flavonoid-rich fraction of G. glabra roots and S. japonica leaves resulted in the tentative identification of 32 and 23 compounds, respectively. Additionally, the wound healing potential of topical preparations of each fraction, individually and in combination (1:1) ointment and gel preparations, were investigated in vivo, supported by histopathological examinations and biomarker evaluations, as well as molecular docking studies for the major constituents. The topical application of G. glabra ointment and gel, S. japonica ointment and gel and combination preparations significantly increase the wound healing rate and the reduction of oxidative stress in the wound area via MDA reduction and the elevation of reduced GSH and SOD levels as compared to the wound and Nolaver®-treated groups. The molecular docking study revealed that that major compounds in G. glabra and S. japonica can efficiently bind to the active sites of three proteins related to wound healing: glycogen synthase kinase 3-ß (GSK3-ß), matrix metalloproteinases-8 (MMP-8) and nitric oxide synthase (iNOS). Consequently, G. glabra roots and S. japonica leaves may be a rich source of bioactive metabolites with antioxidant, anti-inflammatory and wound healing properties.
Assuntos
Flavonoides , Glycyrrhiza , Flavonoides/farmacologia , Flavonoides/análise , Sophora japonica , Simulação de Acoplamento Molecular , Quinase 3 da Glicogênio Sintase , Pomadas , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Glycyrrhiza/química , CicatrizaçãoRESUMO
The genus Moricandia (Brassicaceae) comprises about eight species that were used in traditional medicine. Moricandia sinaica is used to alleviate certain disorders such as syphilis and exhibits analgesic, anti-inflammatory, antipyretic, antioxidant, and antigenotoxic properties. Throughout this study, we aimed to figure out the chemical composition of lipophilic extract and essential oil obtained from M. sinaica aerial parts using GC/MS analysis, as well as their cytotoxic and antioxidant activities correlated with the major detected compounds' molecular docking. The results revealed that both the lipophilic extract and the oil were found to be rich in aliphatic hydrocarbons, accounting for 72.00% and 79.85%, respectively. Furthermore, the lipophilic extract's major constituents are octacosanol, γ-sitosterol, α-amyrin, ß-amyrin acetate, and α-tocopherol. Contrarily, monoterpenes and sesquiterpenes accounted for the majority of the essential oil. The essential oil and the lipophilic extract of M. sinaica showed cytotoxic properties towards human liver cancer cells (HepG2) with IC50 values of 126.65 and 220.21 µg/mL, respectively. The lipophilic extract revealed antioxidant activity in the DPPH assay with an IC50 value of 2679 ± 128.13 µg/mL and in the FRAP assay, moderate antioxidant potential was expressed as 44.30 ± 3.73 µM Trolox equivalent/mg sample. The molecular docking studies revealed that êµ-amyrin acetate, α -tocopherol, γ-sitosterol, and n-pentacosaneachieved the best docking scores for NADPH oxidase, phosphoinositide-3 kinase, and protein kinase B. Consequently, M. sinaica essential oil and lipophilic extract can be employed as a viable management strategy for oxidative stress conditions and the formulation of improved cytotoxic treatment regimens.
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Antineoplásicos , Óleos Voláteis , Humanos , Óleos Voláteis/química , Antioxidantes/química , Simulação de Acoplamento Molecular , Extratos VegetaisRESUMO
Culex pipiens mosquitoes are transmitters of many viruses and are associated with the transmission of many diseases, such as filariasis and avian malaria, that have a high rate of mortality. The current study draws attention to the larvicidal efficacy of three methanolic algal extracts, Cystoseira myrica, C. trinodis, and C. tamariscifolia, against the third larval instar of Cx. pipiens. The UPLC-ESI-MS analysis of three methanol fractions of algal samples led to the tentative characterization of twelve compounds with different percentages among the three samples belonging to phenolics and terpenoids. Probit analysis was used to calculate the lethal concentrations (LC50 and LC90). The highest level of toxicity was attained after treatment with C. myrica extract using a lethal concentration 50 (LC50) of 105.06 ppm, followed by C. trinodis (135.08 ppm), and the lowest level of toxicity was achieved by C. tamariscifolia (138.71 ppm) after 24 h. The elevation of glutathione-S-transferase (GST) and reduction of acetylcholine esterase (AChE) enzymes confirm the larvicidal activity of the three algal extracts. When compared to untreated larvae, all evaluated extracts revealed a significant reduction in protein, lipid, and carbohydrate contents, verifying their larvicidal effectiveness. To further support the observed activity, an in silico study for the identified compounds was carried out on the two tested enzymes. Results showed that the identified compounds and the tested enzymes had excellent binding affinities for each other. Overall, the current work suggests that the three algal extractions are a prospective source for the development of innovative, environmentally friendly larvicides.
