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1.
J Ethnopharmacol ; 300: 115738, 2023 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-36165961

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: The bark of Matayba oppositifolia (A. Rich.) Britton (commonly known as "huaya" or "palo huacax") is commonly utilized in traditional Mayan medicine for treating diarrhea and for canker and other sores. AIM OF THE STUDY: The aim of this study was to investigate the in-vitro antimicrobial activity of M. oppositifolia bark extracts against drug-susceptible and -resistant ESKAPE-E pathogens. In addition, the phytochemical composition of the best antibacterial extract was analyzed. MATERIALS AND METHODS: The bark extracts were prepared with different solvents, including water, n-hexane, ethyl acetate and methanol. These were tested against ESKAPE-E (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa and Enterobacter spp., including Escherichia coli) strains using Resazurin Microtiter Assay. In addition, the composition of the most active extract was analyzed by GC-MS. RESULTS: The aqueous and organic bark extracts showed activity on drug-susceptible and -resistant ESKAPE-E microbes (MIC = 1000-31.25 µg/mL). The n-hexane bark extract was more active against the superbugs carbapenem-resistant K. pneumoniae (MIC = 500-31.25 µg/mL) and A. baumannii (MIC = 250-125 µg/mL). The GC-MS analysis of this extract allowed the identification of 12 phytochemicals as the potential antibacterial compounds. The major compounds identified were palmitic acid (1), friedelan-3-one (2) and 7-dehydrodiosgenin (3). CONCLUSION: The present study reveals the strong in-vitro antibacterial activity of the n-hexane extract from the bark of M. oppositifolia and demonstrates the potential of natural products as a source of antibacterial compounds or phytomedicines that are specifically effective against drug-resistant ESKAPE-E bugs. Additionally, our investigation contributes to the ethnopharmacological knowledge and reappraisal of Mayan medicinal flora, as well as supports the traditional use of the bark of the medicinal plant M. oppositifolia for the treatment of infectious diseases.


Assuntos
Antibacterianos , Plantas Medicinais , Antibacterianos/química , Antibacterianos/farmacologia , Bactérias , Carbapenêmicos/farmacologia , Escherichia coli , Hexanos , Klebsiella pneumoniae , Metanol/farmacologia , Testes de Sensibilidade Microbiana , Ácido Palmítico , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Sapindaceae , Solventes/farmacologia , Água/farmacologia
2.
Cells ; 11(21)2022 Oct 27.
Artigo em Inglês | MEDLINE | ID: mdl-36359799

RESUMO

Bee bread has numerous nutritional benefits and bioactive compounds. Other bee byproducts have been used as extender additives to improve semen cryopreservation. Here, we examined the effects of supplementing egg yolk extender (EYE) or soybean lecithin extender (SBLE) with bee bread extract (BBE) on the quality of cryopreserved ram semen. Semen was collected from five adult Rahmani rams once a week for 7 weeks. EYE and SBLE were supplemented with BBE. Antioxidant capacity and total phenolic compound, total flavonoid compound, and total soluble carbohydrate levels of BBE were measured. Sperm characteristics, including progressive motility, viability, abnormalities, membrane integrity, and acrosome integrity, were analyzed after equilibration, thawing, and thawing followed by a 2-h incubation. The total antioxidant capacity and malondialdehyde, hydrogen peroxide, aspartate transaminase, alanine transaminase, alkaline phosphatase, and total acid phosphatase levels in extenders were determined after thawing. Sperm apoptosis was analyzed using annexin V assays. SBLE was more effective than EYE for cryopreserving ram semen. Extender supplementation with BBE improved ram semen quality during freezing in a concentration-dependent pattern. Motility, vitality, and membrane integrity were particularly enhanced in BBE-treated semen. Additionally, BBE promoted antioxidant and enzymatic activities and reduced apoptosis in semen. Thus, extender supplementation with BBE improved sperm cryopreservation.


Assuntos
Própole , Preservação do Sêmen , Masculino , Animais , Lecitinas/farmacologia , Gema de Ovo , Soja , Própole/farmacologia , Crioprotetores/farmacologia , Análise do Sêmen , Motilidade Espermática , Antioxidantes/farmacologia , Metanol/farmacologia , Sementes , Criopreservação , Suplementos Nutricionais
3.
Trop Anim Health Prod ; 54(6): 344, 2022 Oct 13.
Artigo em Inglês | MEDLINE | ID: mdl-36227373

RESUMO

To increase rams' post-thaw semen quality following cryopreservation, this study used enriched Tris-based diluent with varying amounts of moringa leaf methanolic extract (MLME). The antioxidant activity, total phenolic, and total flavonoid content were all assessed in MLME. The sperm of five healthy Awassi rams were collected, divided into 4 equal aliquots, and diluted [1:5; (v/v)] in Tris-citrate-glucose extender supplemented with 0.48, 0.56, and 0.64 mg MLME/ml or without MLME supplementation (control). The percentages of sperm total motility (STM, %), sperm progressive motility (SPM, %) and viability (V, %), abnormal morphology (AM, %), membrane functional integrity (MFI, %), and acrosome integrity (AI %) were measured. Malondialdehyde (MDA), nitric oxide (NO), ascorbic acid (AA), superoxide dismutase (SOD), glutathione peroxidase (GPx), total cholesterol (TC), low-density lipoproteins (LDL), lactate dehydrogenase (LDH), alkaline phosphatase (ALP), zinc (Zn), and copper (Cu) were measured. The total phenolic gallic acid and flavonoid catechin (equivalent) contents were 19.78 mg/g and 11.94 mg/g, respectively. 2,2-Diphenyl-1-picrylhydrazyl (34.37 mM TE/g) and 2,2'-azino-bis/3-ethylbenzothiazoline-6-sulfonic acid (53.47 mM TE/g) were found in MLME. MLME had a 64.59 mM TE/g ferric-reducing power. In comparison to control, the addition of 0.64 mg/ml MLME to Tris-based extender resulted in the highest (P < 0.001) STM (55.22 ± 0.98), SPM (45.41 ± .70), SV (60.01 ± 1.05), MFI (75.23 ± 0.77), and AI (73.13 ± 0.72) and the lowest (P < 0.001) AM (21.34 ± 0.72) values. In comparison to the control, the addition of 0.56 mg/ml semen extender resulted in lower STM, SPM, SV, MFI, and AI with higher AM percentages. MDA (P = 0.03), NO (P = 0.012), CHO (P = 0.0001), and LDL (P = 0.004) were reduced by 0.64 mg/ml MLME, while AA (P = 0.017) and SOD (P = 0.0001) were elevated. In conclusion, the highest copper (P = 0.006) and lowest zinc concentrations in MLME (0.48 mg/ml extender) deteriorated the post-thaw semen quality, prompting us to suggest the addition of 0.64 mg MLME to rams' Tris-based semen extender.


