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1.
Microb Pathog ; 194: 106797, 2024 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-39029597

RESUMEN

Candida auris, an emerging multidrug-resistant fungal pathogen discovered in Japan in 2009, poses a significant global health threat, with infections reported in about 25 countries. The escalation of drug-resistant strains underscores the urgent need for new treatment options. This study aimed to investigate the antifungal potential of 2,3,4,4a-tetrahydro-1H-xanthen-1-one (XA1) against C. auris, as well as its mechanism of action and toxic profile. The antifungal activity of XA1 was first evaluated by determining the minimum inhibitory concentration (MIC), time-kill kinetics and biofilm inhibition. In addition, structural changes, membrane permeability, reactive oxygen species (ROS) production, and in vitro and in vivo toxicity of C. auris after exposure to XA1 were investigated. The results indicated that XA1 exhibited an MIC of 50 µg/mL against C. auris, with time-kill kinetics highlighting its efficacy. Field emission scanning electron microscopy (FE-SEM) showed structural damage in XA1-treated cells, supported by increased membrane permeability leading to cell death. Furthermore, XA1 induced ROS production and significantly inhibited biofilm formation. Importantly, XA1 exhibited low cytotoxicity in human epidermal keratinocytes (HaCaT), with a cell viability of over 90 % at 6.25 µg/mL. In addition, an LD50 of 17.68 µg/mL was determined in zebrafish embryos 24 h post fertilization (hpf), with developmental delay observed at prolonged exposure at 6.25 µg/mL (48-96 hpf). These findings position XA1 as a promising candidate for further research and development of an effective antifungal agent.


Asunto(s)
Antifúngicos , Biopelículas , Candida auris , Candidiasis , Farmacorresistencia Fúngica , Fluconazol , Pruebas de Sensibilidad Microbiana , Especies Reactivas de Oxígeno , Pez Cebra , Antifúngicos/farmacología , Biopelículas/efectos de los fármacos , Especies Reactivas de Oxígeno/metabolismo , Humanos , Animales , Fluconazol/farmacología , Farmacorresistencia Fúngica/efectos de los fármacos , Candida auris/efectos de los fármacos , Candidiasis/tratamiento farmacológico , Candidiasis/microbiología , Permeabilidad de la Membrana Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Línea Celular , Queratinocitos/efectos de los fármacos , Candida/efectos de los fármacos
2.
Molecules ; 28(8)2023 Apr 21.
Artículo en Inglés | MEDLINE | ID: mdl-37110846

RESUMEN

Globally, breast cancer is the most prevalent form of cancer in women and there is a need for alternative therapies such as plant-derived compounds with low systemic toxicity and selective toxicity to cancer cells. The aim of this study is to assess the cytotoxicity effects of 7-geranyloxycinnamic acid isolated from leaves of Melicope lunu-ankenda, a traditional medicinal plant, on the human breast cancer cell lines. Dried leaf powder was used for the preparation of different crude extracts using different solvents of increasing order of polarity. The structure of the isolated compound from the petroleum ether extract was elucidated by 1H and 13C NMR, LC-MS, and DIP-MS spectroscopy. The cytotoxic activity of the crude extract and 7-geranyloxycinnamic acid analyzed using MTT assay. Apoptotic analysis was evaluated using Annexin V-PI staining, AO/PI staining, intracellular ROS measurement, and measurement of activities of caspases 3/7, 8, and 9. Crude extracts and the isolated pure compound showed significant cytotoxicity against tested cancer cell lines. 7-geranyloxycinnamic acid was found to exert significant cytotoxic effects against breast cancer cell lines such as the MCF-7 and MDA-MB-231 cell lines. The cytotoxic effects are attributed to its ability to induce apoptosis via accumulation of ROS and activation of caspases in both breast cancer cell lines. The pure compound, 7-geranyloxycinnamic acid isolated from the leaves of M. lunu-ankenda, can exert significant cytotoxic effects against breast cancer cell lines without affecting the normal cells.


Asunto(s)
Antineoplásicos Fitogénicos , Neoplasias de la Mama , Neoplasias del Colon , Rutaceae , Humanos , Femenino , Células MCF-7 , Extractos Vegetales/química , Neoplasias de la Mama/tratamiento farmacológico , Especies Reactivas de Oxígeno/análisis , Rutaceae/química , Hojas de la Planta/química , Caspasas , Apoptosis , Antineoplásicos Fitogénicos/uso terapéutico , Línea Celular Tumoral
3.
Molecules ; 28(7)2023 Apr 04.
Artículo en Inglés | MEDLINE | ID: mdl-37049977

