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1.
Chem Biodivers ; 21(9): e202401367, 2024 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-38923285

RESUMEN

This study explored the composition of essential oil (EO) and the first phytotoxic screening of EO obtained from the stems and leaves of Mentha vagans Boriss (MVEO) via hydro-distillation technique. The EO ingredients were detected through Gas Chromatography-Mass Spectrometry (GC-MS). GC-MS analysis revealed that MVEO contained 49 constituents, constituting 93.95 % of the total oil. Among MVEO constituents, dihydrocarvone was observed as the dominant constituent (24.14 %), followed by D-carvone (16.28 %) and piperitone (18.14 %). The phytotoxic effects of MVEO and its dominant compounds were examined against Amaranthus retroflexus, Lolium perenne, and Poa annua. Significant inhibition was observed by MVEO in comparison with the major constituents and their mixture, suppressing the seedling growth of tested species at the lowest dosage (0.01 mg/mL); in general, seedling growth of all tested species was markedly inhibited when applied concentration of the EO and its constituents reached 0.05 mg/mL. Our results also indicated that constituents other than the dominant compounds of MVEO possessed considerable phytotoxic effects because the EO's activity was stronger than its major constituents and their mixture. Thus, additional studies are required to investigate MVEO and its constituents and commercialize them as environment-friendly bio-herbicides.


Asunto(s)
Amaranthus , Lolium , Mentha , Aceites Volátiles , Poa , Aceites Volátiles/química , Aceites Volátiles/farmacología , Aceites Volátiles/aislamiento & purificación , Amaranthus/efectos de los fármacos , Amaranthus/crecimiento & desarrollo , Amaranthus/química , Mentha/química , Poa/efectos de los fármacos , Lolium/efectos de los fármacos , Hojas de la Planta/química , Cromatografía de Gases y Espectrometría de Masas , Plantones/efectos de los fármacos , Herbicidas/química , Herbicidas/farmacología , Herbicidas/aislamiento & purificación , Tallos de la Planta/química
3.
Cell Mol Biol (Noisy-le-grand) ; 67(5): 27-37, 2022 Feb 04.
Artículo en Inglés | MEDLINE | ID: mdl-35818275

RESUMEN

Fenbfen is used for pain, pyrexia and in the management of osteoarthritis, rheumatoid arthritis and other musculoskeletal disorders. The present research was planned to examine the immunomodulatory activity of fenbufen in different models of cell-mediated immunity (CMI) and humoral immunity (HI). The CMI was evaluated by delayed-type hypersensitivity (DTH) and cyclophosphamide-induced neutropenia assays while HI was appraised by hemagglutination (HA) assay by administering fenbufen at 2, 6 and 10 mg.kg-1 and azathioprine 40 mg.kg-1 (as standard therapy) to albino mice by intraperitoneal route. The ex vivo immunomodulatory action was determined by red blood cell (RBC) membrane stabilization and protein denaturation assays. The results showed that fenbufen treatment had significantly (p<0.05-p<0.001) reduced white blood cells, hemoglobin content, and red blood cells in the healthy and neutropenic mice. A significant (p<0.001) reduction in activities of superoxide dismutase and catalase and glutathione contents, and enhancement of malondialdehyde level were observed in neutropenic mice that were restored by fenbufen treatment. It suppressed DTH reaction after 24, 48 and 72 h post topical application of 2, 4-dinitrofluorobenzene (DNFB). Fenbufen or azathioprine treated groups also showed a significant reduction in the antibody titer against human RBCs induced immune activation in mice as compared to the disease control mice. Fenbufen showed IC50 of 14.0, 50.5 and 66.2 µg.ml-1 whereas, diclofenac sodium showed IC50 of 61.0, 126 and 50.5 µg/ml in RBCs membrane stabilization, egg albumin and bovine serum albumin denaturation assays respectively. The current study shows that fenbufen might have potential immunomodulatory activity against CMI and HI. It can be utilized to treat immune system disorders.


Asunto(s)
Hipersensibilidad Tardía , Animales , Azatioprina/efectos adversos , Humanos , Hipersensibilidad Tardía/inducido químicamente , Hipersensibilidad Tardía/tratamiento farmacológico , Inmunidad Celular , Inmunidad Humoral , Ratones , Fenilbutiratos
4.
Int J Mol Sci ; 23(5)2022 Mar 05.
Artículo en Inglés | MEDLINE | ID: mdl-35269998

RESUMEN

Breast cancer is one of the most common types of cancer among women globally. It is caused by mutations in the estrogen/progesterone receptors and conventional treatment methods are commonly utilized. About 70-80 percent of individuals with the early-stage non-metastatic disease may be cured. Conventional treatment is far less than the optimal ratio, as demonstrated through the high mortality rate of women with this cancer. However, conventional treatment methods like surgery, radiotherapy, and chemotherapy are not as effective as expected and lead to concerns about low bioavailability, low cellular uptake, emerging resistance, and adverse toxicities. A nanomedicine-based approach is a promising alternative for breast cancer treatment. The present era is witnessing rapid advancements in nanomedicine as a platform for investigating novel therapeutic applications and modern intelligent healthcare management strategies. This paper focuses on nanomedicine-based therapeutic interventions that are becoming more widely accepted for improving treatment effectiveness and reducing undesired side effects in breast cancer patients. By evaluating the state-of-the-art tools and taking the challenges involved into consideration, various aspects of the proposed nano-enabled therapeutic approaches have been discussed in this review.


