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1.
Dermatol Surg ; 50(4): 360-365, 2024 Apr 01.
Artículo en Inglés | MEDLINE | ID: mdl-38318968

RESUMEN

BACKGROUND: Using a thread for wound closure promotes healing and minimizes contamination by foreign substances. Threads have also been employed in esthetic surgery; however, functional threads that can improve wrinkles and rejuvenate the skin are required. OBJECTIVE: To evaluate the suitability of polydioxanone threads coated with polyethylene glycol, hyaluronic acid, and amino acids for use in the medical field because such formulations are expected to promote regeneration and collagen synthesis. MATERIALS AND METHODS: Physical properties (diameter [ n = 20], tensile strength [ n = 20], strength retention rate [ n = 10], and scanning electron microscopy images) and cytotoxicity (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide and lactate dehydrogenase assays) of polydioxanone threads coated with polyethylene glycol, hyaluronic acid, and amino acids were assessed and compared with those of uncoated polydioxanone threads. Analyses were performed using IBM SPSS Statistics (Statistical significance; p values <.05). RESULTS: The size standards for tensile strength (≥63.5 N) and diameter (average 0.570-0.610 mm) were met. There were no differences in the physical properties of the coated and uncoated threads; however, the biocompatibility of coated threads was high owing to low cytotoxicity. CONCLUSION: Threads coated with materials that can promote regeneration are suitable for use in the medical field.


Asunto(s)
Polidioxanona , Ritidoplastia , Humanos , Ácido Hialurónico , Ritidoplastia/métodos , Aminoácidos , Polietilenglicoles , Suturas
2.
J Clin Lab Anal ; 36(10): e24682, 2022 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-36036770

RESUMEN

BACKGROUND: Sexually transmitted infections (STIs) can have serious consequences, and the global STI incidence remains high. However, there is little information on the frequency of STIs with multiple pathogens according to age. Accordingly, we conducted a study to determine the trends of coinfection with sexually transmitted pathogens according to age in the Republic of Korea from 2018 to 2020. METHODS: From January 2018 to December 2020, 65,191 samples of swab, urine, and other types submitted for STI screening were obtained from U2Bio Co. Ltd. (Seoul, Republic of Korea). Multiplex polymerase chain reaction, a sensitive and rapid method for simultaneous detection of STIs caused by multiple different pathogens, was performed using an AccuPower STI4C-Plex Real-Time PCR kit, AccuPower STI8A-Plex Real-Time PCR kit, and AccuPower STI8B-Plex Real-Time PCR kit with an Exicycler 96 Real-Time Quantitative Thermal Block. RESULTS: Of the 65,191 samples tested, 35,366 (54.3%) tested positive for one or more sexually transmitted pathogens. The prevalence of coinfections with two or more sexually transmitted pathogens was inversely proportional to age. Furthermore, the rates of coinfection with sexually transmitted pathogens and age distribution differed according to sex and the sexually transmitted pathogen type. CONCLUSION: This study confirmed that a significant proportion of patients with STIs are coinfected with multiple pathogens. Public health managers could use these results to recognize and prevent STIs according to age.


Asunto(s)
Coinfección , Enfermedades de Transmisión Sexual , Coinfección/epidemiología , Humanos , Reacción en Cadena de la Polimerasa Multiplex/métodos , Prevalencia , Reacción en Cadena en Tiempo Real de la Polimerasa/métodos , Enfermedades de Transmisión Sexual/diagnóstico , Enfermedades de Transmisión Sexual/epidemiología
3.
Bioorg Med Chem Lett ; 43: 128096, 2021 07 01.
Artículo en Inglés | MEDLINE | ID: mdl-33984475

RESUMEN

Previously, we isolated six heterocyclic compounds (1-6) from the fruits of mulberry trees (Morus alba L.) and determined that loliolide affords rat pancreatic islet ß-cell (INS-1) protection against streptozotocin­induced cytotoxicity. In the present study, we further investigated the effect of the six heterocyclic compounds (1-6) on glucose-stimulated insulin secretion (GSIS) in INS-1 cells. Among them, (R)­5­hydroxypyrrolidin­2­one(1) and indole (6) increased GSIS without inducing cytotoxicity. Additionally, compounds 1 and 6 enhanced the phosphorylation of total insulin receptor substrate-2, phosphatidylinositol 3-kinase, and Akt, and activated pancreatic and duodenal homeobox-1, which play a crucial role in ß-cell functions related to insulin secretion. Collectively, these findings indicate that (R)­5­hydroxypyrrolidin­2­one(1) and indole (6), isolated from M. alba fruits, may be beneficial in managing type 2 diabetes.