RESUMEN

Inhibition of several protein pathways involved in cancer cell regulation is a necessary key in the discovery of cancer chemotherapy. Moringa oleifera Lam is often used in traditional medicine for the treatment of various illnesses. The plant contains glucomoringin isothiocyanate (GMG-ITC) with therapeutic potential against various cancer cells. Therefore, GMG-ITC was evaluated for its cytotoxicity against the PC-3 prostate cancer cell line and its potential to induce apoptosis. GMG-ITC inhibited cell proliferation in the PC-3 cell line with IC50 value 3.5 µg/mL. Morphological changes as a result of GMG-ITC-induced apoptosis showed chromatin condensation, nuclear fragmentation, and membrane blebbing. Additionally, Annexin V assay showed proportion of cells in early and late apoptosis upon exposure to GMG-ITC in a time-dependent manner. Moreover, GMG-ITC induced a time-dependent G2/M phase arrest, with reduction of 39.1% in the PC-3 cell line. GMG-ITC also activates apoptotic genes including caspase, tumor suppressor gene (p53), Akt/MAPK, and Bax of the proapoptotic Bcl family. Early apoptosis proteins (JNK, Bad, Bcl2, and p53) were significantly upregulated upon GMG-ITC treatment. It is concluded that apoptosis induction was observed in PC-3 cells treated with GMG-ITC. These phenomena suggest that GMG-ITC from M. oleifera seeds could be useful as a future cytotoxic agent against prostate cancer.


Asunto(s)
Moringa oleifera , Neoplasias de la Próstata , Masculino , Humanos , Células PC-3 , Proteína p53 Supresora de Tumor , Apoptosis/genética , Semillas , Neoplasias de la Próstata/tratamiento farmacológico , Línea Celular Tumoral
4.
Molecules ; 26(17)2021 Aug 30.
Artículo en Inglés | MEDLINE | ID: mdl-34500692

RESUMEN

Table eggs are an affordable yet nutritious protein source for humans. Unfortunately, eggs are a vector for bacteria that could cause foodborne illness. This study aimed to investigate the effectiveness of a quaternary ammonium compound (quat) sanitizer against aerobic mesophilic bacteria, yeast, and mold load on the eggshell surface of free-range and commercial farms and the post-treatment effect on microbial load during storage. Total aerobic mesophilic bacteria, yeast, and molds were enumerated using plate count techniques. The efficacy of the quaternary ammonium sanitizer (quat) was tested using two levels: full factorial with two replicates for corner points, factor A (maximum: 200 ppm, minimum: 100 ppm) and factor B (maximum: 15 min, minimum: 5 min). Quat sanitizer significantly (p < 0.05) reduced approximately 4 log10 CFU/cm2 of the aerobic mesophilic bacteria, 1.5 to 2.5 log10 CFU/cm2 of the mold population, and 1.5 to 2 log10 CFU/cm2 of the yeast population. However, there was no significant (p ≥ 0.05) response observed between individual factor levels (maximum and minimum), and two-way interaction terms were also not statistically significant (p ≥ 0.05). A low (<1 log10 CFU/cm2) aerobic mesophilic bacteria trend was observed when shell eggs were stored in a cold environment up to the production expiry date. No internal microbial load was observed; thus, it was postulated that washing with quat sanitizer discreetly (without physically damaging the eggshell) does not facilitate microbial penetration during storage at either room temperature or cold storage. Current study findings demonstrated that the quat sanitizer effectively reduced the microbial population on eggshells without promoting internal microbial growth.


Asunto(s)
Cáscara de Huevo/microbiología , Huevos/microbiología , Compuestos de Amonio Cuaternario/farmacología , Animales , Bacterias Aerobias/efectos de los fármacos , Desinfección , Microbiología de Alimentos , Humanos
5.
Molecules ; 26(17)2021 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-34500755

RESUMEN

Bacterial infections are regarded as one of the leading causes of fatal morbidity and death in patients infected with diseases. The ability of microorganisms, particularly methicillin-resistant Staphylococcus aureus (MRSA), to develop resistance to current drugs has evoked the need for a continuous search for new drugs with better efficacies. Hence, a series of non-PAINS associated pyrrolylated-chalcones (1-15) were synthesized and evaluated for their potency against MRSA. The hydroxyl-containing compounds (8, 9, and 10) showed the most significant anti-MRSA efficiency, with the MIC and MBC values ranging from 0.08 to 0.70 mg/mL and 0.16 to 1.88 mg/mL, respectively. The time-kill curve and SEM analyses exhibited bacterial cell death within four hours after exposure to 9, suggesting its bactericidal properties. Furthermore, the docking simulation between 9 and penicillin-binding protein 2a (PBP2a, PDB ID: 6Q9N) suggests a relatively similar bonding interaction to the standard drug with a binding affinity score of -7.0 kcal/mol. Moreover, the zebrafish model showed no toxic effects in the normal embryonic development, blood vessel formation, and apoptosis when exposed to up to 40 µM of compound 9. The overall results suggest that the pyrrolylated-chalcones may be considered as a potential inhibitor in the design of new anti-MRSA agents.


