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1.
Curr Issues Mol Biol ; 46(3): 2320-2342, 2024 Mar 11.
Artículo en Inglés | MEDLINE | ID: mdl-38534764

RESUMEN

Rare ginsenoside compound K (CK) is an intestinal microbial metabolite with a low natural abundance that is primarily produced by physicochemical processing, side chain modification, or metabolic transformation in the gut. Moreover, CK exhibits potent biological activity compared to primary ginsenosides, which has raised concerns in the field of ginseng research and development, as well as ginsenoside-related dietary supplements and natural products. Ginsenosides Rb1, Rb2, and Rc are generally used as a substrate to generate CK via several bioconversion processes. Current research shows that CK has a wide range of pharmacological actions, including boosting osteogenesis, lipid and glucose metabolism, lipid oxidation, insulin resistance, and anti-inflammatory and anti-apoptosis properties. Further research on the bioavailability and toxicology of CK can advance its medicinal application. The purpose of this review is to lay the groundwork for future clinical studies and the development of CK as a therapy for metabolic disorders. Furthermore, the toxicology and pharmacology of CK are investigated as well in this review. The findings indicate that CK primarily modulates signaling pathways associated with AMPK, SIRT1, PPARs, WNTs, and NF-kB. It also demonstrates a positive therapeutic effect of CK on non-alcoholic fatty liver disease (NAFLD), obesity, hyperlipidemia, diabetes, and its complications, as well as osteoporosis. Additionally, the analogues of CK showed more bioavailability, less toxicity, and more efficacy against disease states. Enhancing bioavailability and regulating hazardous variables are crucial for its use in clinical trials.

2.
Cancer Sci ; 2024 Jun 18.
Artículo en Inglés | MEDLINE | ID: mdl-38888067

RESUMEN

The rhizome of Zingiber officinale (Z. officinale), commonly known as ginger, has been characterized as a potential drug candidate due to its antitumor effects. However, the chemotherapeutic effect of ginger on human oral cancer remains poorly understood. In this study, we examined the effects of an ethanol extract of Z. officinale rhizomes (ZOE) on oral cancer and identified the components responsible for its pharmacological activity. ZOE exerts its inhibitory activity in oral cancer by inducing both autophagy and apoptosis simultaneously. Mechanistically, ZOE-induced autophagy and apoptosis in oral cancer are attributed to the reactive oxygen species (ROS)-mediated endoplasmic reticulum stress response. Additionally, we identified two active components of ZOE, 1-dehydro-6-gingerdione and 8-shogaol, which were sufficient to stimulate autophagy initiation and apoptosis induction by enhancing CHOP expression. These results suggest that ZOE and its two active components induce ROS generation, upregulate CHOP, initiate autophagy and apoptosis, and hold promising therapeutics against human oral cancer.

3.
Med Sci Monit ; 30: e942899, 2024 Mar 10.
Artículo en Inglés | MEDLINE | ID: mdl-38509819

RESUMEN

BACKGROUND The gut microbial metabolites demonstrate significant activity against metabolic diseases including osteoporosis (OP) and obesity, but active compounds, targets, and mechanisms have not been fully identified. Hence, the current investigation explored the mechanisms of active metabolites and targets against OP and obesity by using network pharmacology approaches. MATERIAL AND METHODS The gutMGene database was used to collect gut microbial targets-associated metabolites; DisGeNET and OMIM databases were used to identify targets relevant to OP and obesity. A total of 63 and 89 overlapped targets were considered the final OP and obesity targets after creating a Venn diagram of metabolites-related targets and disease-related targets. Furthermore, the top 20% of degrees, betweenness, and closeness were used to form the sub-network of protein-protein interaction of these targets. Finally, the biotransformation-increased receptors and biological mechanisms were identified and validated using ADMET properties analysis, molecular docking, and molecular dynamic simulation. RESULTS GO, KEGG pathway analysis, and protein-protein interactions were performed to establish metabolites and target networks. According to the enrichment analysis, OP and obesity are highly linked to the lipid and atherosclerosis pathways. Moreover, ADMET analysis depicts that the major metabolites have drug-likeliness activity and no or less toxicity. Following that, the molecular docking studies showed that compound K and TP53 target have a remarkable negative affinity (-8.0 kcal/mol) among all metabolites and targets for both diseases. Finally, the conformity of compound K against the targeted protein TP53 was validated by 250ns MD simulation. CONCLUSIONS Therefore, we summarized that compound K can regulate TP53 and could be developed as a therapy option for OP and obesity.