Assuntos
Catequina , Moringa , Preservação do Sêmen , Fosfatase Alcalina , Animais , Antioxidantes/farmacologia , Ácido Ascórbico/farmacologia , Catequina/farmacologia , Colesterol , Citratos/farmacologia , Cobre , Criopreservação/veterinária , Crioprotetores/farmacologia , Suplementos Nutricionais , Ácido Gálico/farmacologia , Glucose/farmacologia , Glutationa Peroxidase , Lactato Desidrogenases , Lipoproteínas LDL/farmacologia , Masculino , Malondialdeído , Metanol/farmacologia , Óxido Nítrico , Oxidantes , Folhas de Planta , Sementes , Análise do Sêmen/veterinária , Preservação do Sêmen/métodos , Preservação do Sêmen/veterinária , Ovinos , Espermatozoides , Ácidos Sulfônicos/farmacologia , Superóxido Dismutase , Zinco/farmacologia
4.
An Acad Bras Cienc ; 94(4): e20210145, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36228215

RESUMO

This study evaluated some biological activities of extracts from Abuta selloana. The gastroprotective potential was determined against ethanol/HCl- and indomethacin-induced gastric ulcers, whereas the antinociceptive effect was evaluated by acetic acid-induced abdominal contortions in mice. The cytotoxicity activity was measured against human cancer cell lines: U251 (glioma), MCF-7 (breast cancer) and NCI-H460 (lung cancer). The radical scavenger potential was verified; and preliminary phytochemical analyses were performed. The phytochemical screening revealed higher levels of phenolic compounds in all extracts. Moreover, the methanolic extract from pulp fruit (MEPu), peel fruit (MEPe), branches (MEB) and leaves (MEL) scavenged the DPPH radical at 100 µg/mL. Besides, only MEL presented GI50 < 30 µg/mL in all tested cells. Besides, MEPu, MEPe, MEB or MEL at 10 mg/kg (i.p) reduced the abdominal contortions at 47.22%, 63.31%, 84.59% and 37.76%, respectively. The MEPu, MEPe, MEB and MEL reduced the ethanol/HCl- and indomethacin- induced ulcer at 250 mg/kg (p.o). In conclusion, A. selloana had interesting biological activities; presenting the leaves as a promising source for compounds with cytotoxic potential, however, further studies should be performed to confirm its antitumoral activity. Besides, the whole plant can be an important source of bioactive compounds associated with gastroprotective and antinociceptive properties.


Assuntos
Antiulcerosos , Frutas , Analgésicos/farmacologia , Animais , Brasil , Etanol/farmacologia , Frutas/química , Mucosa Gástrica , Humanos , Indometacina/análise , Indometacina/farmacologia , Metanol/análise , Metanol/química , Metanol/farmacologia , Camundongos , Compostos Fitoquímicos/análise , Fitoterapia , Extratos Vegetais/química , Folhas de Planta
5.
Exp Parasitol ; 242: 108401, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-36209935

RESUMO

The purpose of the present study was to assay the in vitro and in vivo anthelmintic activity (AA) of Caesalpinia coriaria (Cc) mature fruits against the nematode Haemonchus contortus (Hc). The Hc infective larvae were used to assess the in vitro AA through larval mortality assay. The exposure of larvae to the different treatments was performed in 96-well microtitration plates. The treatments were as follows: hydroalcoholic extract (HA-E, at 25-100 mg/mL), aqueous fraction (Aq-F, at 12.5-50 mg/mL), organic fraction (EtOAc-F at 12.5-50 mg/mL), compounds (1, methyl gallate and 2, gallic acid at 1.25-10 mg/mL), positive control (ivermectin at 5 mg/mL) and two negative controls (distilled water and 4% methanol). After exposure, dead and live larvae were quantified and results were compared to their controls. The in vivo assay was carried out by a faecal egg count reduction test (FECRT); artificially infected goat kids (F1: Boer x Nubia) were treated with Cc ground dried fruits to assess the AA. The treatments were established as follows: G1-untreated goats (negative control), G2-goats dewormed with ivermectin (positive control), G3-goats fed with Cc mature fruits (10% of their diet). Results in both in vitro and in vivo assays were analysed using an ANOVA through random design, applying a general linear model and mixed models. The in vitro results showed an evident larvicidal effect of the HA-E, EtOAc-F from Cc, indicating that the compound responsible for the AA was gallic acid. The results of the in vivo study corroborated the anthelmintic properties of Cc, reaching 78.6% reduction in the elimination of Hc eggs per gram of faeces. This plant represents a potential natural anthelmintic for the control of haemonchosis in goats under grazing conditions. Future studies should standardise the Cc extract or dried fruits for use in the management of nematodiasis in goat herds.