Asunto(s)
Antibacterianos/farmacología , Chalconas/farmacología , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Pirroles/farmacología , Antibacterianos/química , Chalconas/química , Relación Dosis-Respuesta a Droga , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Pirroles/química , Relación Estructura-Actividad
6.
Molecules ; 25(13)2020 Jul 06.
Artículo en Inglés | MEDLINE | ID: mdl-32640512

RESUMEN

2,4,6-trihydroxy-3-geranylacetophenone (tHGA) is a bioactive compound that shows excellent anti-inflammatory properties. However, its pharmacokinetics and metabolism have yet to be evaluated. In this study, a sensitive LC-HRMS method was developed and validated to quantify tHGA in rat plasma. The method showed good linearity (0.5-80 ng/mL). The accuracy and precision were within 10%. Pharmacokinetic investigations were performed on three groups of six rats. The first two groups were given oral administrations of unformulated and liposome-encapsulated tHGA, respectively, while the third group received intraperitoneal administration of liposome-encapsulated tHGA. The maximum concentration (Cmax), the time required to reach Cmax (tmax), elimination half-life (t1/2) and area under curve (AUC0-24) values for intraperitoneal administration were 54.6 ng/mL, 1.5 h, 6.7 h, and 193.9 ng/mL·h, respectively. For the oral administration of unformulated and formulated tHGA, Cmax values were 5.4 and 14.5 ng/mL, tmax values were 0.25 h for both, t1/2 values were 6.9 and 6.6 h, and AUC0-24 values were 17.6 and 40.7 ng/mL·h, respectively. The liposomal formulation improved the relative oral bioavailability of tHGA from 9.1% to 21.0% which was a 2.3-fold increment. Further, a total of 12 metabolites were detected and structurally characterized. The metabolites were mainly products of oxidation and glucuronide conjugation.


Asunto(s)
Acetofenonas/sangre , Acetofenonas/farmacocinética , Cromatografía Liquida/métodos , Liposomas/administración & dosificación , Floroglucinol/análogos & derivados , Espectrometría de Masas en Tándem/métodos , Acetofenonas/administración & dosificación , Acetofenonas/metabolismo , Administración Oral , Animales , Disponibilidad Biológica , Inyecciones Intraperitoneales , Masculino , Floroglucinol/administración & dosificación , Floroglucinol/sangre , Floroglucinol/metabolismo , Floroglucinol/farmacocinética , Plasma/química , Ratas , Ratas Sprague-Dawley
7.
Molecules ; 24(17)2019 Aug 26.
Artículo en Inglés | MEDLINE | ID: mdl-31454974

RESUMEN

Piper cubeba L. is the berry of a shrub that is indigenous to Java, Southern Borneo, Sumatra, and other islands in the Indian Ocean. The plant is usually used in folk traditional medicine and is an important ingredient in cooking. The purpose of this study was to isolate and purify the bioactive compounds from P. cubeba L. fractions. In addition, the isolated compounds were tested for their antibacterial and antispore activities against vegetative cells and spores of Bacillus cereus ATCC33019, B. subtilis ATCC6633, B. pumilus ATCC14884, and B. megaterium ATCC14581. The phytochemical investigation of the DCM fraction yielded two known compounds: ß-asarone (1), and asaronaldehyde (2) were successfully isolated and identified from the methanol extract and its fractions of P. cubeba L. Results showed that exposing the vegetative cells of Bacillus sp. to isolated compounds resulted in an inhibition zone with a large diameter ranging between 7.21 to 9.61 mm. The range of the minimum inhibitory concentration (MIC) was between 63.0 to 125.0 µg/mL and had minimum bactericidal concentration (MBC) at 250.0 to 500.0 µg/mL against Bacillus sp. Isolated compounds at a concentration of 0.05% inactivated more than 3-Log10 (90.99%) of the spores of Bacillus sp. after an incubation period of four hours, and all the spores were killed at a concentration of 0.1%. The structures were recognizably elucidated based on 1D and 2D-NMR analyses (1H, 13C, COSY, HSQC, and HMBC) and mass spectrometry data. Compounds 1, and 2 were isolated for the first time from this plant. In conclusion, the two compounds show a promising potential of antibacterial and sporicidal activities against Bacillus sp. and thus can be developed as an anti-Bacillus agent.


Asunto(s)
Aldehídos/farmacología , Anisoles/farmacología , Antibacterianos/farmacología , Piper/química , Esporas Bacterianas/efectos de los fármacos , Aldehídos/aislamiento & purificación , Derivados de Alilbenceno , Anisoles/aislamiento & purificación , Antibacterianos/aislamiento & purificación , Bacillus cereus/efectos de los fármacos , Bacillus cereus/fisiología , Bacillus megaterium/química , Bacillus megaterium/efectos de los fármacos , Bacillus pumilus/efectos de los fármacos , Bacillus pumilus/fisiología , Bacillus subtilis/efectos de los fármacos , Bacillus subtilis/fisiología , Cromatografía en Capa Delgada , Medicina Tradicional , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología
8.
Phytother Res ; 32(8): 1608-1616, 2018 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-29672974