Asunto(s)
Medicamentos Herbarios Chinos , Microbioma Gastrointestinal , Ginsenósidos , Osteoporosis , Humanos , Simulación del Acoplamiento Molecular , Farmacología en Red , Biología Computacional , Simulación de Dinámica Molecular , Obesidad/tratamiento farmacológico , Osteoporosis/tratamiento farmacológico
4.
Int J Mol Sci ; 25(5)2024 Mar 04.
Artículo en Inglés | MEDLINE | ID: mdl-38474229

RESUMEN

The prevalence of metabolic syndrome is increasing globally due to behavioral and environmental changes. There are many therapeutic agents available for the treatment of chronic metabolic diseases, such as obesity and diabetes, but the data on their efficacy and safety are lacking. Through a pilot study by our group, Zingiber officinale rhizomes used as a spice and functional food were selected as an anti-obesity candidate. In this study, steam-processed ginger extract (GGE) was used and we compared its efficacy at alleviating metabolic syndrome-related symptoms with that of conventional ginger extract (GE). Compared with GE, GGE (25-100 µg/mL) had an increased antioxidant capacity and α-glucosidase inhibitory activity in vitro. GGE was better at suppressing the differentiation of 3T3-L1 adipocytes and lipid accumulation in HepG2 cells and promoting glucose utilization in C2C12 cells than GE. In 16-week high-fat-diet (HFD)-fed mice, GGE (100 and 200 mg/kg) improved biochemical profiles, including lipid status and liver function, to a greater extent than GE (200 mg/kg). The supplementation of HFD-fed mice with GGE (200 mg/kg) resulted in the downregulation of SREBP-1c and FAS gene expression in the liver. Collectively, our results indicate that GGE is a promising therapeutic for the treatment of obesity and metabolic syndrome.


Asunto(s)
Fármacos Antiobesidad , Síndrome Metabólico , Zingiber officinale , Ratones , Animales , Vapor , Síndrome Metabólico/tratamiento farmacológico , Proyectos Piloto , Tejido Adiposo/metabolismo , Obesidad/metabolismo , Extractos Vegetales/farmacología , Dieta Alta en Grasa , Fármacos Antiobesidad/farmacología , Lípidos/farmacología , Ratones Endogámicos C57BL , Células 3T3-L1 , Adipogénesis
5.
Chem Biodivers ; 20(1): e202200823, 2023 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-36376246

RESUMEN

This research was supported by Cooperative Research Program for Agriculture Science & Technology Development (Project No. PJ014204032019) and the Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education (NRF-2020R1A6A3A01100042).


Asunto(s)
Prunus , Rosaceae , Antioxidantes/farmacología , Flavonoides , Frutas/química , Fenoles/farmacología , Fenoles/análisis
6.
J Environ Manage ; 328: 116969, 2023 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-36495825

RESUMEN

Antibiotic-resistant bacteria and antibiotic resistance genes (ARGs) are pollutants of worldwide concern that seriously threaten public health and ecosystems. Machine learning (ML) prediction models have been applied to predict ARGs in beach waters. However, the existing studies were conducted at a single location and had low prediction performance. Moreover, ML models are "black boxes" that do not reveal their predictions' internal nuances and mechanisms. This lack of transparency and trust can result in serious consequences when using these models in high-stakes decisions. In this study, we developed a gradient boosted regression tree based (GBRT) ML model and then described its behavior using six explainable artificial intelligence (XAI) model-agnostic explanation methods. We used hydro-meteorological and qPCR data from the beaches in South Korea and Pakistan and developed ML prediction models for aac (6'-lb-cr), sul1, and tetX with 10-fold time-blocked cross-validation performances of 4.9, 2.06 and 4.4 root mean squared logarithmic error, respectively. We then analyzed the local and global behavior of the developed ML model using four interpretation methods. The developed ML models showed that water temperature, precipitation and tide are the most important predictors for prediction of ARGs at recreational beaches. We show that the model-agnostic interpretation methods not only explain the behavior of the ML model but also provide insights into the behavior of the ML model under new unseen conditions. Moreover, these post-processing techniques can be a debugging tool for ML-based modeling.


Asunto(s)
Inteligencia Artificial , Ecosistema , Bacterias/genética , Aprendizaje Automático , Farmacorresistencia Microbiana/genética
7.
Molecules ; 28(2)2023 Jan 16.
Artículo en Inglés | MEDLINE | ID: mdl-36677964