Asunto(s)
Glucosa/antagonistas & inhibidores , Compuestos Heterocíclicos/farmacología , Hipoglucemiantes/farmacología , Secreción de Insulina/efectos de los fármacos , Animales , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Glucosa/farmacología , Compuestos Heterocíclicos/química , Hipoglucemiantes/química , Células Secretoras de Insulina/efectos de los fármacos , Células Secretoras de Insulina/metabolismo , Estructura Molecular , Ratas , Relación Estructura-Actividad
4.
Bioorg Med Chem Lett ; 41: 127989, 2021 06 01.
Artículo en Inglés | MEDLINE | ID: mdl-33794317

RESUMEN

Hepatic fibrosis is a chronic liver disease characterized by the accumulation of extracellular matrix (ECM). Activation of hepatic stellate cells (HSCs) after repetitive liver damage is a key event in hepatic fibrogenesis. As part of ongoing research projects to identify pharmacologically effective natural products, the phytochemical investigation of a MeOH extract of Centipeda minima led to the isolation of a sesquiterpene lactone, brevilin A, which was explored to elucidate potential anti-fibrotic effects by reversing HSC activation. First, we observed that transforming growth factor (TGF)-ß1 treatment significantly increased the expression levels of HSC activation marker, α-smooth muscle actin (α-SMA), and ECM protein such as collagen and fibronectin. Then, we demonstrated that brevilin A reversed the TGF-ß1-induced increase in protein and mRNA expression levels of α-SMA and collagen. To investigate the underlying molecular mechanism of brevilin A, we evaluated the effects of brevilin A on the STAT3 signaling pathway. STAT3 phosphorylation, increased by TGF-ß1 treatment, was strongly inhibited by brevilin A; the expression levels of fibronectin and connective tissue growth factor were also significantly decreased by brevilin A. The present study indicated that brevilin A has a preventive and therapeutic potential against hepatic fibrosis.


Asunto(s)
Crotonatos/farmacología , Diseño de Fármacos , Cirrosis Hepática/tratamiento farmacológico , Factor de Transcripción STAT3/antagonistas & inhibidores , Sesquiterpenos/farmacología , Crotonatos/química , Relación Dosis-Respuesta a Droga , Células Estrelladas Hepáticas/efectos de los fármacos , Humanos , Cirrosis Hepática/metabolismo , Cirrosis Hepática/patología , Estructura Molecular , Factor de Transcripción STAT3/genética , Factor de Transcripción STAT3/metabolismo , Sesquiterpenos/química , Transducción de Señal/efectos de los fármacos , Relación Estructura-Actividad
5.
Bioorg Med Chem Lett ; 36: 127828, 2021 03 15.
Artículo en Inglés | MEDLINE | ID: mdl-33508466

RESUMEN

Bioactivity-driven LC/MS-based phytochemical analysis of the root bark extract of Ulmus davidiana var. japonica led to the isolation of 10 compounds including a new coumarin glycoside derivative, ulmusakidian (1). The structure of the new compound was elucidated using extensive spectroscopic analyses via 1D and 2D NMR spectroscopic data interpretations, HR-ESIMS, and chemical transformation. The isolated compounds 1-10 were tested for their antifungal activity against human fungal pathogens Cryptococcus neoformans and Candida albicans. Compounds 9 and 10 showed antifungal activity against C. neoformans, with the lowest minimal inhibitory concentration (MIC) of 12.5-25.0 µg/mL, whereas none of the compounds showed antifungal activity against C. albicans.


Asunto(s)
Antifúngicos/farmacología , Candida albicans/efectos de los fármacos , Cryptococcus neoformans/efectos de los fármacos , Fenoles/farmacología , Extractos Vegetales/farmacología , Ulmus/química , Antifúngicos/química , Antifúngicos/aislamiento & purificación , Relación Dosis-Respuesta a Droga , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Fenoles/química , Fenoles/aislamiento & purificación , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Raíces de Plantas/química , Relación Estructura-Actividad
6.
Molecules ; 26(6)2021 Mar 14.
Artículo en Inglés | MEDLINE | ID: mdl-33799458