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Aedes , Anopheles , Inseticidas , Animais , Estudos Prospectivos , Inseticidas/química , Compostos Fitoquímicos/análise , Metanol/química , Plantas , Larva , Extratos Vegetais/química , Folhas de Planta/químicaRESUMO
Myrtaceae is one of the most important plants families, being regarded as the eighth largest flowering plant family. It includes many genera of utmost ecological and economical importance distributed all over the world. This review aimed to report the latest studies on this family focusing on certain widely used plants including Eucalyptus sp., Eugenia sp. (Eugenia uniflora, Eugenia sulcata), Syzygium sp. (Syzygium aromaticum and Syzygium cumini), Psidium sp., Pimenta dioica, Myrtus sp. (Myrtus communis), Myrciaria sp. and Melaleuca alternifolia. The extraction of bioactive compounds has been evolving through the optimization of conventional methods and the use of emerging technologies. Supercritical CO2 was applied for essential oils and ultrasound for polyphenols leading to extracts and essential oils rich in bioactive compounds. Advances in the field of encapsulation and delivery systems showed promising results in the production of stable essential oils nanoemulsions and liposomes and the production of plant extracts in the form of nanoparticles. Moreover, a significant increase in the number of patents was noticed especially the application of Myrtaceae extracts in the pharrmacuetucal field. The applications of ceratin plants (Pimenta dioica, Melaleuca alternifolia, Syzygium aromaticum essential oils or Myrciaria cauliflora peel extract) in food area (either as a free or encapsulated form) also showed interesting results in limiting microbial spoilage of fresh meat and fish, slowing oxidative degradation in meat products, and inhibiting aflatoxin production in maize. Despite the massive literature on Myrtaceae plants, advances are still necessary to optimize the extraction with environmentally friendly technologies and carry out risk assessment studies should be accomplished to harness the full potential in food, industrial and pharmaceutical applications.
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Psidium guajava (Guava tree) is one of the most widely known species in the family Myrtaceae. The Guava tree has been reported for its potential antioxidant, anti-inflammatory, antimicrobial, and cytotoxic activities. In the current study, the chemical compositions of the n-hexane extract and the essential oil of P. guajava were investigated using the GC/MS analysis, along with an evaluation of their antioxidant potential, and an investigation into the enzyme inhibition of acetylcholinesterase (AChE), butyrylcholinesterase (BchE), tyrosinase, α-amylase, and α-glucosidase. Moreover, molecular docking of the major identified active sites of the target enzymes were investigated. The chemical characterization of the n-hexane extract and essential oil revealed that squalene (9.76%), α-tocopherol (8.53%), and γ-sitosterol (3.90%) are the major compounds in the n-hexane extract. In contrast, the major constituents of the essential oil are D-limonene (36.68%) and viridiflorol (9.68%). The n-hexane extract showed more antioxidant potential in the cupric reducing antioxidant capacity (CUPRAC), the ferric reducing power (FRAP), and the metal chelating ability (MCA) assays, equivalent to 70.80 ± 1.46 mg TE/g, 26.01 ± 0.97 mg TE/g, and 24.83 ± 0.35 mg EDTAE/g, respectively. In the phosphomolybdenum (PM) assay, the essential oil showed more antioxidant activity equivalent to 2.58 ± 0.14 mmol TE/g. The essential oil demonstrated a potent BChE and tyrosinase inhibitory ability at 6.85 ± 0.03 mg GALAE/g and 61.70 ± 3.21 mg KAE/g, respectively. The α-amylase, and α-glucosidase inhibitory activity of the n-hexane extract and the essential oil varied from 0.52 to 1.49 mmol ACAE/g. Additionally, the molecular docking study revealed that the major compounds achieved acceptable binding scores upon docking with the tested enzymes. Consequently, the P. guajava n-hexane extract and oil can be used as a promising candidate for the development of novel treatment strategies for oxidative stress, neurodegeneration, and diabetes mellitus diseases.