RESUMEN

The unique and tailorable physicochemical features of zinc oxide nanoparticles (ZnO-NPs) synthesized from green sources make them attractive for use in cancer treatment. Hydroponic-cultured ginseng-root-synthesized ZnO-NPs (HGRCm-ZnO NPs) were coated with O-carboxymethyl chitosan (CMC) polymer, which stabilized and enhanced the biological efficacy of the nanoparticles. Nanoparticles were characterized by X-ray diffraction (XRD), UV-Vis spectroscopy, transmission electron microscopy (TEM), Fourier-transform infrared spectroscopy (FT-IR), and energy-dispersive X-ray spectroscopy (EDS). The flower-shaped nanoparticles were crystalline in nature with a particle size of 28 nm. To evaluate if these NPs had anti-lung cancer activity, analysis was performed on a human lung carcinoma cell line (A549). HGRCm-ZnO nanoparticles showed less toxicity to normal keratinocytes (HaCaTs), at concentrations up to 20 µg/mL, than A549 cancer cells. Additionally, these NPs showed dose-dependent colony formation and cell migration inhibition ability, which makes them more promising for lung cancer treatment. Additionally, Hoechst and propidium iodide dye staining also confirmed that the NP formulation had apoptotic activity in cancer cells. Further, to evaluate the mechanism of cancer cell death via checking the gene expression, HGRCm ZnO NPs upregulated the BAX and Caspase 3 and 9 expression levels but downregulated Bcl-2 expression, indicating that the nanoformulation induced mitochondrial-mediated apoptosis. Moreover, these preliminary results suggest that HGRCm ZnO NPs can be a potential candidate for future lung cancer treatment.


Asunto(s)
Nanopartículas del Metal , Neoplasias , Panax , Óxido de Zinc , Humanos , Óxido de Zinc/química , Espectroscopía Infrarroja por Transformada de Fourier , Regulación hacia Abajo , Hidroponía , Apoptosis , Línea Celular , Proteínas Proto-Oncogénicas c-bcl-2/genética , Proteínas Proto-Oncogénicas c-bcl-2/metabolismo , Expresión Génica , Panax/metabolismo , Nanopartículas del Metal/uso terapéutico , Nanopartículas del Metal/química , Antibacterianos/farmacología , Difracción de Rayos X , Extractos Vegetales/farmacología , Extractos Vegetales/química
8.
Cell Biol Toxicol ; 38(1): 147-165, 2022 02.
Artículo en Inglés | MEDLINE | ID: mdl-33665778

RESUMEN

Abnormal expression of claudin-1 (CLDN1) has important roles in carcinogenesis and metastasis in various cancers. The role of CLDN1 in human oral squamous cell carcinoma (OSCC) remains unknown. Here, we report the functional role of CLDN1 in metastasis of human OSCC, as a potential target regulated by withaferin A. From gene expression profiling with microarray technology, we found that the majority of notable differentially expressed genes were classified into migration/invasion category. Withaferin A impaired the motility of human OSCC cells in vitro and suppressed metastatic nodule formation in an in vivo metastasis model, both associated with reduced CLDN1. CLDN1 overexpression enhanced metastatic nodule formation in vivo, resulting in severe metastatic lesions in lung tissue. Moreover, CLDN1 expression was positively correlated to lymphatic metastasis in OSCC patients. The impaired motility of human OSCC cells upon withaferin A treatment was restored by CLDN1 overexpression. Furthermore, upregulation of let-7a induced by withaferin A was inversely correlated to CLDN1 expression. Overall, these give us an insight into the function of CLDN1 for prognosis and treatment of human OSCC, substantiating further investigation into the use of withaferin A as good anti-metastatic drug candidate.


Asunto(s)
Carcinoma de Células Escamosas , Neoplasias de Cabeza y Cuello , Neoplasias de la Boca , Carcinoma de Células Escamosas/patología , Línea Celular Tumoral , Movimiento Celular/genética , Claudina-1/genética , Claudina-1/metabolismo , Regulación Neoplásica de la Expresión Génica , Neoplasias de Cabeza y Cuello/genética , Humanos , Neoplasias de la Boca/genética , Neoplasias de la Boca/metabolismo , Neoplasias de la Boca/patología , Carcinoma de Células Escamosas de Cabeza y Cuello/genética , Witanólidos
9.
Molecules ; 27(23)2022 Nov 28.
Artículo en Inglés | MEDLINE | ID: mdl-36500403