Asunto(s)
Antineoplásicos , Neoplasias de la Mama , Nanopartículas , Antineoplásicos/uso terapéutico , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/genética , Sistemas de Liberación de Medicamentos , Femenino , Humanos , Nanomedicina/métodos
5.
Molecules ; 27(4)2022 Feb 16.
Artículo en Inglés | MEDLINE | ID: mdl-35209111

RESUMEN

The recent study investigated the in vitro anti-diabetic impact of the crude extract (MeOH) and subfractions ethyl acetate (EtOAc); chloroform; n-butanol; n-hexane; and aqueous fraction of S. edelbergii and processed the active EtOAc fraction for the identification of chemical constituents for the first time via ESI-LC-MS analysis through positive ionization mode (PIM) and negative ionization mode (NIM); the identified compounds were further validated through computational analysis via standard approaches. The crude extract and subfractions presented appreciable activity against the α-glucosidase inhibitory assay. However, the EtOAc fraction with IC50 = 0.14 ± 0.06 µg/mL revealed the maximum potential among the fractions used, followed by the MeOH and n-hexane extract with IC50 = 1.47 ± 0.14 and 2.18 ± 0.30 µg/mL, respectively. Moreover, the acarbose showed an IC50 = 377.26 ± 1.20 µg/ mL whereas the least inhibition was observed for the chloroform fraction, with an IC50 = 23.97 ± 0.14 µg/mL. Due to the significance of the EtOAc fraction, when profiled for its chemical constituents, it presented 16 compounds among which the flavonoid class was dominant, and offered eight compounds, of which six were identified in NIM, and two compounds in PIM. Moreover, five terpenoids were identified-three and two in NIM and PIM, respectively-as well as two alkaloids, both of which were detected in PIM. The EtOAc fraction also contained one phenol that was noticed in PIM. The detected flavonoids, terpenoids, alkaloids, and phenols are well-known for their diverse biomedical applications. The potent EtOAc fraction was submitted to computational analysis for further validation of α-glucosidase significance to profile the responsible compounds. The pharmacokinetic estimations and protein-ligand molecular docking results with the support of molecular dynamic simulation trajectories at 100 ns suggested that two bioactive compounds-dihydrocatalpol and leucosceptoside A-from the EtOAc fraction presented excellent drug-like properties and stable conformations; hence, these bioactive compounds could be potential inhibitors of alpha-glucosidase enzyme based on intermolecular interactions with significant residues, docking score, and binding free energy estimation. The stated findings reflect that S. edelbergii is a rich source of bioactive compounds offering potential cures for diabetes mellitus; in particular, dihydrocatalpol and leucosceptoside A could be excellent therapeutic options for the progress of novel drugs to overcome diabetes mellitus.


Asunto(s)
Descubrimiento de Drogas , Inhibidores de Glicósido Hidrolasas/química , Inhibidores de Glicósido Hidrolasas/farmacología , Modelos Moleculares , Extractos Vegetales/química , Extractos Vegetales/farmacología , Scutellaria/química , Fraccionamiento Químico , Cromatografía Liquida , Descubrimiento de Drogas/métodos , Activación Enzimática/efectos de los fármacos , Inhibidores de Glicósido Hidrolasas/aislamiento & purificación , Hipoglucemiantes/química , Hipoglucemiantes/aislamiento & purificación , Hipoglucemiantes/farmacología , Ligandos , Simulación del Acoplamiento Molecular , Simulación de Dinámica Molecular , Estructura Molecular , Extractos Vegetales/aislamiento & purificación , Espectrometría de Masa por Ionización de Electrospray , Relación Estructura-Actividad , Espectrometría de Masas en Tándem
6.
Molecules ; 27(16)2022 Aug 15.
Artículo en Inglés | MEDLINE | ID: mdl-36014440

RESUMEN

The present analysis explores the chemical constituents and determines the in vitro antimicrobial, antidiabetic, and antioxidant significance of the essential oils (EOs) of the stem, leaves, and flowers of Ochradenus arabicus for the first time. The EOs of the flowers presented seventy-four constituents contributing to 81.46% of the total EOs, with the major compounds being 24-norursa-3,12-diene (13.06%), 24-norursa-3,12-dien-11-one (6.61%), and 24-noroleana-3,12-diene (6.25%). The stem EOs with sixty-one compounds contributed 95.95% of the total oil, whose main bioactive compounds were (+)-camphene (21.50%), eremophilene (5.87%), and δ-selinene (5.03%), while a minimum of fifty-one compounds in the leaves' EOs (98.75%) were found, with the main constituents being n-hexadecanoic acid (12.32%), octacosane (8.62%), tetradecanoic acid (8.54%), and prehydro fersenyl acetone (7.27%). The antimicrobial activity of the EOs of O. arabicus stem, leaves, and flowers was assessed against two bacterial strains (Escherichia coli and Streptococcus aureus) and two fungal strains (Penicillium simplicissimum and Rhizoctonia solani) via the disc diffusion assay. However, the EOs extracted from the stem were found effective against one bacterial strain, E. coli, and one fungal strain, R. Solani, among the examined microbes in comparison to the standard and negative control. The tested EOs samples of the O. arabicus stem displayed a maximum potential to cure diabetes with an IC50 = 0.40 ± 0.10 µg/mL, followed by leaves and flowers with an IC50 = 0.71 ± 0.11 µg/mL and IC50 = 10.57 ± 0.18 µg/mL, respectively, as compared to the standard acarbose (IC50 = 377.26 ± 1.20 µg/mL). In addition, the EOs of O. arabicus flowers had the highest antioxidant activity (IC50 = 106.40 ± 0.19 µg/mL) as compared to the standard ascorbic acid (IC50 = 73.20 ± 0.17 µg/mL) using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. In the ABTS assay, the EOs of the same sample (flower) depicted the utmost potential to scavenge the free radicals with an IC50 = 178.0 ± 0.14 µg/mL as compared with the ascorbic acid, having an IC50 of 87.34 ± 0.10 µg/mL the using 2,2-Azino-Bis-3-Ethylbenzothiazoline-6-Sulfonic acid (ABTS) assay. The EOs of all parts of O. arabicus have useful bioactive components due to which they present antidiabetic and antioxidant significance. Furthermore, additional investigations are considered necessary to expose the responsible components of the examined biological capabilities, which would be effective in the production of innovative drugs.