Assuntos
Anti-Helmínticos , Caesalpinia , Doenças das Cabras , Hemoncose , Haemonchus , Infecções por Nematoides , Animais , Hemoncose/tratamento farmacológico , Hemoncose/veterinária , Frutas , Ivermectina/farmacologia , Metanol/farmacologia , Metanol/uso terapêutico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Anti-Helmínticos/farmacologia , Anti-Helmínticos/uso terapêutico , Infecções por Nematoides/tratamento farmacológico , Ácido Gálico/farmacologia , Ácido Gálico/uso terapêutico , Cabras , Água , Doenças das Cabras/tratamento farmacológico , Contagem de Ovos de Parasitas/veterinária
6.
Life Sci ; 309: 121044, 2022 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-36208657

RESUMO

The present study attempted to scrutinize the protective effect of the methanolic extract of P. chaba stem bark against paracetamol-induced hepatotoxicity in Sprague-Dawley rats, along with the gas chromatography-mass spectrometry (GC-MS) analysis to identify phytochemicals, which were further docked in the catalytic site of CYP2E1 and the MD simulation for system that plays a major role in the bio-activation of toxic substances that produce reactive metabolites, leading to hepatotoxicity. P. chaba stem methanol extract (250 and 500 mg/kg) were treated orally with the negative control and the negative control silymarin (50 mg/kg) groups. Phytochemical profiling was conducted using GC-MS. In in-silico studies, PyRx software was used for docking analysis and the stability of the binding mode in the target active sites was evaluated through a set of standard MD-simulation protocols using the Charmm 27 force field and Swiss PARAM. Co-administration of P. chaba at both doses with APAP significantly reduced the APAP-augmented liver marker enzymes ALT, AST, ALP, and LDH, along with serum albumin, globulin, hepatic enzymes, histopathological architecture, lipid profiles, total protein, and total bilirubin, and elevated the levels of MDA. The GC-MS analysis indicated that P. chaba extract is enriched in fatty acid methyl esters (46.23 %) and alkaloids (10.91 %) and piperine is represented as a main phytochemical. Among all the identified phytochemicals, piperine (-8.0 kcal/mol) was found to be more interacting and stable with the binding site of CYP2E1. Therefore, all of our findings may conclude that the P. chaba stem extract and its main compound, piperine, are able to neutralize APAP-induced hepatic damage.


Assuntos
Alcaloides , Doença Hepática Induzida por Substâncias e Drogas , Piper , Silimarina , Ratos , Animais , Acetaminofen/toxicidade , Ratos Sprague-Dawley , Citocromo P-450 CYP2E1 , Cromatografia Gasosa-Espectrometria de Massas , Doença Hepática Induzida por Substâncias e Drogas/patologia , Metanol/farmacologia , Casca de Planta , Extratos Vegetais/uso terapêutico , Fígado , Alcaloides/farmacologia , Silimarina/farmacologia , Bilirrubina , Lipídeos/farmacologia , Ácidos Graxos , Albumina Sérica , Ésteres/farmacologia
7.
Malar J ; 21(1): 295, 2022 Oct 21.
Artigo em Inglês | MEDLINE | ID: mdl-36271447

RESUMO

BACKGROUND: The use of synthetic insecticides against mosquitoes may lead to resistance development and potential health hazards in humans and the environment. Consequently, a paradigm needs to shift towards the alternative use of botanical insecticides that could strengthen an insecticide resistance management programme. This study aimed to assess the insecticidal effects aqueous, hexane, and methanol crude leaf extracts of Calpurnia aurea, Momordica foetida, and Zehneria scabra on an insectary colony of Anopheles stephensi larvae and adults. METHODS: Fresh leaves of C. aurea, M. foetida and Z. scabra were collected and dried, then separately ground to powder. Powdered leaves of test plants were extracted using sonication with aqueous, hexane, and methanol solvents. The extracts were concentrated, and a stock solution was prepared. For comparison, Temephos (Abate®) and control solutions (a mixture of water and emulsifier) were used as the positive and negative controls, respectively. Different test concentrations for the larvae and the adults were prepared and tested according to WHO (2005) and CDC (2010) guidelines to determine lethal concentration (LC) values. Mortality was observed after 24 h exposure. The statistical analyses were performed using Statistical Package for the Social Sciences (SPSS) software (Kruskal-Wallis test) and R software (a generalized linear model was used to determine LC50 and LC90 values of the extracts). RESULTS: The lowest LC50 values were observed in aqueous extracts of M. foetida followed by Z. scabra extract and C. aurea leaves at 34.61, 35.85, and 38.69 ppm, respectively, against the larvae. Larval mortality was not observed from the hexane extracts and negative control, while the standard larvicide (temephos) achieved 100% mortality. Further, the adulticidal efficacy was greatest for aqueous extract of Z. scabra with LC50 = 176.20 ppm followed by aqueous extract of C. aurea (LC50 = 297.75 ppm). CONCLUSION: The results suggest that the leaf extracts of the three test plants have the potential of being used for the control of vector An. stephensi larvae and adult instead of synthetic mosquitocides. Further studies need to be conducted to identify the active ingredients and their mode of action.


Assuntos
Aedes , Anopheles , Culex , Culicidae , Inseticidas , Humanos , Animais , Inseticidas/farmacologia , Hexanos/farmacologia , Temefós/farmacologia , Metanol/farmacologia , Pós/farmacologia , Mosquitos Vetores , Larva , Extratos Vegetais/farmacologia , Solventes/farmacologia , Água , Folhas de Planta
8.
Toxicon ; 218: 57-65, 2022 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-36113683