RESUMEN

Inhibition of the megakaryocyte protein tyrosine phosphatase 2 (PTP-MEG2, also named PTPN9) activity has been shown to be a potential therapeutic strategy for the treatment of type 2 diabetes. Previously, we reported that PTP-MEG2 knockdown enhances adenosine monophosphate activated protein kinase (AMPK) phosphorylation, suggesting that PTP-MEG2 may be a potential antidiabetic target. In this study, we found that phloridzin, isolated from Ulmus davidiana var. japonica, inhibits the catalytic activity of PTP-MEG2 (half-inhibitory concentration, IC50 = 32 ± 1.06 µM) in vitro, indicating that it could be a potential antidiabetic drug candidate. Importantly, phloridzin stimulated glucose uptake by differentiated 3T3-L1 adipocytes and C2C12 muscle cells compared to that by the control cells. Moreover, phloridzin led to the enhanced phosphorylation of AMPK and Akt relevant to increased insulin sensitivity. Importantly, phloridzin attenuated palmitate-induced insulin resistance in C2C12 muscle cells. We also found that phloridzin did not accelerate adipocyte differentiation, suggesting that phloridzin improves insulin sensitivity without significant lipid accumulation. Taken together, our results demonstrate that phloridzin, an inhibitor of PTP-MEG2, stimulates glucose uptake through the activation of both AMPK and Akt signaling pathways. These results strongly suggest that phloridzin could be used as a potential therapeutic candidate for the treatment of type 2 diabetes.


Asunto(s)
Resistencia a la Insulina/fisiología , Florizina/farmacología , Proteínas Tirosina Fosfatasas no Receptoras/antagonistas & inhibidores , Proteínas Tirosina Fosfatasas/antagonistas & inhibidores , Células 3T3 , Adipocitos/efectos de los fármacos , Adipocitos/metabolismo , Animales , Diferenciación Celular/efectos de los fármacos , Línea Celular , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Diabetes Mellitus Tipo 2/metabolismo , Glucosa/metabolismo , Hipoglucemiantes/farmacología , Insulina/metabolismo , Ratones , Palmitatos/farmacología , Fosforilación/efectos de los fármacos , Transducción de Señal/efectos de los fármacos
7.
Bioorg Med Chem Lett ; 28(6): 1084-1089, 2018 04 01.
Artículo en Inglés | MEDLINE | ID: mdl-29459209

RESUMEN

Pinus koraiensis pinecones are considered an undesired waste by-product of the processing of seeds. However, recent studies of the potential anti-tumor effects of the pinecones have led to increasing interest in their chemical constituents. The present study examined the potential antiangiogenic effects of the constituents of pinecones and further characterized their underlying mechanisms of action. Chemical investigation of a water extract of P. koraiensis pinecones led to the isolation and identification of the eight main components including five diterpenoids (1-5), two monoterpenes (6,7) and a phenolic acid (8). The structure of the compounds was determined by spectroscopic analysis of NMR spectra and LC/MS analysis. Of the isolated compounds, 7α,15-dihydroxydehydroabietic acid (5) significantly inhibited the promotion of angiogenesis in human umbilical vein endothelial cells (HUVECs). Compound 5 inhibited angiogenesis through downregulation of the VEGF, p-Akt and p-ERK signaling pathways. These results provide experimental evidence of a novel biological activity of 7α,15-dihydroxydehydroabietic acid (5) as a potential antiangiogenic substance. This study also suggests that compound 5 could potentially be a useful adjuvant therapeutic substance for cancer prevention and treatment.


Asunto(s)
Abietanos/farmacología , Quinasas MAP Reguladas por Señal Extracelular/antagonistas & inhibidores , Células Endoteliales de la Vena Umbilical Humana/efectos de los fármacos , Neovascularización Patológica/tratamiento farmacológico , Pinus/química , Proteínas Proto-Oncogénicas c-akt/antagonistas & inhibidores , Factor A de Crecimiento Endotelial Vascular/antagonistas & inhibidores , Abietanos/síntesis química , Abietanos/química , Relación Dosis-Respuesta a Droga , Regulación hacia Abajo/efectos de los fármacos , Quinasas MAP Reguladas por Señal Extracelular/metabolismo , Humanos , Estructura Molecular , Neovascularización Patológica/metabolismo , Proteínas Proto-Oncogénicas c-akt/metabolismo , Relación Estructura-Actividad , Factor A de Crecimiento Endotelial Vascular/metabolismo
8.
Bioorg Chem ; 76: 28-36, 2018 02.
Artículo en Inglés | MEDLINE | ID: mdl-29125970