Asunto(s)
Aceites Volátiles , Resedaceae , Antibacterianos/química , Antioxidantes/química , Ácido Ascórbico/análisis , Bacterias , Escherichia coli , Flores/química , Hipoglucemiantes/farmacología , Odorantes , Aceites Volátiles/química
7.
Molecules ; 27(3)2022 Jan 27.
Artículo en Inglés | MEDLINE | ID: mdl-35164093

RESUMEN

Cosmetic-containing herbals are a cosmetic that has or is claimed to have medicinal properties, with bioactive ingredients purported to have medical benefits. There are no legal requirements to prove that these products live up to their claims. The name is a combination of "cosmetics" and "pharmaceuticals". "Nutricosmetics" are related dietary supplements or food or beverage products with additives that are marketed as having medical benefits that affect appearance. Cosmetic-containing herbals are topical cosmetic-pharmaceutical hybrids intended to enhance the health and beauty of the skin. Cosmetic-containing herbals improve appearance by delivering essential nutrients to the skin. Several herbal products, such as cosmetic-containing herbals, are available. The present review highlights the use of natural products in cosmetic-containing herbals, as natural products have many curative effects as well as healing effects on skin and hair growth with minimal to no side effects. A brief description is given on such plants, their used parts, active ingredients, and the therapeutic properties associated with them. Mainly, the utilization of phytoconstituents as cosmetic-containing herbals in the care of skin and hair, such as dryness of skin, acne, eczema, inflammation of the skin, aging, hair growth, and dandruff, along with natural ingredients, such as for hair colorant, are explained in detail in the present review.


Asunto(s)
Productos Biológicos/uso terapéutico , Cosmecéuticos/uso terapéutico , Cosméticos/uso terapéutico , Envejecimiento de la Piel/efectos de los fármacos , Enfermedades de la Piel/tratamiento farmacológico , Piel/metabolismo , Humanos
8.
Molecules ; 26(19)2021 Oct 02.
Artículo en Inglés | MEDLINE | ID: mdl-34641542

RESUMEN

Cancer is the second leading cause of death in the world. Chemotherapy and radiotherapy (RT) are the common cancer treatments. In addition to these limitations, the development of adverse effects from chemotherapy and RT reduces the quality of life for cancer patients. Cellular radiosensitivity, or the ability to resist and overcome cell damage caused by ionizing radiation (IR), is directly related to cancer cells' response to RT. Therefore, radiobiological research is emphasizing chemical compounds 'radiosensitization of cancer cells so that they are more reactive in the IR spectrum. Recent years researchers have seen an increase in interest in natural products that have antitumor effects with minimal side effects. Natural products, on the other hand, are easy to recover and therefore less expensive. There have been several scientific studies done based on these compounds that have tested their ability in vitro and in vivo to induce tumor radiosensitization. The role of natural products in RT, as well as their usefulness and potential applications, is the goal of this current review.


Asunto(s)
Productos Biológicos/farmacología , Radioterapia/efectos adversos , Berberina/farmacología , Curcumina/farmacología , Emodina/farmacología , Genisteína/farmacología , Humanos , Neoplasias/radioterapia , Triterpenos Pentacíclicos/farmacología , Protectores contra Radiación/farmacología , Fármacos Sensibilizantes a Radiaciones/farmacología , Resveratrol/farmacología , Sesquiterpenos/farmacología , Triterpenos/farmacología , Vitamina D/farmacología , Witanólidos/farmacología , Ácido Ursólico
9.
Molecules ; 26(12)2021 Jun 19.
Artículo en Inglés | MEDLINE | ID: mdl-34205312