RESUMEN

Ginsenoside Rh1 (G-Rh1), a possible bioactive substance isolated from the Korean Panax ginseng Meyer, has a wide range of pharmacological effects. In this study, we have investigated the anticancer efficacy of G-Rh1 via in silico and in vitro methodologies. This study mainly focuses on the two metastatic regulators, Rho-associated protein kinase 1 (ROCK1) and RhoA, along with other standard apoptosis regulators. The ROCK1 protein is a member of the active serine/threonine kinase family that is crucial for many biological processes, including cell division, differentiation, and death, as well as many cellular processes and muscle contraction. The abnormal activation of ROCK1 kinase causes several disorders, whereas numerous studies have also shown that RhoA is expressed highly in various cancers, including colon, lung, ovarian, gastric, and liver malignancies. Hence, inhibiting both ROCK1 and RhoA will be promising in preventing metastasis. Therefore, the molecular level interaction of G-Rh1 with the ROCK1 and RhoA active site residues from the preliminary screening clearly shows its inhibitory potential. Molecular dynamics simulation and principal component analysis give essential insights for comprehending the conformational changes that result from G-Rh1 binding to ROCK1 and RhoA. Further, MTT assay was employed to examine the potential cytotoxicity in vitro against human lung cancer cells (A549) and Raw 264.7 Murine macrophage cells. Thus, G-Rh1 showed significant cytotoxicity against human lung adenocarcinoma (A549) at 100 µg/mL. In addition, we observed an elevated level of reactive oxygen species (ROS) generation, perhaps promoting cancer cell toxicity. Additionally, G-Rh1 suppressed the mRNA expression of RhoA, ROCK1, MMP1, and MMP9 in cancer cell. Accordingly, G-Rh1 upregulated the p53, Bax, Caspase 3, caspase 9 while Bcl2 is downregulated intrinsic pathway. The findings from our study propose that the anticancer activity of G-Rh1 may be related to the induction of apoptosis by the RhoA/ROCK1 signaling pathway. As a result, this study evaluated the functional drug-like compound G-Rh1 from Panax ginseng in preventing and treating lung cancer adenocarcinoma via regulating metastasis and apoptosis.


Asunto(s)
Ginsenósidos , Neoplasias Pulmonares , Panax , Humanos , Ratones , Animales , Células A549 , Proteína de Unión al GTP rhoA/metabolismo , Quinasas Asociadas a rho/metabolismo , Neoplasias Pulmonares/tratamiento farmacológico , Neoplasias Pulmonares/metabolismo , Ginsenósidos/química , Apoptosis , Panax/metabolismo
10.
Molecules ; 27(9)2022 Apr 27.
Artículo en Inglés | MEDLINE | ID: mdl-35566145

RESUMEN

Nanoscience is a multidisciplinary skill with elucidated nanoscale particles and their advantages in applications to various fields. Owing to their economical synthesis, biocompatible nature, and widespread biomedical and environmental applications, the green synthesis of metal nanoparticles using medicinal plants has become a potential research area in biomedical research and functional food formulations. Gynostemma pentaphyllum (GP) has been extensively used in traditional Chinese medicine to cure several diseases, including diabetes mellitus (DM). This is the first study in which we examined the efficacy of G. pentaphyllum gold nanoparticles (GP-AuNPs) against obesity and related inflammation. GP extract was used as a capping agent to reduce Au2+ to Au0 to form stable gold nanoparticles. The nanoparticles were characterized by using UV-VIS spectroscopy, and TEM images were used to analyze morphology. In contrast, the existence of the functional group was measured using FTIR, and size and shape were examined using XRD analysis. In vitro analysis on GP-AuNPs was nontoxic to RAW 264.7 cells and 3T3-L1 cells up to a specific concentration. It significantly decreased lipid accumulation in 3T3-L1 obese and reduced NO production in Raw 264.7 macrophage cells. The significant adipogenic genes PPARγ and CEPBα and a major pro-inflammatory cytokine TNF-α expression were quantified using RT-PCR. The GP-AuNPs decreased the face of these genes remarkably, revealing the antiadipogenic and anti-inflammatory activity of our synthesized GP-AuNPs. This study represents thorough research on the antiobesity effect of Gynostemma pentaphyllum gold nanoparticles synthesized using a green approach and the efficacy instead of related inflammatory responses.


Asunto(s)
Oro , Nanopartículas del Metal , Animales , Regulación hacia Abajo , Expresión Génica , Oro/química , Oro/farmacología , Tecnología Química Verde/métodos , Gynostemma , Inflamación/tratamiento farmacológico , Inflamación/genética , Nanopartículas del Metal/química , Ratones , Obesidad , PPAR gamma/genética , Extractos Vegetales/química , Extractos Vegetales/farmacología , Factor de Necrosis Tumoral alfa/genética
11.
Molecules ; 27(16)2022 Aug 12.
Artículo en Inglés | MEDLINE | ID: mdl-36014376