RESUMO

Rhinella marina toad is abundant in Brazil. Its poison contains cardiac glycosides called bufadienolides, which are extensively investigated for their bioactivity. Our aim was to characterize the vasoactivity of Rhinella marina poison (RmP) on the aorta of male Wistar rats. For this, the RmP was first collected and processed to obtain an alcoholic extract. To determine cardiovascular effects of RmP, we performed in vivo tests by administering RmP intravenously in doses of 0.1-0.8 mg/kg. Vascular reactivity was also performed through concentration-response curves to RmP (10 ng/mL to 200 µg/mL) in aortic segments with and without endothelium. RmP induced a concentration-dependent contraction in rat aorta which was partly endothelium-mediated. Nitric oxide contributes with this response in view that incubation with L-NAME increased the contractile response. Additionally, treatment with indomethacin [cyclooxygenase, (COX) inhibitor], nifedipine (L-type voltage-gated calcium channels blocker), and BQ-123 (ETA receptors antagonist) decreased maximum response, and ketanserin (5-HT2 receptors antagonist) decreased pEC50, suggesting active participation of these pathways in the contractile response. On the other hand, apocynin (NADPH oxidase inhibitor) did not alter contractility. Incubation with prazosin (α1-adrenergic receptor antagonist) abolished the contractile response, suggesting that the RmP-induced contraction is dependent on the adrenergic pathway. In the Na+/K+ ATPase protocol, a higher Emax was observed in the RmP experimental group, suggesting that RmP potentiated Na+/K+ATPase hyperpolarizing response. When this extract was injected (i.v.) in vivo, increase in blood pressure and decrease in heart rate were observed. The results were immediate and transitory, and occurred in a dose-dependent manner. Overall, these data suggest that the poison extract of R. marina toad has an important vasoconstrictor action and subsequent vasopressor effects, and its use can be investigated to some cardiovascular disorders.


Assuntos
Bufanolídeos , Venenos , Adenosina Trifosfatases/metabolismo , Adenosina Trifosfatases/farmacologia , Adrenérgicos/farmacologia , Antagonistas Adrenérgicos/farmacologia , Animais , Bufanolídeos/toxicidade , Bufo marinus/metabolismo , Canais de Cálcio , Endotélio Vascular , Hemodinâmica , Indometacina/farmacologia , Ketanserina/farmacologia , Masculino , Metanol/farmacologia , NADPH Oxidases , NG-Nitroarginina Metil Éster , Nifedipino/farmacologia , Óxido Nítrico/metabolismo , Prazosina/farmacologia , Prostaglandina-Endoperóxido Sintases/metabolismo , Ratos , Ratos Wistar , Serotonina/farmacologia , Vasoconstritores
9.
BMC Complement Med Ther ; 22(1): 239, 2022 Sep 10.
Artigo em Inglês | MEDLINE | ID: mdl-36088372

RESUMO

BACKGROUND: Cervical cancer remains one of the significant causes of mortality in women due to the limitations of current treatment strategies and their associated side effects. Investigation of alternative medicine, including phytomedicine, has shown effective anti-cancer potential with fewer side effects. Azadirachta indica (commonly known as neem) is known for its medicinal properties. The present study investigated the anti-cancer potential of methanolic neem stem bark extract (MNBE) against cervical cancer using HeLa, SiHa, and ME-180 cell lines. METHODS: Cytotoxic effect of MNBE on cultured cell lines was evaluated by MTT and clonogenic assay. The growth-inhibiting effect of MNBE was further confirmed by performing cell cycle analysis and apoptosis assay using flow cytometry. The anti-migratory effect of MNBE was evaluated by using wound healing and Boyden chamber assay. Real-time PCR was used to determine the mRNA expression, and western blot and flow cytometry was used to determine the protein levels of growth and migration-related genes. RESULTS: MNBE significantly suppressed the growth and survival of cervical cancer cells in a dose-dependent manner by inducing cell cycle arrest and apoptosis. In addition, the growth inhibitory effect of MNBE was specific to cervical cancer cells than normal cells. Cell cycle arrest was correlated to transcriptional downregulation of cyclin dependent kinase 1 (CDK1), cyclin A, and cyclin B. Additionally, MNBE treatment resulted in the upregulation of active caspase-3 protein and downregulation of prosurvival genes, Bcl2, and survivin at mRNA level and NFkB-p65 at the protein level. Furthermore, MNBE inhibited the migration of cervical cancer cells accompanied by modulation of migration-related genes, including zona occludens-1 (ZO-1), matrix metalloproteinase 2 (MMP2), focal adhesion kinase (FAK), N-cadherin, snail, and E-cadherin. CONCLUSION: In summary, the present study provides the first evidence of MNBE in restricting cervical cancer cell growth and migration, which warrants further investigation for developing novel anti-cancer drugs.


Assuntos
Azadirachta , Neoplasias do Colo do Útero , Apoptose , Pontos de Checagem do Ciclo Celular , Feminino , Humanos , Metaloproteinase 2 da Matriz/metabolismo , Metaloproteinase 2 da Matriz/farmacologia , Metanol/farmacologia , Metanol/uso terapêutico , Casca de Planta , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , RNA Mensageiro , Neoplasias do Colo do Útero/tratamento farmacológico , Neoplasias do Colo do Útero/genética , Neoplasias do Colo do Útero/metabolismo
10.
Bioresour Technol ; 363: 127893, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-36067897

RESUMO

In this study, Caulerpa racemosa oil was used to produce biodiesel by recombinant Pichia pastoris displaying bound (rPp-BL) and secretory lipase (rPp-SL). Collected algae was pre-treated using ultrasonication, microwave and solvent extraction. Defatted C. racemosa was subjected to dilute acid treatment to obtain algal biomass hydrolysate. Both rPp-BL and rPp-SL were cultivated in algal biomass hydrolysate and glycerol. Surfactant treatment was performed on rPp-BL. Screening and optimization of variables were performed for biodiesel production using Plackett Burman design and central composite design, respectively. About 10.64 % (w/w) of algal oil was extracted from C. racemosa. Both rPp-BL and rPp-SL effectively utilized C. racemosa biomass hydrolysate and glycerol. rPp-SL combined with triton X (1.0 % w/v) treated rPp-BL for 3 min improved lipase activity. Methanol to oil ratio, combined whole cell biocatalyst and temperature were significant factors. Under optimum conditions, biodiesel yield reached about 93.64 % after 30 h using developed whole cell biocatalyst.