Assuntos
Óleos Voláteis , Psidium , Antioxidantes/química , Butirilcolinesterase/metabolismo , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Acetilcolinesterase/metabolismo , Simulação de Acoplamento Molecular , Monofenol Mono-Oxigenase , alfa-Glucosidases/metabolismo , Extratos Vegetais/farmacologia , Extratos Vegetais/química , alfa-AmilasesRESUMO
Ziziphus spina-christi L. (ZSC-L) is a tree with thorny branches, belongs to the family Rhamnaceae and grows in the sub-tropics. The purpose of this research is to isolate and partially purify bioactive components from the crude ethanol extract of the stem bark of ZSC-L. Besides, bioassay-guided fractionation of ZSC-L stem bark was conducted using different solvents. The solvents were reutilized to minimize the production cost and environmental harm. In addition, the antimicrobial activities of the fractions were analyzed, followed by metabolic profiling using LC-HRMS. The n-butanol fraction showed the highest antimicrobial efficacy, so it was subjected to further purification. For the first time, two major compounds were isolated from the stem bark of ZSC-L and identified as lupane-type pentacyclic triterpenoids betulinic acid and betulin. Both compounds were used as antibacterial and anticancer agents and considered as a green product as the extraction procedure reduced the use of hazardous chemicals. Metabolic characterization of ZSC-L and its bioactive fractions were performed using LC-HR-ESI-MS and the results revealed the dereplication of 36 compounds belonging to different chemical classes. Flavonoids and triterpenes were the most prominent metabolite classes in the different fractions. The molecular docking results were obtained by studying the interaction of betulin and betulinic acid with antimicrobial receptors (4UYM, 1IYL, 1AJ2, 6J7L, 1AD4, 2VEG) to support the in vitro results. Our study highlights that Ziziphus spina-christi and its phytoconstituents, especially triterpenoids, act as a promising antimicrobial candidate in pharmaceutical and clinical applications.
Assuntos
Anti-Infecciosos , Triterpenos , Ziziphus , Antibacterianos/análise , Antibacterianos/farmacologia , Anti-Infecciosos/análise , Anti-Infecciosos/farmacologia , Simulação de Acoplamento Molecular , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Casca de Planta/química , Triterpenos/análise , Triterpenos/farmacologia , Ziziphus/químicaRESUMO
BACKGROUND: Breast cancer is the most frequently diagnosed type of cancer in women, accounting for 2.1 million cases, and stands as the fifth leading cause of death. Several treatment strategies are available, such as surgical resection, radiation, hormonal therapy, and conventional chemotherapy; however, these are associated with severe adverse effects in the patients. OBJECTIVES: This review aims to summarize the different studies (in vitro, in vivo, and new patents) concerning the therapeutic potential of plant polyphenolics in the management of breast cancer, published in the period from January 2016 to January 2021. Moreover, this review will focus on the underlying mechanisms of action and molecular characteristics of these compounds. METHODS: The data of this review were collected from different scientific databases, such as Pub- Med, Science Direct, Google Scholarship, SciFinder, and Egyptian Knowledge Bank (EKB). RESULTS: During the period 2016-2021, in the in vitro studies, investigation on 52 compounds of polyphenolic nature with promising anti-breast cancer activity has been conducted, while 14 compounds have been reported via in vivo studies. Besides, about 15 compounds have been registered as patent drugs. Different mechanisms of action and molecular targets have been reported, providing a clarified basis and precise reflection of the anticancer properties of these compounds against breast cancer. CONCLUSION: Polyphenolics represent a comprehensive source of anticancer lead compounds against the progression of breast cancer invasion and metastasis.