RESUMEN

The skin tissue of the scalp is unique from other skin tissues because it coexists with hair, and many differences in microbial composition have been confirmed. In scalp tissues, hair loss occurs due to a combination of internal and external factors, and several studies are being conducted to counteract this. However, not many studies have addressed hair loss from the perspective of the microbiome. In this study, subjects with hair loss and those with normal scalps were set as experimental and control groups, respectively. In the experimental group, hair loss had progressed, and there was a large difference in microbiome composition compared to the group with normal scalps. In particular, differences in Accumulibacter, Staphylococcus, and Corynebacterium were found. From Staphylococcus epidermidis Cicaria, two active components were isolated as a result of repeated column chromatography. Spectroscopic data led to the determination of chemical structures for adenosine and biotin. Fractions were obtained, and ex vivo tests were conducted using hair follicles derived from human scalp tissue. When the microbiome adenosine-treated group was compared to the control group, hair follicle length was increased, and hair root diameter was maintained during the experimental periods. In addition, the Cicaria culture medium and the microbial adenosine- and biotin-treated groups maintained the anagen phase, reducing progression to the catagen phase in the hair growth cycle. In conclusion, it was confirmed that the Cicaria culture medium and the microbial adenosine and biotin derived from the culture were effective in inhibiting hair loss.


Asunto(s)
Microbiota , Staphylococcus epidermidis , Adenosina , Alopecia , Biotina , Folículo Piloso , Humanos
12.
J Gen Virol ; 102(3)2021 03.
Artículo en Inglés | MEDLINE | ID: mdl-33416468

RESUMEN

Chios mastic gum (CMG), a resin of the mastic tree (Pistacia lentiscus var. chia), has been used to treat multiple disorders caused by gastrointestinal malfunctions and bacterial infections for more than 2500 years. However, little is known about CMG's antiviral activity. CMG is known to influence multiple cellular processes such as cell proliferation, differentiation and apoptosis. As virus replication is largely dependent on the host cellular metabolism, it is conceivable that CMG regulates virus infectivity. Therefore, in this study, we evaluated CMG's potential as an antiviral drug to treat influenza A virus (IAV) infection. CMG treatment dramatically reduced the cytopathogenic effect and production of RNAs, proteins and infectious particles of IAV. Interestingly, CMG interfered with the early stage of the virus life cycle after viral attachment. Importantly, the administration of CMG greatly ameliorated morbidity and mortality in IAV-infected mice. The results suggest that CMG displays a potent anti-IAV activity by blocking the early stage of viral replication. Thus, mastic gum could be exploited as a novel therapeutic agent against IAV infection.


Asunto(s)
Subtipo H1N1 del Virus de la Influenza A/efectos de los fármacos , Subtipo H1N1 del Virus de la Influenza A/patogenicidad , Resina Mástique/farmacología , Infecciones por Orthomyxoviridae/tratamiento farmacológico , Animales , Antivirales/farmacología , Antivirales/uso terapéutico , Supervivencia Celular/efectos de los fármacos , Efecto Citopatogénico Viral/efectos de los fármacos , Perros , Células HEK293 , Humanos , Subtipo H1N1 del Virus de la Influenza A/fisiología , Células de Riñón Canino Madin Darby , Resina Mástique/uso terapéutico , Infecciones por Orthomyxoviridae/virología , Virulencia/efectos de los fármacos , Acoplamiento Viral , Replicación Viral/efectos de los fármacos
13.
Arch Microbiol ; 203(5): 2193-2198, 2021 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-33620525

RESUMEN

A novel Gram-reaction positive-, catalase and oxidase negative-, rod-shaped, facultatively anaerobic bacterial strain, DCY120T, was isolated from the gut of honeybee (Apis cerana) in Gyeonggi-do, South Korea. Strain DCY120T belongs to the genus Bombilactobacillus and is moderately related to Bombilactobacillus mellis Hon2T (94.1% similarity), Bombilactobacillus bombi BTLCH M1/2T (93.8%), and Bombilactobacillus mellifer Bin4NT (93.5%) based on 16S rRNA gene sequence analysis. The genome of strain DCY120T was sequenced and the average nucleotide identity (ANI) between strain DCY120T and the related Bombilactobacillus type strains were below the threshold value (95-96%) for species delineation. The major fatty acids were C16:0, C18:1 ω9c, Summed C19:1 ω6c/C19:0 cyclo ω10c/C19:0 ω6 and Summed C18:1 ω7c/C18:1 ω6c. The major polar lipids were diphosphatidylglycerol (DPG), phosphatidylglycerol (PG), one glycolipid (GL), and one unidentified aminophospholipid (APL). The amino acids in peptidoglycan of strain DCY120T were lysine, alanine, glutamic acid, and aspartic acid. In conclusion, the description of phenotypic and genotypic properties support strain DCY120T as a novel species within the genus Bombilactobacillus, for which the name Bombilactobacillus apium sp. nov. is proposed. The type strain is DCY120T (= KCTC 43194T = JCM 34006T).