Assuntos
Biocombustíveis , Caulerpa , Candida/metabolismo , Caulerpa/metabolismo , Glicerol/metabolismo , Lipase/metabolismo , Metanol/metabolismo , Metanol/farmacologia , Pichia/genética , Pichia/metabolismo , Saccharomycetales , Solventes/metabolismo , Tensoativos/metabolismo
11.
Biomed Pharmacother ; 155: 113734, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-36152408

RESUMO

Oxidative stress and chronic inflammation are closely linked to various diseases. However, previous studies have demonstrated that plant extracts could prevent and alleviate these adverse outcomes. Piper betle Linn. (Piper betle L.) is a cosmopolitan plant that belongs to the Piperaceae family, whose leaves are edible and possess several health benefits. This study sought to characterize the anti-inflammatory and antioxidant effects of a methanol extract of Piper betle L. leaves and stems (MPBLLS). MPBLLS was found to have a dose-dependent radical scavenging effect, as demonstrated by the 2,2-diphenyl-1-picrylhydrazyl assay. Additionally, MPBLLS inhibited the lipopolysaccharide (LPS)-stimulated production of nitric oxide and prostaglandin E2 by reducing the expression of inducible nitric oxide synthase and cyclooxygenase-2 in RAW 264.7 macrophages without affecting cell viability. Furthermore, our findings suggested that the inhibitory effects of MPBLLS on pro-inflammatory cytokines such as tumor necrosis factor-α, interleukin-1ß, and interleukin-6 were due to the inhibition of the nuclear factor-κB (NF-κB) and mitogen-activated protein kinase (MAPK) signaling pathways in LPS-treated RAW 264.7 macrophages. MPBLLS and hydroxychavicol, a major constituent of MPBLLS, suppressed LPS-induced translocation of NF-κB p65 from cytoplasm to nucleus. Interestingly, MPBLLS increased nuclear factor erythroid 2-related factor 2 (Nrf2) protein levels and transcription levels of Nrf2 target genes in a dose-dependent manner. Collectively, our findings suggest that MPBLLS could serve as a basis for the development of novel orally-administered therapies due to its inhibitory effects on oxidative and inflammatory stress. DATA AVAILABILITY: The data presented in this study are available on request from the corresponding author.


Assuntos
NF-kappa B , Piper betle , Camundongos , Animais , NF-kappa B/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Antioxidantes/farmacologia , Antioxidantes/metabolismo , Lipopolissacarídeos/farmacologia , Lipopolissacarídeos/metabolismo , Fator 2 Relacionado a NF-E2/metabolismo , Interleucina-1beta/metabolismo , Metanol/farmacologia , Ciclo-Oxigenase 2/metabolismo , Óxido Nítrico/metabolismo , Fator de Necrose Tumoral alfa/metabolismo , Células RAW 264.7 , Interleucina-6/metabolismo , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/metabolismo , Macrófagos , Extratos Vegetais/farmacologia , Extratos Vegetais/metabolismo , Sistema de Sinalização das MAP Quinases , Citocinas/metabolismo , Proteínas Quinases Ativadas por Mitógeno/metabolismo , Prostaglandinas/metabolismo
12.
Pak J Pharm Sci ; 35(4): 1109-1116, 2022 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-36008909

RESUMO

The study was undertaken to determine antioxidant, anticancer and antimicrobial activities of Moringa oleifera flowers. We used three different solvents, hexane (MOF-H), ethyl acetate (MOF-EA) and methanol (MOF-M), to extract the flowers of M. oleifera using the ultrasound-assisted extraction (UAE) approach. Disc diffusion method was used to test for antimicrobial activity. In cytotoxicity research, cell lines derived from breast cancer (MCF-7) and ovarian cancer (ES-2) were used. IC50 values for DPPH, ABTS and Nitric oxide for MOF-EA are 33.54±1.13, 29.86±0.08 and 49.7±1.12µg/mL, respectively, making it the most effective antioxidant in terms of scavenging free radicals. The order of suppression of bacterial growth by the methanolic extract was E. coli>P. aeruginosa>S. aureus, making it the most effective antibacterial agent tested. MOF-H, MOF-EA and MOF-M had fungal inhibition zones of 5.6mm, 7mm and 10.7mm, respectively, compared to DMSO. It was found that MOF-EA had potent antioxidant, cytotoxic and antibacterial capabilities that could be employed as an alternate treatment therapy following clinical trials.


Assuntos
Moringa oleifera , Antibacterianos/toxicidade , Antioxidantes/farmacologia , Escherichia coli , Flores , Metanol/farmacologia , Extratos Vegetais/farmacologia , Staphylococcus aureus
13.
J Ethnopharmacol ; 299: 115621, 2022 Dec 05.
Artigo em Inglês | MEDLINE | ID: mdl-35987413

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Lignosus rhinocerus, also known as Tiger Milk Mushroom has been used traditionally to treat a variety of human conditions, including asthma, diabetes, respiratory disease, skin allergy, and food poisoning. The reported activities of Lignosus rhinocerus extracts include anti-inflammatory, anti-oxidant, anti-asthmatic, anti-microbial, anti-cancer, neuroprotection, and immune modulation effects. However, its effect on human skin is not well documented, including human skin exposed to ultraviolet light (UV). Exposure to UV can trigger various cellular responses, including inflammation, oxidative stress, DNA damage, cell death, and cellular aging. AIM OF THE STUDY: The study aims to investigate the effects of methanolic extract prepared from cultured Lignosus rhinocerus (herein referred to as TM02 and its methanol extract as TM02-ME) on UV-irradiated human keratinocytes. MATERIALS AND METHODS: Powdered stock of TM02 was dissolved and sequentially extracted with different solvents to prepare the extracts and the methanol extract was subsequently characterized based on its bio-activities on HaCaT human keratinocytes. The keratinocytes were pre-treated with the methanol extract followed by UV-irradiation. Cellular responses of the HaCaT cells such as cell viability, DNA damage, as well as gene and protein expressions that were responsive to the treatments, were characterized by using bio-assays, including reverse-transcription based PCR, Western blot, cell viability, and mitochondrial Cytochrome C release assays. RESULTS: TM02-ME protected HaCaT cells from UV-induced DNA damage and cell death in a dose-dependent manner. Pre-treatment of HaCaT cells with TM02-ME led to a 39% reduction of cyclobutane pyrimidine dimers (CPD) and up-regulated the gene expression of REV1 and SPINK5 in UVB-irradiated HaCaT cells when compared to the control. In addition, TM-02-ME treated HaCaT cells increased the expression of BCL-XL and BCL-2 proteins which coincided with the down-regulation of mitochondrial Cyt. C release in the UV-B irradiated HaCaT cells. The results were further supported by data that showed the stable clones of HaCaT cells stably expressed BCL-XL were resistant to UVB-induced cell death. CONCLUSIONS: __The results showed that TM02-ME confers photoprotective activities to UVB-irradiated HaCaT cells, leading to a reduction in DNA damage and cell death as well as up-regulated the expression of REV1 and SPINK5 which are involved in DNA repair and skin barrier function, respectively. The up-regulation of pro-survival members of the BCL-2 family by TM02-ME confers protection against UVB-induced cell death.