Assuntos
Antineoplásicos , Neoplasias da Mama , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Neoplasias da Mama/tratamento farmacológico , Feminino , Humanos , Patentes como AssuntoRESUMO
Phytochemical investigation of Sophora secundiflora alkaloid fraction led to isolation of one new quinolizidine alkaloid (1) 13-methoxyanagyrine together with six known ones (2-7). The insecticidal activity of 70% methanol extract of leaves of S. secundiflora, S. tomentosa and the isolated alkaloids were assessed against 3rd instar larvae of Culex pipiens (Diptera: Culicidae) using different concentrations and mortality rate was recorded. Sophora tomentosa extract showed highest mortality rate with median lethal concentration LC50 3.11 ppm after 24 h and 0.66 ppm after 48 h and anagyrine (6) exhibited remarkably insecticidal activity with LC50 value of 3.42 ppm after 24 h of exposure. Additionally, cytotoxic activity of alkaloid fraction of S. secundiflora, S. tomentosa and isolated alkaloids was also studied using crystal violet assay against MCF-7 and HEPG-2 cell lines. Anagyrine (6) exhibited IC50 values of 27.3 ± 0.7 and 30.2 ± 0.9 µg/mL against MCF-7 and HEPG-2 cancer cells, respectively.
Assuntos
Alcaloides , Antineoplásicos , Culex , Culicidae , Inseticidas , Quinolizidinas , Sophora , Alcaloides/toxicidade , Animais , Antineoplásicos/farmacologia , Inseticidas/farmacologia , Larva , Extratos Vegetais/farmacologia , Sophora/químicaRESUMO
The chemical composition of the n-hexane extract of Tamarindus indica's various organs-bark, leaves, seeds, and fruits (TIB, TIL, TIS, TIF)-was investigated using gas chromatography-mass spectrometry (GC/MS) analysis. A total of 113 metabolites were identified, accounting for 93.07, 83.17, 84.05, and 85.08 % of the total identified components in TIB, TIL, TIS, and TIF, respectively. Lupeol was the most predominant component in TIB and TIL, accounting for 23.61 and 22.78%, respectively. However, n-Docosanoic acid (10.49%) and methyl tricosanoate (7.09%) were present in a high percentage in TIS. However, α-terpinyl acetate (7.36%) and α-muurolene (7.52%) were the major components of TIF n-hexane extract. By applying a principal component analysis (PCA) and hierarchal cluster analysis (HCA) to GC/MS-based metabolites, a clear differentiation of Tamarindus indica organs was achieved. The anti-inflammatory activity was evaluated in vitro on lipopolysaccharide (LPS)-induced RAW 264.7 macrophages. In addition, the wound healing potential for the n-hexane extract of various plant organs was assessed using the in-vitro wound scratch assay using Human Skin Fibroblast cells. The tested extracts showed considerable anti-inflammatory and wound-healing activities. At a concentration of 10 µg/mL, TIL showed the highest nitric oxide (NO) inhibition by 53.97 ± 5.89%. Regarding the wound healing potential, after 24 h, TIB, TIL, TIS, and TIF n-hexane extracts at 10 g/mL reduced the wound width to 1.09 ± 0.04, 1.12 ± 0.18, 1.09 ± 0.28, and 1.41 ± 0.35 mm, respectively, as compared to the control cells (1.37 ± 0.15 mm). These findings showed that the n-hexane extract of T. indica enhanced wound healing by promoting fibroblast migration. Additionally, a docking study was conducted to assess the major identified phytoconstituents' affinity for binding to glycogen synthase kinase 3-ß (GSK3-ß), matrix metalloproteinases-8 (MMP-8), and nitric oxide synthase (iNOS). Lupeol showed the most favourable binding affinity to GSK3-ß and iNOS, equal to -12.5 and -13.7 Kcal/mol, respectively, while methyl tricosanoate showed the highest binding affinity with MMP-8 equal to -13.1 Kcal/mol. Accordingly, the n-hexane extract of T. indica's various organs can be considered a good candidate for the management of wound healing and inflammatory conditions.