RESUMEN

In the current study, in vitro antimicrobial and antioxidant activities and in vivo anti-inflammatory and analgesic activities of Scutellaria edelbergii Rech. f. (crude extract and subfractions, i.e., n-hexane, ethyl acetate (EtOAc), chloroform, n-butanol (n-BuOH) and aqueous) were explored. Initially, extraction and fractionation of the selected medicinal plant were carried out, followed by phytochemical qualitative tests, which were mostly positive for all the extracts. EtOAc fraction possessed a significant amount of phenolic (79.2 ± 0.30 mg GAE/g) and flavonoid (84.0 ± 0.39 mg QE/g) content. The EtOAc fraction of S. edelbergii exhibited appreciable antibacterial activity against Gram-negative (Escherichia coli and Klebsiella pneumoniae) strains and significant zones of inhibition were observed against Gram-positive bacterial strains (Bacillus subtilis and Staphylococcus aureus). However, it was found inactive against Candida Albicans and Fusarium oxysporum fungal strains. The chloroform fraction was the most effective with an IC50 value of 172 and 74 µg/mL against DPPH (1,1-Diphenyl-2-picryl-hydrazyl) and ABTS assays, in comparison with standard ascorbic acid 59 and 63 µg/mL, respectively. Moreover, the EtOAc fraction displayed significant in vivo anti-inflammatory activity (54%) using carrageenan-induced assay and significant (55%) in vivo analgesic activity using acetic acid-induced writing assay. In addition, nine known compounds, ursolic acid (UA), ovaul (OV), oleanolic acid (OA), ß-sitosterol (BS), micromeric acid (MA), taraxasterol acetate (TA), 5,3',4'-trihydroxy-7-methoxy flavone (FL-1), 5,7,4'-trihydroxy-6,3'-dimiethoxyflavone (FL-2) and 7-methoxy catechin (FL-3), were isolated from methanolic extract of S. edelbergii. These constituents have never been obtained from this source. The structures of all the isolated constituents were elucidated by spectroscopic means. In conclusion, the EtOAc fraction and all other fractions of S. edelbergii, in general, displayed a significant role as antibacterial, free radical scavenger, anti-inflammatory and analgesic agents which may be due to the presence of these constituents and other flavonoids.


Asunto(s)
Extractos Vegetales/farmacología , Scutellaria/química , Antibacterianos/química , Antibacterianos/farmacología , Antiinflamatorios/farmacología , Antifúngicos/farmacología , Antioxidantes/farmacología , Investigación Biomédica/métodos , Flavonoides/farmacología , Hongos/efectos de los fármacos , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Fenoles/farmacología , Fitoquímicos/farmacología , Plantas Medicinales/química
10.
Molecules ; 26(24)2021 Dec 18.
Artículo en Inglés | MEDLINE | ID: mdl-34946757

RESUMEN

The current study aimed to explore the crude oils obtained from the n-hexane fraction of Scutellaria edelbergii and further analyzed, for the first time, for their chemical composition, in vitro antibacterial, antifungal, antioxidant, antidiabetic, and in vivo anti-inflammatory, and analgesic activities. For the phytochemical composition, the oils proceeded to gas chromatography-mass spectrometry (GC-MS) analysis and from the resultant chromatogram, 42 bioactive constituents were identified. Among them, the major components were linoleic acid ethyl ester (19.67%) followed by ethyl oleate (18.45%), linolenic acid methyl ester (11.67%), and palmitic acid ethyl ester (11.01%). Tetrazolium 96-well plate MTT assay and agar-well diffusion methods were used to evaluate the isolated oil for its minimum inhibitory concentrations (MIC), minimum bactericidal concentration (MBC), half-maximal inhibitory concentrations (IC50), and zone of inhibitions that could determine the potential antimicrobial efficacy's. Substantial antibacterial activities were observed against the clinical isolates comprising of three Gram-negative bacteria, viz., Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa, and one Gram-positive bacterial strain, Enterococcus faecalis. The oils were also effective against Candida albicans and Fusarium oxysporum when evaluated for their antifungal potential. Moreover, significant antioxidant potential with IC50 values of 136.4 and 161.5 µg/mL for extracted oil was evaluated through DPPH (1,1-Diphenyl-2-picryl-hydrazyl) and ABTS assays compared with standard ascorbic acid where the IC50 values were 44.49 and 67.78 µg/mL, respectively, against the tested free radicals. The oils was also potent, inhibiting the α-glucosidase (IC50 5.45 ± 0.42 µg/mL) enzyme compared to the standard. Anti-glucosidase potential was visualized through molecular docking simulations where ten compounds of the oil were found to be the leading inhibitors of the selected enzyme based on interactions, binding energy, and binding affinity. The oil was found to be an effective anti-inflammatory (61%) agent compared with diclofenac sodium (70.92%) via the carrageenan-induced assay. An appreciable (48.28%) analgesic activity in correlation with the standard aspirin was observed through the acetic acid-induced writhing bioassay. The oil from the n-hexane fraction of S. edelbergii contained valuable bioactive constituents that can act as in vitro biological and in vivo pharmacological agents. However, further studies are needed to uncover individual responsible compounds of the observed biological potentials which would be helpful in devising novel drugs.


Asunto(s)
Antibacterianos/análisis , Antifúngicos/análisis , Antioxidantes/análisis , Inhibidores de Glicósido Hidrolasas/análisis , Aceites de Plantas/análisis , Scutellaria/química , Animales , Antibacterianos/farmacología , Antifúngicos/farmacología , Antioxidantes/farmacología , Benzotiazoles/antagonistas & inhibidores , Compuestos de Bifenilo/antagonistas & inhibidores , Carragenina , Edema/inducido químicamente , Edema/tratamiento farmacológico , Hongos/efectos de los fármacos , Cromatografía de Gases y Espectrometría de Masas , Inhibidores de Glicósido Hidrolasas/farmacología , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Hexanos/química , Humanos , Ratones , Pruebas de Sensibilidad Microbiana , Simulación del Acoplamiento Molecular , Picratos/antagonistas & inhibidores , Aceites de Plantas/farmacología , Plantas Medicinales , Ácidos Sulfónicos/antagonistas & inhibidores , alfa-Glucosidasas/metabolismo
11.
Molecules ; 26(16)2021 Aug 18.
Artículo en Inglés | MEDLINE | ID: mdl-34443593