Assuntos
Antiasmáticos , Raios Ultravioleta , Antiasmáticos/farmacologia , Anti-Inflamatórios/metabolismo , Anti-Inflamatórios/farmacologia , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Citocromos c/metabolismo , Humanos , Queratinócitos , Metanol/farmacologia , Polyporaceae , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Dímeros de Pirimidina/metabolismo , Dímeros de Pirimidina/farmacologia , Solventes/farmacologia , Raios Ultravioleta/efeitos adversos
14.
BMC Complement Med Ther ; 22(1): 223, 2022 Aug 23.
Artigo em Inglês | MEDLINE | ID: mdl-35999537

RESUMO

INTRODUCTION: Symphonia globulifera and Allophylus abyssinicus are used in the management of skin rashes and sores, cough, malaria, digestive diseases, stomach ache, wounds and helminthic infections among others in Uganda, Kenya, Ethiopia, Cameroon. This study aimed at determining the phytochemical profile and antimicrobial activity of these two plants. METHODS: The stem bark and leaves of both plants were collected from Bwindi Impenetrable National Park and air-dried under shade at room temperature. Cold maceration, decoction and infusion with methanol, water and ethyl acetate as solvents were used in phytochemical extraction. Preliminary qualitative screening and thin layer chromatography were used for phytochemical profiling. Antimicrobial activity was analysed by agar well diffusion assay, broth macro-dilution assay and fractional inhibition concentration index (FICI). RESULTS: The leaves and stem bark of both plants have a diverse set of phytochemical compounds of variable polarity including, tannins, alkaloids, flavonoids, saponins, quinones and anthraquinones among others. Generally, methanol and water extracts of S. globulifera and A. abyssinicus had in-vitro bactericidal activity against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa but weak fungistatic activity against Candida albicans. Allophylus abyssinicus leaf water and S. globulifera leaf methanol extract combination had a synergistic activity (ΣFICI = 0.37) against S. aureus. Similarly, A. abyssinicus stem bark water extract and A. abyssinicus leaf water extract combination had an additive effect (ΣFICI = 1) against P. aeruginosa. CONCLUSION: The leaves and stem bark crude extracts of S. globulifera and A. abyssinicus possess a wide range of bioactive phytochemical compounds but have weak antimicrobial activity against S. aureus, E. coli, P. aeruginosa and C. albicans.


Assuntos
Anti-Infecciosos , Staphylococcus aureus , Anti-Infecciosos/farmacologia , Candida albicans , Escherichia coli , Metanol/análise , Metanol/farmacologia , Testes de Sensibilidade Microbiana , Compostos Fitoquímicos/química , Casca de Planta/química , Extratos Vegetais/química , Folhas de Planta/química , Sapindaceae , Água
15.
J Ethnopharmacol ; 298: 115636, 2022 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-35998785

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Malaria causes extensive morbidity and mortality, and the decreasing efficacy of artemisinin and its partner drugs has posed a serious concern. Therefore, it is important to identify new antimalarials, and the natural compounds from plants provide a promising platform. Mentha spicata L. representing the Lamiaceae family has been used in traditional medicine for various diseases including malaria. AIM OF THE STUDY: This study was aimed at evaluating the antiplasmodial activity of M. spicata methanolic leaf extract using Plasmodium falciparum (Pf) cultures (Pf3D7 and artemisinin (ART)-resistant PfCam3.IR539T strains) and antimalarial activity using Plasmodium berghei (Pb)-infected mice. Dry leaf powder and methanolic leaf extract were examined for in vivo antimalarial activity and the efficacy of oral versus parenteral administration was compared. MATERIALS AND METHODS: Leaves of M. spicata were collected and extracted using 70% methanol in water (v/v). [3H]-hypoxanthine incorporation assays and Giemsa-stained smears were used to assess the in vitro antiplasmodial activity of M. spicata methanolic extract against Pf3D7 and ART-resistant PfCam3.IR539T strains. Cytotoxicity was evaluated in HeLa and HEK-293T cell lines using MTT assays. Hemolysis assays were performed using red blood cells (RBCs). In vivo antimalarial activities of M. spicata dry leaf powder and methanolic leaf extract were examined in P. berghei-infected mice by Rane's curative test and Peters' 4-day suppressive test. RESULTS: Phytochemical screening of M. spicata methanolic leaf extract indicated the presence of reducing sugars, phenolic compounds, flavonoids, glycosides, sterols, saponins, alkaloids, coumarins, tannins, carbohydrates, and proteins. In vitro studies carried out using Pf cultures showed that M. spicata methanolic leaf extract had significant antiplasmodial activity against Pf3D7 cultures with a 50% inhibitory concentration (IC50) of 57.99 ± 2.82 µg/ml. The extract was also effective against ART-resistant PfCam3.IR539T strain with an IC50 of 71.23 ± 3.85 µg/ml. The extract did not show significant in vitro cytotoxicity, hemolysis, and in vivo toxicity. In vivo studies performed using Pb-infected mice treated with M. spicata dry leaf powder and methanolic leaf extract showed ∼50% inhibition in parasite growth at 1500 mg/kg and 1000 mg/kg doses, respectively. There was also a significant delay in the mortality of treated mice. Parenteral administration was found to be appropriate for the in vivo treatment. CONCLUSIONS: Our in vitro and in vivo findings from Pf and Pb parasites suggested the therapeutic potential of M. spicata leaf extract as an antimalarial. M. spicata leaf extract could also inhibit the growth of ART-resistant Pf strain. Further studies on fractionation and active component analysis of M. spicata leaf extract would be required to identify the bioactive phytochemicals having pharmaceutical and therapeutic values. Such efforts would help us in developing new antimalarials to combat malaria.