RESUMEN

The antiphoto aging property of Zanthoxylum rhetsa obtained from Pangkor Island, Malaysia, was evaluated. Solvent fractions of different polarity obtained from the methanolic extract of the bark material were initially tested for anticollagenase and antielastase activities. The ethyl acetate fraction showed bioactivity against the protease enzymes. Hence, it was subjected to further purification via column chromatography, to yield a major constituent, hesperidin. Subsequently, the ethyl acetate fraction and hesperidin were tested for their effects against UVB-induced cytotoxicity and expressions of inflammatory cytokines (IL-6, IL-1ß, and TNF-α), NF-κB, and MMPs (MMP1, 3, and 9) in human dermal fibroblasts (HDF). Both fraction and pure compound prevented UVB-induced cytotoxicity in HDF cells, in a dose dependent manner. Moreover, the ethyl acetate fraction inhibited the increase of pro-inflammatory cytokines induced by UVB to a level similar to the control (without UV treatment). Additionally, the fraction significantly inhibited the expressions of NF-κB, MMP 1, MMP 3, and MMP 9 in HDF cells treated with UVB. Similar effects were observed with hesperidin. The results obtained suggested that the ethyl acetate fraction of Z. rhetsa and its bioactive constituent, hesperidin, have the potential to be used as active ingredients in sunscreen and antiphoto aging formulations.


Asunto(s)
Citocinas/metabolismo , Hesperidina/farmacología , Metaloproteinasas de la Matriz/metabolismo , Corteza de la Planta/química , Extractos Vegetales/farmacología , Rayos Ultravioleta , Zanthoxylum/química , Células Cultivadas , Fibroblastos/efectos de los fármacos , Fibroblastos/efectos de la radiación , Humanos , Interleucina-1beta/metabolismo , Interleucina-6/metabolismo , Malasia , Metaloproteinasa 1 de la Matriz/metabolismo , Metaloproteinasa 3 de la Matriz/metabolismo , Metaloproteinasa 9 de la Matriz/metabolismo , Inhibidores de la Metaloproteinasa de la Matriz/farmacología , FN-kappa B/metabolismo , Elastasa Pancreática/antagonistas & inhibidores , Factor de Necrosis Tumoral alfa/metabolismo
9.
Molecules ; 23(7)2018 Jul 16.
Artículo en Inglés | MEDLINE | ID: mdl-30012946

RESUMEN

The aim of this study was to determine the effects of different solvents for extraction, liquid⁻liquid partition, and concentrations of extracts and fractions of Piper cubeba L. on anticariogenic; antibacterial and anti-inflammatory activity against oral bacteria. Furthermore, ¹H-Nuclear Magnetic Resonance (NMR) coupled with multivariate data analysis (MVDA) was applied to discriminate between the extracts and fractions and examine the metabolites that correlate to the bioactivities. All tested bacteria were susceptible to Piper cubeba L. extracts and fractions. Different solvents extraction, liquid⁻liquid partition and concentrations of extracts and fractions have partially influenced the antibacterial activity. MTT assay showed that P. cubeba L. extracts and fractions were not toxic to RAW 264.7 cells at selected concentrations. Anti-inflammatory activity evaluated by nitric oxide (NO) production in lipopolysaccharide (LPS) stimulated cells showed a reduction in NO production in cells treated with P. cubeba L. extracts and fractions, compared to those without treatment. Twelve putative metabolites have been identified, which are (1) cubebin, (2) yatein, (3) hinokinin, (4) dihydrocubebin, (5) dihydroclusin, (6) cubebinin, (7) magnosalin, (8) p-cymene, (9) piperidine, (10) cubebol, (11) d-germacrene and (12) ledol. Different extraction and liquid⁻liquid partition solvents caused separation in principal component analysis (PCA) models. The partial least squares (PLS) models showed that higher anticariogenic activity was related more to the polar solvents, despite some of the active metabolites also present in the non-polar solvents. Hence, P. cubeba L. extracts and fractions exhibited antibacterial and anti-inflammatory activity and have potential to be developed as the anticariogenic agent.


Asunto(s)
Antibacterianos , Antiinflamatorios , Antineoplásicos Fitogénicos , Bacterias/crecimiento & desarrollo , Piper/química , Extractos Vegetales/química , Solventes/química , Animales , Antibacterianos/química , Antibacterianos/aislamiento & purificación , Antibacterianos/farmacología , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Antiinflamatorios/farmacología , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Antineoplásicos Fitogénicos/farmacología , Ratones , Células RAW 264.7
10.
Molecules ; 23(10)2018 Oct 20.
Artículo en Inglés | MEDLINE | ID: mdl-30347850

RESUMEN

Natural products, either pure compounds or standardized plant extracts, have provided opportunities for the discovery of new drugs. Nowadays, most of the world's population still relies on traditional medicines for healthcare purposes. Plants, in particular, are always used as traditional medicine, as they contain a diverse number of phytochemicals that can be used for the treatment of diseases. The multicomponent feature in the plants is considered a positive phytotherapeutic hallmark. Hence, ethnopharmacognosy has been the focus for finding alternative treatments for diseases. Melicope lunu-ankenda, also known as Euodia lunu-ankenda, is widely distributed in tropical regions of Asia. Different parts of M. lunu-ankenda have been used for treatment of hypertension, menstrual disorder, diabetes, and fever, and as an emmenagogue and tonic. It has also been consumed as salad and as a condiment for food flavorings. The justification of use of M. lunu-ankenda in folk medicines is supported by its reported biological activities, including its cytotoxic, antibacterial, antioxidant, analgesic, antidiabetic, and anti-inflammatory activities. This review summarizes the phytochemical compounds isolated from various parts of M. lunu-ankenda, such as root and leaves, and also its biological activities, which could make the species a new therapeutic agent for some diseases, including diabetes, in the future.