Asunto(s)
Abejas/microbiología , Lactobacillaceae , Animales , Técnicas de Tipificación Bacteriana , Composición de Base/genética , ADN Bacteriano/genética , Ácidos Grasos/química , Genoma Bacteriano/genética , Glucolípidos , Lactobacillaceae/clasificación , Lactobacillaceae/genética , Lactobacillaceae/aislamiento & purificación , Hibridación de Ácido Nucleico , Peptidoglicano/química , Fosfolípidos/química , Filogenia , ARN Ribosómico 16S/genética , República de Corea , Análisis de Secuencia de ADN
14.
Bioorg Med Chem ; 45: 116329, 2021 09 01.
Artículo en Inglés | MEDLINE | ID: mdl-34329818

RESUMEN

Agrimonia pilosa (AP), Galla rhois (RG), and their mixture (APRG64) strongly inhibited SARS-CoV-2 by interfering with multiple steps of the viral life cycle including viral entry and replication. Furthermore, among 12 components identified in APRG64, three displayed strong antiviral activity, ursolic acid (1), quercetin (7), and 1,2,3,4,6-penta-O-galloyl-ß-d-glucose (12). Molecular docking analysis showed these components to bind potently to the spike receptor-binding-domain (RBD) of the SARS-CoV-2 and its variant B.1.1.7. Taken together, these findings indicate APRG64 as a potent drug candidate to treat SARS-CoV-2 and its variants.


Asunto(s)
Agrimonia/química , Antivirales/química , Productos Biológicos/química , Tratamiento Farmacológico de COVID-19 , Extractos Vegetales/química , SARS-CoV-2/efectos de los fármacos , Secuencia de Aminoácidos , Antivirales/farmacología , Productos Biológicos/farmacología , Descubrimiento de Drogas , Humanos , Taninos Hidrolizables/química , Simulación del Acoplamiento Molecular , Extractos Vegetales/farmacología , Unión Proteica , Quercetina/química , Glicoproteína de la Espiga del Coronavirus/química , Triterpenos/química , Internalización del Virus/efectos de los fármacos , Ácido Ursólico
15.
Molecules ; 26(7)2021 Mar 26.
Artículo en Inglés | MEDLINE | ID: mdl-33810618

RESUMEN

Background: Phytoncide is known to have antimicrobial and anti-inflammatory properties. Purpose: This study was carried out to confirm the anti-inflammatory activity of two types of phytoncide extracts from pinecone waste. Methods: We made two types of animal models to evaluate the efficacy, an indomethacin-induced gastroenteritis rat model and a dextran sulfate sodium-induced colitis mouse model. Result: In the gastroenteritis experiment, the expression of induced-nitric oxide synthase (iNOS), a marker for inflammation, decreased in the phytoncide-supplemented groups, and gastric ulcer development was significantly inhibited (p < 0.05). In the colitis experiment, the shortening of the colon length and the iNOS expression were significantly suppressed in the phytoncide-supplemented group (p < 0.05). Conclusions: Through this study, we confirmed that phytoncide can directly inhibit inflammation in digestive organs. Although further research is needed, we conclude that phytoncide has potential anti-inflammatory properties in the digestive tract and can be developed as a functional agent.


Asunto(s)
Antiinflamatorios , Colitis Ulcerosa/tratamiento farmacológico , Tracto Gastrointestinal/efectos de los fármacos , Monoterpenos , Pinus/química , Extractos Vegetales , Animales , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Modelos Animales de Enfermedad , Tracto Gastrointestinal/patología , Masculino , Ratones , Ratones Endogámicos C57BL , Monoterpenos/farmacología , Monoterpenos/uso terapéutico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Ratas , Ratas Sprague-Dawley
16.
Molecules ; 27(1)2021 Dec 30.
Artículo en Inglés | MEDLINE | ID: mdl-35011448

RESUMEN

This study focused on developing Panos nanoemulsion (P-NE) and enhancing the anti-inflammatory efficacy for the treatment of inflammation. The effects of P-NE were evaluated in terms of Nitric oxide (NO production) in Lipopolysaccharide (LPS), induced RAW 264.7 cells, Reactive oxygen species (ROS) generation using Human Keratinocyte cells (HaCaT), and quantitative polymerase chain reaction (qPCR) analysis. Sea buckthorn oil, Tween 80, and span 80 were used and optimize the process. Panos extract (P-Ext) was prepared using the fermentation process. Further high-energy ultra-sonication was used for the preparation of P-NE. The developed nanoemulsion (NE) was characterized using different analytical methods. Field emission transmission electron microscopy (FE-TEM) analyzed the spherical shape and morphology. In addition, stability was analyzed by Dynamic light scattering (DLS) analysis, where particle size was analyzed 83 nm, and Zeta potential -28.20 ± 2 (mV). Furthermore, 90 days of stability was tested using different temperatures conditions where excellent stability was observed. P-NE are non-toxic in (HaCaT), and RAW264.7 cells up to 100 µg/mL further showed effects on ROS and NO production of the cells at 50 µg/mL. The qPCR analysis demonstrated the suppression of pro-inflammatory mediators for (Cox 2, IL-6, IL-1ß, and TNF-α, NF-κB, Ikkα, and iNOS) gene expression. The prepared NE exhibited anti-inflammatory effects, demonstrating its potential as a safe and non-toxic nanomedicine.