RESUMEN

Curcuma longa is very well-known medicinal plant not only in the Asian hemisphere but also known across the globe for its therapeutic and medicinal benefits. The active moiety of Curcuma longa is curcumin and has gained importance in various treatments of various disorders such as antibacterial, antiprotozoal, cancer, obesity, diabetics and wound healing applications. Several techniques had been exploited as reported by researchers for increasing the therapeutic potential and its pharmacological activity. Here, the dictum is the new room for the development of physicochemical, as well as biological, studies for the efficacy in target specificity. Here, we discussed nanoformulation techniques, which lend support to upgrade the characters to the curcumin such as enhancing bioavailability, increasing solubility, modifying metabolisms, and target specificity, prolonged circulation, enhanced permeation. Our manuscript tried to seek the attention of the researcher by framing some solutions of some existing troubleshoots of this bioactive component for enhanced applications and making the formulations feasible at an industrial production scale. This manuscript focuses on recent inventions as well, which can further be implemented at the community level.


Asunto(s)
Curcumina/química , Curcumina/uso terapéutico , Terapia Molecular Dirigida/métodos , Nanomedicina/métodos , Nanopartículas , Animales , Humanos
12.
Molecules ; 26(17)2021 Aug 26.
Artículo en Inglés | MEDLINE | ID: mdl-34500597

RESUMEN

Breast cancer persists as a diffuse source of cancer despite persistent detection and treatment. Flavonoids, a type of polyphenol, appear to be a productive option in the treatment of breast cancer, because of their capacity to regulate the tumor related functions of class of compounds. Plant polyphenols are flavonoids that appear to exhibit properties which are beneficial for breast cancer therapy. Numerous epidemiologic studies have been performed on the dynamic effect of plant polyphenols in the prevention of breast cancer. There are also subclasses of flavonoids that have antioxidant and anticarcinogenic activity. These can regulate the scavenging activity of reactive oxygen species (ROS) which help in cell cycle arrest and suppress the uncontrolled division of cancer cells. Numerous studies have also been performed at the population level, one of which reported a connection between cancer risk and intake of dietary flavonoids. Breast cancer appears to show intertumoral heterogeneity with estrogen receptor positive and negative cells. This review describes breast cancer, its various factors, and the function of flavonoids in the prevention and treatment of breast cancer, namely, how flavonoids and their subtypes are used in treatment. This review proposes that cancer risk can be reduced, and that cancer can be even cured by improving dietary intake. A large number of studies also suggested that the intake of fruit and vegetables is associated with reduced breast cancer and paper also includes the role and the use of nanodelivery of flavonoids in the healing of breast cancer. In addition, the therapeutic potential of orally administered phyto-bioactive compounds (PBCs) is narrowed because of poor stability and oral bioavailability of compounds in the gastrointestinal tract (GIT), and solubility also affects bioavailability. In recent years, creative nanotechnology-based approaches have been advised to enhance the activity of PBCs. Nanotechnology also offers the potential to become aware of disease at earlier stages, such as the detection of hidden or unconcealed metastasis colonies in patients diagnosed with lung, colon, prostate, ovarian, and breast cancer. However, nanoformulation-related effects and safety must not be overlooked. This review gives a brief discussion of nanoformulations and the effect of nanotechnology on herbal drugs.


Asunto(s)
Neoplasias de la Mama/tratamiento farmacológico , Flavonoides/farmacología , Nanopartículas/administración & dosificación , Animales , Antioxidantes/farmacología , Disponibilidad Biológica , Neoplasias de la Mama/metabolismo , Femenino , Frutas/química , Humanos , Polifenoles/farmacología , Especies Reactivas de Oxígeno/metabolismo , Verduras/química
13.
Molecules ; 26(23)2021 Nov 24.
Artículo en Inglés | MEDLINE | ID: mdl-34885693

RESUMEN

Curcumin is the primary polyphenol in turmeric's curcuminoid class. It has a wide range of therapeutic applications, such as anti-inflammatory, antioxidant, antidiabetic, hepatoprotective, antibacterial, and anticancer effects against various cancers, but has poor solubility and low bioavailability. Objective: To improve curcumin's bioavailability, plasma concentration, and cellular permeability processes. The nanocurcumin approach over curcumin has been proven appropriate for encapsulating or loading curcumin (nanocurcumin) to increase its therapeutic potential. Conclusion: Though incorporating curcumin into nanocurcumin form may be a viable method for overcoming its intrinsic limitations, and there are reasonable concerns regarding its toxicological safety once it enters biological pathways. This review article mainly highlights the therapeutic benefits of nanocurcumin over curcumin.