Asunto(s)
Descubrimiento de Drogas , Fitoquímicos/uso terapéutico , Extractos Vegetales/uso terapéutico , Rutaceae/química , Antioxidantes/química , Antioxidantes/uso terapéutico , Diabetes Mellitus/tratamiento farmacológico , Diabetes Mellitus/epidemiología , Evodia/química , Humanos , Fitoquímicos/química , Extractos Vegetales/química
11.
Crit Rev Food Sci Nutr ; 57(18): 3971-3986, 2017 Dec 12.
Artículo en Inglés | MEDLINE | ID: mdl-28001082

RESUMEN

Campylobacter is globally recognized as a major cause of foodborne infection in humans, whilst the development of antimicrobial resistance and the possibility of repelling therapy increase the threat to public health. Poultry is the most frequent source of Campylobacter infection in humans, and southeast Asia is a global leader in poultry production, consumption, and exports. Though three of the world's top 20 most populated countries are located in southeast Asia, the true burden of Campylobacter infection in the region has not been fully elucidated. Based on published data, Campylobacter has been reported in humans, animals, and food commodities in the region. To our knowledge, this study is the first to review the status of human Campylobacter infection in southeast Asia and to discuss future perspectives. Gaining insight into the true burden of the infection and prevalence levels of Campylobacter spp. in the southeast Asian region is essential to ensuring global and regional food safety through facilitating improvements in surveillance systems, food safety regulations, and mitigation strategies.


Asunto(s)
Infecciones por Campylobacter/prevención & control , Enfermedades Transmitidas por los Alimentos/prevención & control , Animales , Asia Sudoriental , Campylobacter , Infecciones por Campylobacter/veterinaria , Contaminación de Alimentos , Microbiología de Alimentos , Inocuidad de los Alimentos , Enfermedades Transmitidas por los Alimentos/microbiología , Humanos , Aves de Corral , Enfermedades de las Aves de Corral/prevención & control , Enfermedades de las Aves de Corral/transmisión , Salud Pública
12.
Int J Mol Sci ; 17(5)2016 May 19.
Artículo en Inglés | MEDLINE | ID: mdl-27213349

RESUMEN

The use of nanoparticle delivery systems to enhance intracellular penetration of antibiotics and their retention time is becoming popular. The challenge, however, is that the interaction of nanoparticles with biological systems at the cellular level must be established prior to biomedical applications. Ciprofloxacin-cockle shells-derived calcium carbonate (aragonite) nanoparticles (C-CSCCAN) were developed and characterized. Antibacterial activity was determined using a modified disc diffusion protocol on Salmonella Typhimurium (S. Typhimurium). Biocompatibilittes with macrophage were evaluated using the 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and 5-Bromo-2'-deoxyuridine (BrdU) assays. Transcriptional regulation of interleukin 1 beta (IL-1ß) was determined using reverse transcriptase-polymerase chain reaction (RT-PCR). C-CSCCAN were spherical in shape, with particle sizes ranging from 11.93 to 22.12 nm. Encapsulation efficiency (EE) and loading content (LC) were 99.5% and 5.9%, respectively, with negative ζ potential. X-ray diffraction patterns revealed strong crystallizations and purity in the formulations. The mean diameter of inhibition zone was 18.6 ± 0.5 mm, which was better than ciprofloxacin alone (11.7 ± 0.9 mm). Study of biocompatability established the cytocompatability of the delivery system without upregulation of IL-1ß. The results indicated that ciprofloxacin-nanoparticles enhanced the antibacterial efficacy of the antibiotic, and could act as a suitable delivery system against intracellular infections.