Assuntos
Antimaláricos , Artemisininas , Malária , Mentha spicata , Animais , Antimaláricos/química , Antimaláricos/farmacologia , Antimaláricos/uso terapêutico , Artemisininas/farmacologia , Hemólise , Chumbo/farmacologia , Chumbo/uso terapêutico , Malária/tratamento farmacológico , Malária/parasitologia , Metanol/farmacologia , Camundongos , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Extratos Vegetais/uso terapêutico , Extratos Vegetais/toxicidade , Plasmodium berghei , Plasmodium falciparum , Pós/uso terapêutico
16.
Antimicrob Agents Chemother ; 66(9): e0041422, 2022 09 20.
Artigo em Inglês | MEDLINE | ID: mdl-35972242

RESUMO

Drug-resistant Neisseria gonorrhoeae is a serious global health concern. New drugs are needed that can overcome existing drug resistance and limit the development of new resistances. Here, we describe the small molecule tricyclic pyrimidoindole JSF-2414 [8-(6-fluoro-8-(methylamino)-2-((2-methylpyrimidin-5-yl)oxy)-9H-pyrimido[4,5-b]indol-4-yl)-2-oxa-8-azaspiro[4.5]decan-3-yl)methanol], which was developed to target both ATP-binding regions of DNA gyrase (GyrB) and topoisomerase (ParE). JSF-2414 displays potent activity against N. gonorrhoeae, including drug-resistant strains. A phosphate pro-drug, JSF-2659, was developed to facilitate oral dosing. In two different animal models of Neisseria gonorrhoeae vaginal infection, JSF-2659 was highly efficacious in reducing microbial burdens to the limit of detection. The parent molecule also showed potent in vitro activity against high-threat Gram-positive organisms, and JSF-2659 was shown in a deep tissue model of vancomycin-resistant Staphylococcus aureus (VRSA) and a model of Clostridioides difficile-induced colitis to be highly efficacious and protective. JSF-2659 is a novel preclinical drug candidate against high-threat multidrug resistant organisms with low potential to develop new resistance.


Assuntos
Gonorreia , Staphylococcus aureus Resistente à Meticilina , Pró-Fármacos , Trifosfato de Adenosina , Animais , Antibacterianos/química , Antibacterianos/farmacologia , DNA Girase/genética , Farmacorresistência Bacteriana , Feminino , Gonorreia/tratamento farmacológico , Metanol/farmacologia , Staphylococcus aureus Resistente à Meticilina/metabolismo , Testes de Sensibilidade Microbiana , Neisseria gonorrhoeae , Fosfatos/farmacologia , Pró-Fármacos/farmacologia , Inibidores da Topoisomerase II/farmacologia
17.
Int J Mol Sci ; 23(13)2022 Jul 05.
Artigo em Inglês | MEDLINE | ID: mdl-35806473

RESUMO

Cosmetic ingredients originating from natural resources have garnered considerable attention, and the demand for whitening ingredients is increasing, particularly in Asian countries. Lignin is a natural phenolic biopolymer significantly effective as a natural sunscreen, as its ultraviolet protection efficacy ranges from 250 to 400 nm. However, using different types of lignin as cosmetic ingredients is difficult owing to the heterogeneity of lignin and the lack of in vitro and in vivo safety and efficacy data. Thus, steam-exploded lignin (SEL) was prepared from bamboo, fractionated via successive organic solvent extraction, and sequentially fractionated using ethyl acetate, methanol, and acetone to investigate its potential as a natural whitening material. Gel permeation chromatography showed that the molecular weight of acetone-soluble and acetone-insoluble SEL fractions were the lowest and the highest, respectively. Monomer structures of the four lignin fractions were elucidated using 1H, 13C, and 2D heteronuclear single quantum coherence nuclear magnetic resonance and pyrolysis gas chromatography/mass spectrometry. The antioxidant and tyrosinase inhibition activities of the four fractions were compared. The methanol-soluble SEL fraction (SEL-F2) showed the highest antioxidant activity (except 2,2-diphenyl-1-picrylhydrazyl scavenging activity), and the enzyme inhibition kinetics were confirmed. In this study, the expression pattern of the anti-melanogenic-related proteins by SEL-F2 was confirmed for the first time via the protein kinase A (PKA)/cAMP-response element-binding (CREB) protein signaling pathway in B16F10 melanoma cells. Thus, SEL may serve as a valuable cosmetic whitening ingredient.