Asunto(s)
Antiinflamatorios/química , Antiinflamatorios/farmacología , Benzodiazepinas/química , Benzodiazepinas/farmacología , Emulsiones , Fermentación , Extractos Vegetales/química , Animales , Supervivencia Celular/efectos de los fármacos , Fenómenos Químicos , Estabilidad de Medicamentos , Mediadores de Inflamación , Ratones , Óxido Nítrico/metabolismo , Células RAW 264.7 , Especies Reactivas de Oxígeno/metabolismo , Análisis Espectral
17.
Phytother Res ; 34(9): 2313-2322, 2020 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-32243009

RESUMEN

This trial aimed to determine the effect of a standardized Cynanchum wilfordii Radix extract (CWE) on the lipid profiles of individuals with elevated total cholesterol (T-Chol) using a double-blind randomized placebo-controlled design. Ninety-six Korean individuals with elevated T-Chol level (200-240 mg/dL) were recruited and randomly allocated to groups that received VasH300 (300 mg CWE/day, n = 32), VasH600 (600 mg CWE/day, n = 32), or a placebo (n = 32) groups. Primary outcomes included T-Chol, low-density lipoprotein (LDL)-cholesterol, high-density lipoprotein (HDL)-cholesterol, triglyceride, and safety (adverse events, biochemical parameters, and hematological parameters). Data were compared using a one-way analysis of variance followed by Duncan's post-hoc tests (among groups) and paired t tests (within groups). Values for T-Chol and LDL-cholesterol were significantly reduced in the VasH300 and groups (VasH300: 4.0 and 6.4%, respectively; VasH600; 3.8 and 5.8% respectively; both p < .05) compared with the placebo group and were not dose-dependent. VasH300 significantly improved the lipid profiles of individuals with elevated T-Chol without any serious side effects. Daily supplementation with VasH might be an alternative strategy with which to modify cholesterol-related parameters, especially in individuals with elevated T-Chol levels.


Asunto(s)
Cynanchum/química , Suplementos Dietéticos/análisis , Hipercolesterolemia/tratamiento farmacológico , Extractos Vegetales/química , Adulto , Anciano , Método Doble Ciego , Femenino , Humanos , Masculino , Persona de Mediana Edad , Factores de Tiempo , Adulto Joven
18.
Molecules ; 25(19)2020 Sep 24.
Artículo en Inglés | MEDLINE | ID: mdl-32987784

RESUMEN

Ginseng is a traditional medicinal herb commonly consumed world-wide owing to its unique family of saponins called ginsenosides. The absorption and bioavailability of ginsenosides mainly depend on an individual's gastrointestinal bioconversion abilities. There is a need to improve ginseng processing to predictably increase the pharmacologically active of ginsenosides. Various types of ginseng, such as fresh, white, steamed, acid-processed, and fermented ginsengs, are available. The various ginseng processing methods produce a range ginsenoside compositions with diverse pharmacological properties. This review is intended to summarize the properties of the ginsenosides found in different Panax species as well as the different processing methods. The sugar moiety attached to the C-3, C-6, or C-20 deglycosylated to produce minor ginsenosides, such as Rb1, Rb2, Rc, Rd→Rg3, F2, Rh2; Re, Rf→Rg1, Rg2, F1, Rh1. The malonyl-Rb1, Rb2, Rc, and Rd were demalonylated into ginsenoside Rb1, Rb2, Rc, and Rd by dehydration. Dehydration also produces minor ginsenosides such as Rg3→Rk1, Rg5, Rz1; Rh2→Rk2, Rh3; Rh1→Rh4, Rk3; Rg2→Rg6, F4; Rs3→Rs4, Rs5; Rf→Rg9, Rg10. Acetylation of several ginsenosides may generate acetylated ginsenosides Rg5, Rk1, Rh4, Rk3, Rs4, Rs5, Rs6, and Rs7. Acid processing methods produces Rh1→Rk3, Rh4; Rh2→Rk1, Rg5; Rg3→Rk2, Rh3; Re, Rf, Rg2→F1, Rh1, Rf2, Rf3, Rg6, F4, Rg9. Alkaline produces Rh16, Rh3, Rh1, F4, Rk1, ginsenoslaloside-I, 20(S)-ginsenoside-Rh1-60-acetate, 20(R)-ginsenoside Rh19, zingibroside-R1 through hydrolysis, hydration addition reactions, and dehydration. Moreover, biological processing of ginseng generates the minor ginsenosides of Rg3, F2, Rh2, CK, Rh1, Mc, compound O, compound Y through hydrolysis reactions, and synthetic ginsenosides Rd12 and Ia are produced through glycosylation. This review with respect to the properties of particular ginsenosides could serve to increase the utilization of ginseng in agricultural products, food, dietary supplements, health supplements, and medicines, and may also spur future development of novel highly functional ginseng products through a combination of various processing methods.