Asunto(s)
Carbonato de Calcio , Ciprofloxacina , Portadores de Fármacos , Macrófagos/metabolismo , Ensayo de Materiales , Nanopartículas/química , Animales , Carbonato de Calcio/química , Carbonato de Calcio/farmacocinética , Carbonato de Calcio/farmacología , Línea Celular , Ciprofloxacina/química , Ciprofloxacina/farmacocinética , Ciprofloxacina/farmacología , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Portadores de Fármacos/farmacología , Ratones
13.
Molecules ; 21(6)2016 May 24.
Artículo en Inglés | MEDLINE | ID: mdl-27231889

RESUMEN

Zanthoxylum rhetsa is an aromatic tree, known vernacularly as "Indian Prickly Ash". It has been predominantly used by Indian tribes for the treatment of many infirmities like diabetes, inflammation, rheumatism, toothache and diarrhea. In this study, we identified major volatile constituents present in different solvent fractions of Z. rhetsa bark using GC-MS analysis and isolated two tetrahydrofuran lignans (yangambin and kobusin), a berberine alkaloid (columbamine) and a triterpenoid (lupeol) from the bioactive chloroform fraction. The solvent fractions and purified compounds were tested for their cytotoxic potential against human dermal fibroblasts (HDF) and mouse melanoma (B16-F10) cells, using the MTT assay. All the solvent fractions and purified compounds were found to be non-cytotoxic to HDF cells. However, the chloroform fraction and kobusin exhibited cytotoxic effect against B16-F10 melanoma cells. The presence of bioactive lignans and alkaloids were suggested to be responsible for the cytotoxic property of Z. rhetsa bark against B16-F10 cells.


Asunto(s)
Alcaloides/administración & dosificación , Melanoma Experimental/tratamiento farmacológico , Extractos Vegetales/administración & dosificación , Zanthoxylum/química , Alcaloides/química , Animales , Benzodioxoles/administración & dosificación , Benzodioxoles/química , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Fibroblastos/efectos de los fármacos , Furanos/administración & dosificación , Furanos/química , Humanos , Lignanos/administración & dosificación , Lignanos/química , Melanoma Experimental/patología , Ratones , Corteza de la Planta/química , Extractos Vegetales/química
14.
J Sci Food Agric ; 95(12): 2533-43, 2015 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-25371390

RESUMEN

BACKGROUND: The metabolite changes in three germplasm accessions of Malaysia Andrographis paniculata (Burm. F.) Nees, viz. 11265 (H), 11341 (P) and 11248 (T), due to their different harvesting ages and times were successfully evaluated by attenuated total reflectance (ATR)-Fourier transform infrared (FTIR) spectroscopy and translated through multivariate data analysis of principal component analysis (PCA) and orthogonal partial least square-discriminant analysis (OPLS-DA). This present study revealed the feasibility of ATR-FTIR in detecting the trend changes of the major metabolites - andrographolide and neoandrographolide - functional groups in A. paniculata leaves of different accessions. The harvesting parameter was set at three different ages of 120, 150 and 180 days after transplanting (DAT) and at two different time sessions of morning (7:30-10:30 am) and evening (2:30-5.30 pm). RESULTS: OPLS-DA successfully discriminated the A. paniculata crude extracts into groups of which the main constituents - andrographolide and neoandrographolide - could be mainly observed in the morning session of 120 DAT for P and T, while H gave the highest intensities of these constituents at 150 DAT. CONCLUSION: The information extracted from ATR-FTIR data through OPLS-DA could be useful in tailoring this plant harvest stage in relation to the content of its two major diterpene lactones: andrographolide and neoandrographolide.


Asunto(s)
Andrographis/metabolismo , Agricultura , Análisis Discriminante , Humanos , Hojas de la Planta/metabolismo , Espectroscopía Infrarroja por Transformada de Fourier/métodos , Factores de Tiempo
15.
J Mol Model ; 30(5): 136, 2024 Apr 18.
Artículo en Inglés | MEDLINE | ID: mdl-38634946

RESUMEN

CONTEXT: Further understanding of the molecular mechanisms is necessary since it is important for designing new drugs. This study aimed to understand the molecular mechanisms involved in the design of drugs that are inhibitors of the α-glucosidase enzyme. This research aims to gain further understanding of the molecular mechanisms underlying antidiabetic drug design. The molecular docking process yielded 4 compounds with the best affinity energy, including γ-Mangostin, 1,6-dimethyl-ester-3-isomangostin, 1,3,6-trimethyl-ester-α-mangostin, and 3,6,7-trimethyl-ester-γ-mangostin. Free energy calculation with molecular mechanics with generalized born and surface area solvation indicated that the 3,6,7-trimethyl-γ-mangostin had a better free energy value compared to acarbose and simulated maltose together with 3,6,7-trimethyl-γ-mangostin compound. Based on the analysis of electrostatic, van der Waals, and intermolecular hydrogen interactions, 3,6,7-trimethyl-γ-mangostin adopts a noncompetitive inhibition mechanism, whereas acarbose adopts a competitive inhibition mechanism. Consequently, 3,6,7-trimethyl-ester-γ-mangostin, which is a derivative of γ-mangostin, can provide better activity in silico with molecular docking approaches and molecular dynamics simulations. METHOD: This research commenced with retrieving protein structures from the RCSB database, generating the formation of ligands using the ChemDraw Professional software, conducting molecular docking with the Autodock Vina software, and performing molecular dynamics simulations using the Amber software, along with the evaluation of RMSD values and intermolecular hydrogen bonds. Free energy, electrostatic interactions, and Van der Waals interaction were calculated using MM/GBSA. Acarbose, used as a positive control, and maltose are simulated together with test compound that has the best free energy. The forcefields used for molecular dynamics simulations are ff19SB, gaff2, and tip3p.