Asunto(s)
Enfermedad Crónica/tratamiento farmacológico , Curcumina/uso terapéutico , Antibacterianos/uso terapéutico , Antiinflamatorios/química , Antiinflamatorios/uso terapéutico , Disponibilidad Biológica , Enfermedad Crónica/prevención & control , Curcumina/análogos & derivados , Curcumina/química , Humanos , Nanopartículas/química , Nanopartículas/uso terapéutico , Nanotecnología , Solubilidad
14.
Phytomedicine ; 133: 155928, 2024 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-39126924

RESUMEN

BACKGROUND: The Scutellaria genus has promising therapeutic capabilities as an aromatherapy. Based on that and local practices of S. nuristanica Rech. F. The essential oil was studied for the first time for its diverse biomedical applications. PURPOSE: This study aimed to evaluate and validate their therapeutic capabilities by screening the essential oil ingredients and examining their antimicrobial, antioxidant, carbonic anhydrase, and antidiabetic using further In silico assessment and In vivo anti-inflammatory and analgesic capabilities to devise novel sources as natural remedies alternative to the synthetic drugs. METHODS: Essential oil was obtained through hydrodistillation, and the constituents were profiled using GC-MS. The antimicrobial assessment was conducted using an agar well diffusion assay. Free radical scavenging capabilities were determined by employing DPPH and ABTS assay. The carbonic anhydrase-II was examined using colorimetric assay, while the antidiabetic significance was performed using α-Glucosidase assay. The anti-inflammatory significance was examined through carrageenan-induced paw edema, and the analgesic features of the essential oil were determined using an acetic acid-induced writhing assay. RESULTS: Fifty constituents were detected in S. nuristanica essential oil (SNEO), contributing 95.93 % of the total EO, with the predominant constituents being 24-norursa-3,12-diene (10.12 %), 3-oxomanoyl oxide (9.94 %), methyl 7-abieten-18-oate (8.85 %). SNEO presented significance resistance against the Gram-positive bacterial strains (GPBSs), Bacillus atrophaeus and Bacillus subtilis, as compared to the Salmonella typhi and Klebsiella pneumoniae, Gram-negative bacterial strains (GNBSs) as well as two fungal strains Aspergillus parasiticus and Aspergillus niger associated with their respective standards. Considerable free radical scavenging capacity was observed in DPPH compared to the ABTS assay when correlated with ascorbic acid. In addition, when equated with their standards, SNEO offered considerable in vitro carbonic anhydrase II and antidiabetic capabilities. Additionally, the antidiabetic behavior of the 9 dominant compounds of SNEO was tested via In silico techniques, such as molecular docking, which assisted in the assessment of the significance of binding contacts of protein with each chemical compound and pharmacokinetic evaluations to examine the drug-like characteristics. Molecular dynamic simulations at 100 ns and binding free energy evaluations such as PBSA and GBSA models explain the molecular mechanics and stability of molecular complexes. It was also observed that SNEO depicted substantial anti-inflammatory and analgesic capabilities. CONCLUSION: Hence, it was concluded that the SNEO comprises bioactive ingredients with biomedical significance, such as anti-microbial, antioxidant, CA-II, antidiabetic, anti-inflammatory, and analgesic agents. The computational validation also depicted that SNEO could be a potent source for the discovery of anti-diabetic drugs.


Asunto(s)
Antiinflamatorios , Antioxidantes , Edema , Hipoglucemiantes , Aceites Volátiles , Scutellaria , Animales , Scutellaria/química , Antioxidantes/farmacología , Antioxidantes/química , Antiinflamatorios/farmacología , Antiinflamatorios/química , Aceites Volátiles/farmacología , Aceites Volátiles/química , Hipoglucemiantes/farmacología , Hipoglucemiantes/química , Edema/tratamiento farmacológico , Analgésicos/farmacología , Analgésicos/química , Masculino , Ratones , Simulación del Acoplamiento Molecular , Carragenina , Cromatografía de Gases y Espectrometría de Masas , Antiinfecciosos/farmacología , Antiinfecciosos/química , Aromaterapia/métodos , Antibacterianos/farmacología , Antibacterianos/química
15.
Sci Rep ; 13(1): 20455, 2023 11 22.
Artículo en Inglés | MEDLINE | ID: mdl-37993472

RESUMEN

Arsenic (As), contamination in drinking groundwater resources is commonly environmental problem in many developing countries including Pakistan, with significant human health risk reports. In order to examine the groundwater quality concerning As contamination, its geochemical behavior along with physicochemical parameters, 42 samples were collected from community tube wells from District Bahawalpur, Punjab, Pakistan. The results showed the concentration of elevated As, its source of mobilization, and associated public health risk. The As concentration detected in groundwater samples varied from 0.12 to 104 µg/L with an average value of 34.7 µg/L. Among 42 groundwater samples, 27 samples were beyond the permitted limit of 10 µg/L recommended by World Health Organization (WHO), for drinking purposes. Statistical analysis result show that the groundwater cations values are in decreasing order such as: Na+ > Mg2+ > Ca2+ > K+, while anions were HCO3- > SO42- > Cl- > NO3-. Hydrochemical facies result depict that the groundwater samples of the study area, 14 samples belong to CaHCO3 type, 5 samples belong to NaCl type, 20 samples belong to Mixed CaMgCl type, and 3 samples belong to CaCl2 type. It can be accredited due to weathering and recharge mechanism, evaporation processes, and reverse ion exchange. Gibbs diagram shows that rock water interaction controls the hydrochemistry of groundwater resources of the study area. Saturation Index (SI) result indicated the saturation of calcite, dolomite, gypsum, geothite, and hematite mineral due their positive SI values. The principal component analysis (PCA) results possess a total variability of 80.69% signifying the anthropogenic and geogenic source of contamination. The results of the exposure-health-risk-assessment method for measuring As reveal significant potential non-carcinogenic risk (HQ), exceeding the threshold level of (> 1) for children in the study area. Water quality assessment results shows that 24 samples were not suitable for drinking purposes.