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Syzygium cumini (Pomposia) is a well-known aromatic plant belonging to the family Myrtaceae, and has been reported for its various traditional and pharmacological potentials, such as its antioxidant, antimicrobial, anti-inflammatory, and antidiarrheal properties. The chemical composition of the leaf essential oil via gas chromatography-mass spectrometry (GC/MS) analysis revealed the identification of fifty-three compounds representing about 91.22% of the total oil. The identified oil was predominated by α-pinene (21.09%), followed by ß-(E)-ocimene (11.80%), D-limonene (8.08%), ß-pinene (7.33%), and α-terpineol (5.38%). The tested oil revealed a moderate cytotoxic effect against human liver cancer cells (HepG2) with an IC50 value of 38.15 ± 2.09 µg/mL. In addition, it effectively inhibited acetylcholinesterase with an IC50 value of 32.9 ± 2.1 µg/mL. Furthermore, it showed inhibitory properties against α-amylase and α-glucosidase with IC50 values of 57.80 ± 3.30 and 274.03 ± 12.37 µg/mL, respectively. The molecular docking studies revealed that (E)-ß-caryophyllene, one of the major compounds, achieved the best docking scores of -6.75, -5.61, and -7.75 for acetylcholinesterase, α-amylase, and α-glucosidase, respectively. Thus, it is concluded that S. cumini oil should be considered as a food supplement for the elderly to enhance memory performance and for diabetic patients to control blood glucose.
Assuntos
Inibidores de Glicosídeo Hidrolases/química , Simulação de Acoplamento Molecular , Óleos Voláteis/química , Syzygium/química , alfa-Glucosidases/química , Egito , Inibidores de Glicosídeo Hidrolases/farmacologia , Células Hep G2 , Humanos , Óleos Voláteis/farmacologia , Folhas de Planta , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/químicaRESUMO
Five flavonoids were isolated from the ethyl acetate fraction of leaves of Sophora secundiflora; formononetin (1), 5-hydroxy-4'-methoxyflavone (2), genistein (3), 5-hydroxy-8-(1-hydroxy-1-methyl-ethyl)-2-(4-hydroxyphenyl)-4H-furo-[2, 3-h]-chromen-4-one (4) and ononin (5). Additionally, LC-ESI-MS/MS analysis of the ethyl acetate fraction of S. secundiflora leaves had led to tentative identification of eighteen compounds. Formononetin, S. tomentosa and S. secundiflora leaves methanolic extract were evaluated in vivo for their neuroprotective activity where formononetin and S. tomentosa showed promising neuroprotective activity with reduction in acetylcholine esterase (AchE) enzyme activity and elevation of acetylcholine (Ach) and glutathione(GSH) brain levels and attenuation of dopamine (DA), nor-adrenaline (NA) and malonedialdehyde (MDA) brain level significantly, However S. secundiflora leaves methanolic extract didn't attenuate the AchE enzyme activity, DA and NA brain levels.
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Demência , Fármacos Neuroprotetores , Sophora , Isoflavonas , Fármacos Neuroprotetores/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta , Escopolamina , Espectrometria de Massas em TandemRESUMO
BACKGROUND: The genus Sophora (Fabaceae) represents one of the important medicinal plant genera regarding its chemical constituents and outstanding pharmacological activities. PURPOSE: In this review, we surveyed the latest findings on the bioactivities of different Sophora extracts and isolated phytochemicals during the past 8 years (2011-2019) updating the latest review article in 2011. The aim of this review is to focus on the molecular pharmacology of Sophora species to provide the rationale basis for the development of novel drugs. RESULTS: Sophora and its bioactive compounds possess outstanding pharmacological properties, especially as anticancer and anti-inflammatory drugs, in addition to its antioxidant, antibacterial, antifungal and antiviral properties. CONCLUSION: Based on their use in traditional medicine, Sophora species exert a plethora of cellular and molecular activities, which render them as attractive candidates for rationale drug development. Randomized, placebo-controlled clinical trials are required for further integration of Sophora-based phototherapies into conventional medicine.