Asunto(s)
Hipoglucemiantes , Xantonas , alfa-Glucosidasas , Acarbosa , Maltosa , Simulación del Acoplamiento Molecular , Simulación de Dinámica Molecular , Ésteres
16.
J Mol Model ; 30(8): 260, 2024 Jul 09.
Artículo en Inglés | MEDLINE | ID: mdl-38981921

RESUMEN

CONTEXT: Diabetes mellitus (DM) is a metabolic disorder disease that causes hyperglycemia conditions and associated with various chronic complications leading to mortality. Due to high toxicity of conventional diabetic drugs, the exploration of natural compounds as alternative diabetes treatments has been widely carried out. Previous in silico studies have highlighted berberine, a natural compound, as a promising alternative in antidiabetic therapy, potentially acting through various pathways, including the inhibition of the FOXO1 transcription factor in the gluconeogenesis pathway. However, the specific mechanism by which berberine interacts with FOXO1 remains unclear, and research in this area is relatively limited. Therefore, this study aims to determine the stability of berberine structure with FOXO1 based on RMSD, RMSF, binding energy, and trajectory analysis to determine the potential of berberine to inhibit the gluconeogenesis pathway. This research was conducted by in silico method with molecular docking using AutoDock4.2 and molecular dynamics study using Amber20, then visualized by VMD. METHODS: Docking between ligand and FOXO1 receptor was carried out with Autodock4.2. For molecular dynamics simulations, the force fields of DNA.OL15, protein.ff14SB, gaff2, and tip3p were used.


Asunto(s)
Berberina , Proteína Forkhead Box O1 , Hipoglucemiantes , Simulación del Acoplamiento Molecular , Simulación de Dinámica Molecular , Berberina/química , Berberina/farmacología , Hipoglucemiantes/química , Hipoglucemiantes/farmacología , Proteína Forkhead Box O1/metabolismo , Proteína Forkhead Box O1/química , Humanos , Unión Proteica , Sitios de Unión , Ligandos
17.
Heliyon ; 10(16): e35691, 2024 Aug 30.
Artículo en Inglés | MEDLINE | ID: mdl-39247385

RESUMEN

Gnetum gnemon L. is an evergreen tree that belongs to the Gnetaceae family and is commonly used as a vegetable and medicinal plant among indigenous people. The key goal of this study was to assess the antibacterial efficacy of ethanolic G. gnemon leaf extract (EGLE) against six food-borne pathogens. The antimicrobial activity of EGLE was evaluated using multiple methods, including the well diffusion assay (WDA), minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), and time-kill assay. Gas Chromatography-Mass Spectrometry (GC-MS) analysis was used to identify active volatile compounds responsible for EGLE's antibacterial activities. Total plate count (TPC) was conducted to measure microbial populations and evaluate the efficacy of EGLE as a natural preservative in raw quail eggs. 100 g of dried and powdered sample yielded an average of 11.58 ± 0.38 % post-extraction. The inhibition zone in WDA ranged from 11.00 ± 0.57-13.50 ± 0.58 mm, MIC ranged from 6.25 to 50.00 mg/mL, and MBC values were between 12.5 and >50 mg/mL. Results from the time-kill study showed that at 4 × MIC Bacillus pumilus and B. megaterium were completely killed in 1 h incubation time and other bacteria were killed within 2-4 h. Findings from TPC demonstrated that at the highest tested concentration of EGLE, there was no significant bacterial growth for a 30-day observation period. Thereby, suggesting that it had the potential to function as a natural preservative for raw quail eggs. EGLE may be a viable alternative to synthetic preservatives in combating food-borne pathogens.

18.
Poult Sci ; 103(7): 103764, 2024 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-38669823

RESUMEN

The implementation of the head-only electrical stunning procedure in poultry processing has been aimed at enhancing eating, ethical, and religious quality. However, inconsistencies in voltage and frequency standardization, along with variations in previous research outcomes, have led to numerous cases of both under-stunned and over-stunned birds. Thus, this study aimed to comprehensively evaluate the effects of varying voltages and frequencies during electrical water bath stunning on carcass quality, meat attributes, and textural properties in broiler chickens. A cohort of 240 healthy female broilers (Cobb 500, 42-days-old, 2 kg ± 0.1 kg) was meticulously selected from a commercial farm. The birds underwent exposure to different stunning voltages (2.5, 10.5, 30, and 40 V) and frequencies (50 and 300 Hz). Subsequent analyses were conducted on meat samples to assess physicochemical properties, carcass quality, and textural attributes. The findings revealed a higher incidence of petechial hemorrhage (P < 0.05) in birds stunned at 10.5 V compared to other voltage. Notably, no broken bones were recorded in birds subjected to high voltages (30 and 40 V). Low frequency (50 Hz) significantly increased the occurrence of petechial hemorrhage and simultaneously resulted in pectoralis major muscle with decreased redness (a*). Birds subjected to the 10.5 V stunning treatment exhibited a lower cooking loss percentage. Significant interactions between voltage and ageing (V × A) were observed. Birds stunned at 30 V and aged for 7 d displayed highest drip loss compared to a one-day ageing period across different voltage levels. This interaction also impacted pH values, with birds subjected to 10.5 V showing significantly lower (P < 0.05) pH at d 7 of ageing. The meat hardness was influenced by the V × A interaction, wherein birds stunned at 10.5 V exhibited lower hardness after one day of ageing compared to other voltage levels. Red wing tips, lightness (L*), adhesiveness, and resilience were also significantly impacted (P < 0.05) by the interaction between frequency and voltage. A notable 3-way interaction was observed for gumminess and chewiness (F × V × A), where the 2-way interaction between frequency and voltage (F × V) affected both parameters differently at various ageing periods. Additionally, there was a significant interaction (P < 0.05) between frequency and voltage influencing shear strength and yellowness.