Asunto(s)
Ginsenósidos/química , Ginsenósidos/aislamiento & purificación , Panax/química
19.
Molecules ; 25(23)2020 Dec 04.
Artículo en Inglés | MEDLINE | ID: mdl-33291776

RESUMEN

This study aimed to produce and optimize a Cordyceps militaris-based oil-in-water (O/W) nanoemulsion (NE) encapsulated in sea buckthorn oil (SBT) using an ultrasonication process. Herein, a nonionic surfactant (Tween 80) and chitosan cosurfactant were used as emulsifying agents. The Cordyceps nanoemulsion (COR-NE) was characterized using Fourier-transform infrared spectroscopy (FT-IR), dynamic light scattering (DLS), and field-emission transmission electron microscope (FE-TEM). The DLS analyses revealed that the NE droplets were 87.0 ± 2.1 nm in diameter, with a PDI value of 0.089 ± 0.023, and zeta potential of -26.20 ± 2. The small size, low PDI, and stable zeta potential highlighted the excellent stability of the NE. The NE was tested for stability under different temperature (4 °C, 25 °C, and 60 °C) and storage conditions for 3 months where 4 °C did not affect the stability. Finally, in vitro cytotoxicity and anti-inflammatory activity were assessed. The results suggested that the NE was not toxic to RAW 264.7 or HaCaT (human keratinocyte) cell lines at up to 100 µL/mL. Anti-inflammatory activity in liposaccharides (LPS)-induced RAW 264.7 cells was evident at 50 µg/mL and showed inhibition of NO production and downregulation of pro-inflammatory gene expression. Further, the NE exhibited good antioxidant (2.96 ± 0.10 mg/mL) activity and inhibited E. coli and S. aureus bacterial growth. Overall, the COR-NE had greater efficacy than the free extract and added significant value for future biomedical and cosmetics applications.


Asunto(s)
Antiinfecciosos/farmacología , Antiinflamatorios/farmacología , Antioxidantes/farmacología , Cordyceps/química , Emulsiones/química , Nanopartículas/química , Animales , Antiinfecciosos/química , Antiinflamatorios/química , Antioxidantes/química , Línea Celular , Escherichia coli/efectos de los fármacos , Expresión Génica/efectos de los fármacos , Células HaCaT , Humanos , Ratones , Óxido Nítrico/química , Aceites Volátiles/química , Tamaño de la Partícula , Polisorbatos/química , Células RAW 264.7 , Espectroscopía Infrarroja por Transformada de Fourier/métodos , Staphylococcus aureus/efectos de los fármacos
20.
Bioorg Chem ; 93: 103320, 2019 12.
Artículo en Inglés | MEDLINE | ID: mdl-31585267

RESUMEN

Hepatitis C virus (HCV) infection is a significant health problem, with a worldwide prevalence of about 170 million. Recently, the development of direct acting antiviral (DAA) as a therapeutic agent for HCV has been rapidly increasing. However, DAA has a side effect and is costly. Therefore, it is still necessary to develop a therapeutic agent to treat HCV infection using products. Agrimonia pilosa (AP) and Galla rhois (RG) are traditional medicines and are known to display therapeutic activity on various diseases. Notably, they have been reported to have an anti-viral effect on HBV and influenza virus infections. It is expected that anti-viral activity will increase when two extracts are mixed. To investigate their anti-viral activity, the expression level of HCV Core 1b and NS5A was measured. Remarkably, AP, RG, and their mixed compound (APRG64) strongly inhibited the expression of viral proteins, which led us to identify their metabolites. A total of 14 metabolites were identified using liquid chromatography mass spectrometry (LC-MS). These metabolites were evaluated for their anti-HCV activity to identify active ingredients. In conclusion, our results unveiled that anti-HCV activity of Agrimonia pilosa and Galla rhois extract mixture could lead to the development of a novel therapy for HCV infection.


Asunto(s)
Agrimonia/química , Antivirales/farmacología , Productos Biológicos/química , Hepacivirus/efectos de los fármacos , Extractos Vegetales/farmacología , Línea Celular , Cromatografía Líquida de Alta Presión/métodos , Humanos , Espectrometría de Masas/métodos , Pruebas de Sensibilidad Microbiana
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