Asunto(s)
Arsénico , Agua Potable , Agua Subterránea , Contaminantes Químicos del Agua , Niño , Humanos , Calidad del Agua , Monitoreo del Ambiente , Arsénico/análisis , Contaminantes Químicos del Agua/análisis , Agua Subterránea/análisis , Agua Potable/análisis
16.
Sci Rep ; 13(1): 10961, 2023 07 06.
Artículo en Inglés | MEDLINE | ID: mdl-37415093

RESUMEN

Sitotroga cerealella is one of the major pests of cereals in the field and storage conditions throughout the world. The main objective was to study the life tables of S. cerealella on wheat, maize and barley and its implications on percent parasitism of Trichogramma chilonis. S. cerealella is reared under lab conditions as its eggs are utilized for rearing T. chilonis. Fresh eggs of S. cerealella were collected and after hatching the neonate larvae of S. cerealella were transferred onto each host plant species for obtaining first (F1) generation (G). Seventy eggs were used for each host and each egg was used as a replicate. Daily observations were made for recording the life-table parameters of the S. cerealella. The data showed that the developmental time of S. cerealella eggs and pupae was maximum (5.68 and 7.75 days) when reared on wheat, while the maximum larval duration (19.77 days) of S. cerealella was recorded on barley. The maximum fecundity (290.30 ± 22.47 eggs/female) was recorded on maize, while minimum fecundity per female was recorded on barley (159.30 eggs/ female). The S. cerealella reared on maize had significantly higher values of finite rate of increase (λ), intrinsic rate of increase (r), and net reproductive rate (Ro) (0.14 ± 0.04 day- 1, 1.16 ± 0.05 day- 1, and 136.85 ± 20.25 eggs/ female) respectively. The mean generation time (T) (35.18 ± 0.61 days) was higher on wheat. Likewise, the gross reproductive rate (GRR) and the age-stage specific reproductive values (vxj) of newly oviposited eggs of S. cerealella were recorded higher (136.85 ± 20.25; 1.160 offspring) on maize. The data regarding the efficacy of T. chilonis for different parameters were recorded higher on maize i.e., percent parasitism (89.00 ± 2.30%), percent adult emergence (81.60 ± 1.20%), adult longevity (3.80 ± 0.10 days) and total adult longevity (9.90 ± 0.20 days) as compared to wheat and barley. Our findings revealed that S. cerealella can be best reared on maize under laboratory conditions as it prefers this host as compared to wheat and barley. Therefore, assigning the most susceptible and favorite host (maize) would help us to improve T. chilonis mass production under laboratory conditions.


Asunto(s)
Himenópteros , Mariposas Nocturnas , Avispas , Animales , Femenino , Humanos , Recién Nacido , Grano Comestible , Tablas de Vida , Larva , Triticum , Zea mays
17.
Antioxidants (Basel) ; 12(3)2023 Mar 07.
Artículo en Inglés | MEDLINE | ID: mdl-36978910

RESUMEN

The present study explored Euphorbia larica essential oil (ELEO) constituents for the first time, obtained via hydro-distillation by means of Gas Chromatography-Mass Spectrometry (GC-MS) profiling. The essential oil was screened in vitro against breast cancer cells, normal cell lines, α-glucosidase, carbonic anhydrase-II (CA-II), free radical scavenging and in vivo analgesic and anti-inflammatory capabilities. The GC-MS screening revealed that the ELEO comprises sixty compounds (95.25%) with the dominant constituents being camphene (16.41%), thunbergol (15.33%), limonene (4.29%), eremophilene (3.77%), and ß-eudesmol (3.51%). A promising antidiabetic capacity was noticed with an IC50 of 9.63 ± 0.22 µg/mL by the ELEO as equated to acarbose with an IC50 = 377.71 ± 1.34 µg/mL, while a 162.82 ± 1.24 µg/mL inhibition was observed against CA-II. Regarding breast cancer, the ELEO offered considerable cytotoxic capabilities against the triple-negative breast cancer (MDA-MB-231) cell lines, having an IC50 = 183.8 ± 1.6 µg/mL. Furthermore, the ELEO was also tested with the human breast epithelial (MCF-10A) cell line, and the findings also presumed that the ELEO did not produce any damage to the tested normal cell lines. The ELEO was effective against the Gram-positive bacteria and offered a 19.8 ± 0.02 mm zone of inhibition (ZOI) against B. atrophaeus. At the same time, the maximum resistance with 18.03 ± 0.01 mm ZOI against the fungal strain Aspergillus parasiticus was observed among the tested fungal strains. An appreciable free radical significance was observed via the DPPH assay with an IC50 = 133.53 ± 0.19 µg/mL as equated to the ABTS assay having an IC50 = 154.93 ± 0.17 µg/mL. The ELEO also offered a substantial analgesic capacity and produced 58.33% inhibition in comparison with aspirin, a 68.47% decrease in writhes, and an anti-inflammatory capability of 65.54% inhibition, as equated to the standard diclofenac sodium having 73.64% inhibition. Hence, it was concluded that the ELEO might be a natural source for the treatment of diabetes mellitus, breast cancer, analgesic, inflammatory, and antimicrobial-related diseases. Moreover, additional phytochemical and pharmacological studies are needed to isolate responsible chemical ingredients to formulate new drugs for the examined activities.