Asunto(s)
Mataderos , Pollos , Carne , Animales , Pollos/fisiología , Carne/análisis , Femenino , Electrochoque/veterinaria , Bienestar del Animal , Manipulación de Alimentos/métodos , Agua/química
19.
Phytother Res ; 27(7): 1061-6, 2013 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-22969012

RESUMEN

The purpose of this study was to investigate the activity of xanthorrhizol isolated from Curcuma xanthorrhiza Roxb. on Candida albicans biofilms at adherent, intermediate, and mature phase of growth. C. albicans biofilms were formed in flat-bottom 96-well microtiter plates. The biofilms of C. albicans at different phases of development were exposed to xanthorrhizol at different concentrations (0.5 µg/mL-256 µg/mL) for 24 h. The metabolic activity of cells within the biofilms was quantified using the XTT reduction assay. Sessile minimum inhibitory concentrations (SMICs) were determined at 50% and 80% reduction in the biofilm OD490 compared to the control wells. The SMIC50 and SMIC80 of xanthorrhizol against 18 C. albicans biofilms were 4--16 µg/mL and 8--32 µg/mL, respectively. The results demonstrated that the activity of xanthorrhizol in reducing C. albicans biofilms OD490 was dependent on the concentration and the phase of growth of biofilm. Xanthorrhizol at concentration of 8 µg/mL completely reduced in biofilm referring to XTT-colorimetric readings at adherent phase, whereas 32 µg/mL of xanthorrhizol reduced 87.95% and 67.48 % of biofilm referring to XTT-colorimetric readings at intermediate and mature phases, respectively. Xanthorrhizol displayed potent activity against C. albicans biofilms in vitro and therefore might have potential therapeutic implication for biofilm-associated candidal infections.


Asunto(s)
Antifúngicos/farmacología , Biopelículas/efectos de los fármacos , Candida albicans/fisiología , Curcuma/química , Fenoles/farmacología , Extractos Vegetales/farmacología , Rizoma/química , Biopelículas/crecimiento & desarrollo , Pruebas de Sensibilidad Microbiana
20.
Heliyon ; 9(8): e18749, 2023 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-37600365

RESUMEN

Terminalia catappa L. is a large, spreading type of tree which usually grows in tropical environment, especially at coastal area with sandy stones. The current study evaluated anti-Bacillus potential of the ethanolic ketapang (Terminalia catappa L.) leaf extract (EKLE) as antibacterial and sporicidal agent against vegetative cells and spores of Bacillus spp. The antibacterial activity of EKLE against Bacillus spp. (B. cereus ATCC33019, B. pumilus ATCC14884, B. subtilis ATCC6633 and B. megaterium ATCC14581) vegetative cells were determined by performing well diffusion assay (WDA), minimum inhibition concentration (MIC), minimum bacterial concentration (MBC) and time-kill curve analyses. The sporicidal activity was tested at different concentrations of EKLE. Then, the extract's stability in terms of antibacterial and sporicidal activities upon exposure to different temperatures and pHs were carried out. Results demonstrated inhibition zones of EKLE against Bacillus spp. was in the range of 9.25 ± 0.75 mm - 11.67 ± 0.47 mm. All vegetative cells of Bacillus spp. were inhibited with MIC values at 0.63-1.25 mg/mL and can be completely killed with MBC values of 0.63 - >5.00 mg/mL. Time-kill analysis showed all the Bacillus spp. tested can be completely killed at concentrations of 2.50-5.00 mg/mL from 1 to 4 h. EKLE concentration of 1% (w/v) completely killed all Bacillus spp. spores at different exposure time. The antibacterial and sporicidal activities of EKLE were not affected by exposure to different temperatures (4, 30, 50, 80 and 121 °C) and pHs (3, 7 and 10), revealing the stability of the extract against different conditions. In conclusion, Terminalia catappa L. leaf exhibits antibacterial and sporicidal activities against Bacillus spp., therefore, the extract can be developed as anti-Bacillus agent, paving the way for its utilization in food industry as a natural food preservative.

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