Assuntos
Lignina , Monofenol Mono-Oxigenase , Acetona , Antioxidantes/farmacologia , Proteína de Ligação ao Elemento de Resposta ao AMP Cíclico/metabolismo , Lignina/química , Lignina/farmacologia , Melaninas/metabolismo , Metanol/farmacologia , Monofenol Mono-Oxigenase/metabolismo , Transdução de Sinais
18.
Mol Neurobiol ; 59(9): 5874-5890, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35804280

RESUMO

Boswellia serrata gum is a natural product that showed beneficial effects on neurodegenerative diseases in recent studies. In this study, we investigated the effects of Boswellia serrata resin on rotenone-induced dopaminergic neurotoxicity. Firstly, we attempted to see if the resin can induce AMP-activated protein kinase (AMPK) signaling pathway which has been known to have broad neuroprotective effects. Boswellia increased AMPK phosphorylation and reduced phosphorylation of mammalian target of rapamycin (p-mTOR) and α-synuclein (p-α-synuclein) in the striatum while increased the expression level of Beclin1, a marker for autophagy and brain-derived neurotrophic factor. Next, we examined the neuroprotective effects of the Boswellia extract in the rotenone-injected mice. The results showed that Boswellia evidently attenuated the loss of the nigrostriatal dopaminergic neurons and microglial activation caused by rotenone. Moreover, Boswellia ameliorated rotenone-induced decrease in the striatal dopamine and impairment in motor function. Accumulation of α-synuclein meditated by rotenone was significantly ameliorated by Boswellia. Also, we showed that ß-boswellic acid, the active constituents of Boswellia serrata gum, induced AMPK phosphorylation and attenuated α-synuclein phosphorylation in SHSY5 cells. These results suggest that Boswellia protected the dopaminergic neurons from rotenone neurotoxicity via activation of the AMPK pathway which might be associated with attenuation of α-synuclein aggregation and neuroinflammation. Further investigations are warranted to identify specific molecules in Boswellia which are responsible for the neuroprotection.


Assuntos
Boswellia , Fármacos Neuroprotetores , Síndromes Neurotóxicas , Proteínas Quinases Ativadas por AMP/metabolismo , Animais , Boswellia/metabolismo , Dopamina/metabolismo , Neurônios Dopaminérgicos/metabolismo , Mamíferos/metabolismo , Metanol/metabolismo , Metanol/farmacologia , Camundongos , Fármacos Neuroprotetores/metabolismo , Fármacos Neuroprotetores/farmacologia , Síndromes Neurotóxicas/metabolismo , Extratos Vegetais/metabolismo , Extratos Vegetais/farmacologia , Rotenona/farmacologia , alfa-Sinucleína/metabolismo
19.
J Ethnopharmacol ; 297: 115552, 2022 Oct 28.
Artigo em Inglês | MEDLINE | ID: mdl-35863615

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Urolithiasis is the presence of stones in the kidney, ureters, bladder and/or urethra; it is the third most frequent disease of the urinary tract. Mimosa malacophylla A. Gray, is a species distributed in northern Mexico, where people traditionally use it for its diuretic effect, and to treat kidney diseases; however, no scientific reports have been found in relation to its antiurolithic properties. AIM OF THE STUDY: This study aimed to obtain a qualitative phytochemical profile of the methanolic extract (ME) of M. malacophylla, and to evaluate its potential cytotoxic effect in vitro and its antiurolithic activity in vivo. MATERIAL AND METHODS: Phytochemical screening was performed to demonstrate the presence of secondary metabolite groups in the methanolic extract of M. malacophylla. In vitro cytotoxicity assays (MTT and nucleotide labeling with DAPI) were performed to evaluate the effect of the extract on kidney cell lines. Urolithiasis was induced in the bladder of Wistar rats introducing zinc disks for the calculus formation and exposed to three concentrations of ME. RESULTS: Phytochemical screening showed phenols, steroids, terpenoids and carbohydrates. In vitro analysis demonstrated that concentrations below 300 µg/mL of ME did not produce a cytotoxic effect on renal Vero and HEK-293 cells. In vivo analysis of 15 days of exposition, revealed that the extract at concentrations of 50 mg/kg to 150 mg/kg were effective as an antiurolithic treatment, and did not produce morphological alterations in kidney or bladder in murine model of induced urolithiasis. CONCLUSIONS: The antiurolithic activity may be attributed to the presence of flavonoids, steroids and terpenes detected in the phytochemical screening which have been reported to possess this activity. These results could be useful to evaluate new alternatives and their potential therapeutic effect to treat renal or urinary affections.


Assuntos
Mimosa , Urolitíase , Animais , Células HEK293 , Humanos , Rim , Metanol/farmacologia , Camundongos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Ratos , Ratos Wistar , Bexiga Urinária , Urolitíase/induzido quimicamente
20.
Nutrients ; 14(14)2022 Jul 14.
Artigo em Inglês | MEDLINE | ID: mdl-35889842

RESUMO

Although many natural products have proven their potential to regulate obesity through the modulation of adipocyte biology, none of them has yet been approved for clinical use in obesity therapy. This work aims to isolate valuable secondary metabolites from an orchid species (Dendrobium heterocarpum) and evaluate their possible roles in the growth and differentiation of 3T3-L1 pre-adipocytes. Six compounds were isolated from the orchid's methanolic extracts and identified as amoenylin (1), methyl 3-(4-hydroxyphenyl) propionate (2), 3,4-dihydroxy-5,4'-dimethoxybibenzyl (3), dendrocandin B (4), dendrofalconerol A (5), and syringaresinol (6). Among these phytochemicals, compounds 2, 3, and 6 exhibited lower effects on the viability of 3T3-L1 cells, offering non-cytotoxic concentrations of ≲10 µM. Compared to others tested, compound 3 was responsible for the maximum reduction of lipid storage in 3T3-L1 adipocytes (IC50 = 6.30 ± 0.10 µM). A set of protein expression studies unveiled that compound 3 at non-cytotoxic doses could suppress the expression of some key transcription factors in adipocyte differentiation (i.e., PPARγ and C/EBPα). Furthermore, this compound could deactivate some proteins involved in the MAPK pathways (i.e., JNK, ERK, and p38). Our findings prove that D. heterocarpum is a promising source to explore bioactive molecules capable of modulating adipocytic growth and development, which can potentially be assessed and innovated further as pharmaceutical products to defeat obesity.


Assuntos
Dendrobium , Células 3T3-L1 , Adipócitos , Adipogenia , Animais , Diferenciação Celular , Dendrobium/metabolismo , Lipídeos/farmacologia , Metanol/farmacologia , Camundongos , Obesidade/metabolismo , PPAR gama/metabolismo , Extratos Vegetais/química
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