18.
Sci Rep ; 13(1): 11969, 2023 07 24.
Artículo en Inglés | MEDLINE | ID: mdl-37488190

RESUMEN

The current study regarding the effects of larval diets on the life table parameters of dengue mosquitoes, Aedes aegypti was conducted under laboratory conditions at 27 ± 2 °C and 60 ± 5% relative humidity at NIFA (Nuclear Institute for Food and Agriculture) Peshawar, Pakistan. The data on life table parameters of Ae. aegypti reared on Diet 1 (replacement diet), Diet 2 (Khan's diet for Anopheles), Diet 3 (Khan's modified diet) and Diet 4 (IAEA diet) were analyzed using the age-stage, two-sex life table software. Diet 4 (IAEA) was used as a control for comparison. The results indicated that significantly maximum percentage of egg hatching of Ae. aegypti was observed when reared on Diet 4 (73.86%) and Diet 3 (72.90%), while less % of egg hatching was recorded in Diet 1 (40.67%) and Diet 2 (55.53%). The data further showed that the Diet 3 had a highest intrinsic rate of increase (r) (0.097 ± 5.68 day-1), finite rate of increase (λ) (1.10 ± 6.26 day-1) and net reproductive rate (R0) (11.99 ± 1.52 eggs/female) followed by Diet 2 and Diet 4. The mean generation time (T) of Ae. aegypti reared on Diet 3 (23.67 ± 0.86 days) and Diet 1 (24.05 ± 0.61 days) was significantly shorter than Diet 2 (26.15 ± 0.71 days) and Diet 4 (26.41 ± 0.38 days). The overall results revealed that Diet 3 showed good results at different life table parameters of Ae. aegypti and can be used as the preferred diet in the Sterile Insect Technique (SIT) where the mass culture of mosquitoes is required.


Asunto(s)
Aedes , Dengue , Animales , Femenino , Larva , Tablas de Vida , Dieta , Huevos
19.
Metabolites ; 12(12)2022 Dec 07.
Artículo en Inglés | MEDLINE | ID: mdl-36557265

RESUMEN

Endophytic bacteria boost host plant defense and growth by producing vital compounds. In the current study, a bacterial strain was isolated from the Boswellia sacra plant and identified as Bacillus subtilis strain EP1 (accession number: MT256301) through 16S RNA gene sequencing. From the identified bacteria, four compounds-1 (4-(4-cinnamoyloxy)phenyl)butanoic acid), 2 (cyclo-(L-Pro-D-Tyr)), 3 (cyclo-(L-Val-L-Phe)), and 4 (cyclo-(L-Pro-L-Val))-were isolated and characterized by 1D and 2D NMR and mass spectroscopy. Moreover, antibacterial activity and beta-lactam-producing gene inhibition (δ-(l-α-aminoadipyl)-l-cysteinyl-d-valine synthetase (ACVS) and aminoadipate aminotransferase (AADAT)) assays were performed. Significant antibacterial activity was observed against the human pathogenic bacterial strains (E. coli) by compound 4 with a 13 ± 0.7 mm zone of inhibition (ZOI), followed by compound 1 having an 11 ± 0.7 mm ZOI. In contrast, the least antibacterial activity among the tested samples was offered by compound 2 with a 10 ± 0.9 mm ZOI compared to the standard (26 ± 1.2 mm). Similarly, the molecular analysis of beta-lactam inhibition determined that compounds 3 and 4 inhibited the two genes (2- to 4-fold) in the beta-lactam biosynthesis (ACVS and AADAT) pathway. From these results, it can be concluded that future research on these compounds could lead to the inhibition of antibiotic-resistant pathogenic bacterial strains.

20.
Polymers (Basel) ; 14(13)2022 Jul 01.
Artículo en Inglés | MEDLINE | ID: mdl-35808757

RESUMEN

The emergence of bacterial resistance has increased the economic burden of infectious diseases dramatically during the previous few decades. Multidrug resistance (MDR) is difficult to cure in both Gram-negative and positive bacteria and is often incurable with traditional and broad-range antibiotics. Therefore, developing techniques to increase the antibacterial activity of therapeutic drugs is essential. Metal-organic frameworks (MOFs) are extremely versatile hybrid materials made of metal ions coupled via organic bridging ligands. They have been widely used as an excellent vehicle for drug delivery due to their low toxicity, biodegradability, and structural stability upon loading and functionalization. The present study focused on the synthesis of mannose (MNS)-coated MOFs with enhanced surface contact with S. aureus cells. The MNS coating on the surface of MOFs enhances their adherence to bacteria by binding to lectins present on the bacterial cell, resulting in improved VCM cellular penetration and activity against resistant bacteria. Various techniques, including atomic force microscopy, DLS, TGA, FT-IR, and DSC, were employed to analyze MNS-coated MOFs. They were also evaluated for their efficacy against resistant S. aureus. The results indicated that when VCM was loaded into MNS-coated MOFs, their bactericidal activity rose dramatically, resulting in the greater suppression of resistant S. aureus. AFM investigation of S. aureus strains demonstrated total morphological distortion after treatment with MNS-coated drug-loaded MOFs. The results of this work suggest that MNS-coated MOFs may be effective for reversing bacterial resistance to VCM and open new pathways for improving antibiotic therapy for diseases associated with MDR.

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