RESUMEN

The fruit of the white mulberry tree (Morus alba L.) is a multiple fruit with a sweet flavor commonly consumed around the world. Chemical investigation of the fruits led to the isolation of two indole acetic acid derivatives (1 -2) including a new compound, which turned out to be an isolation artifact, 3S-(ß-D-glucopyranosyloxy)-2,3-dihydro-2-oxo-1H-indole-3-acetic acid butyl ester (1), along with five known compounds (3 -7). Compounds 2 and 7 were newly identified from mulberry fruit. The new isolation artifact (1) exhibited cytotoxic effect on human cervical cancer Hela cells in a dose-dependent manner. Compound 1 activated caspase-8, caspase-9, and caspase-3, followed by cleavage of PARP, a substrate of caspase-3, in a dose-dependent manner. Simultaneous alterations in protein expression of mitochondrial factors Bax, BID and Bcl-2 were also observed. A comparison between compounds 1 and 2 led to a structure-activity relationship analysis of the cytotoxic effect. These results suggest that compound 1 could be beneficial in human cervical cancer treatment, and provide a theoretical basis for further application of compound 1.


Asunto(s)
Antineoplásicos/farmacología , Glucósidos/farmacología , Ácidos Indolacéticos/farmacología , Morus/química , Neoplasias del Cuello Uterino/tratamiento farmacológico , Antineoplásicos/química , Antineoplásicos/aislamiento & purificación , Apoptosis/efectos de los fármacos , Caspasa 8/metabolismo , Caspasa 9/metabolismo , Femenino , Frutas/química , Glucósidos/química , Glucósidos/aislamiento & purificación , Células HeLa , Humanos , Ácidos Indolacéticos/química , Ácidos Indolacéticos/aislamiento & purificación , Estereoisomerismo , Relación Estructura-Actividad
9.
Bioorg Med Chem Lett ; 27(14): 3156-3161, 2017 07 15.
Artículo en Inglés | MEDLINE | ID: mdl-28552338

RESUMEN

Guggulsterone derivatives were prepared using [3+2] click chemistry with aryl and alkyl acetylene. The series of derivatives were evaluated for their cellular protective effects on cisplatin-treated cultured LLC-PK1 kidney epithelial cells. Among the guggulsterone-triazole derivatives, compound 6g, which contains a hydroxyl methyl group, was the most active of all the derivatives. In an additional study, we determined that inhibition of the mitogen-activated protein kinase/caspase-3 signaling cascade by 6g mediates its protective effects against cytotoxicity in cultured LLC-PK1 cells.


Asunto(s)
Apoptosis/efectos de los fármacos , Pregnenodionas/química , Sustancias Protectoras/farmacología , Animales , Antineoplásicos/química , Antineoplásicos/farmacología , Caspasa 3/química , Caspasa 3/metabolismo , Cisplatino/farmacología , Química Clic , Riñón/citología , Riñón/efectos de los fármacos , Riñón/metabolismo , Células LLC-PK1 , Microscopía , Proteínas Quinasas Activadas por Mitógenos/antagonistas & inhibidores , Proteínas Quinasas Activadas por Mitógenos/metabolismo , Pregnenodionas/farmacología , Sustancias Protectoras/química , Transducción de Señal/efectos de los fármacos , Porcinos
10.
Bioorg Med Chem Lett ; 27(17): 4122-4127, 2017 09 01.
Artículo en Inglés | MEDLINE | ID: mdl-28765012

RESUMEN

Calvatia species, also known as puffball mushrooms, are common sources of food worldwide. Calvatia nipponica (Agaricaceae) is one of the most rare species in the Calvatia genus. It was first validated in 2008. Due to its scarcity, C. nipponica has never been chemically investigated. Its recent discovery in Korea allowed to conduct this study, and using bioactivity-guided fractionation for antiangiogenic activity, chemical investigation of the MeOH extract of the fruiting bodies of C. nipponica led to the isolation of five alkaloids (1-5) and two phenolic compounds (6-7). This is the first study to report the chemical investigation of C. nipponica, and compound 1 was previously reported as chemically synthesized only until our report of its isolation and identification from natural sources. The structure of 1 was determined by spectroscopic analysis by 1D and 2D NMR spectra and HR-MS. All compounds (1-7) were tested for inhibition of angiogenesis using human umbilical vein endothelial cells (HUVECs). Compounds 2, 4 and 5 significantly inhibited the promotion of angiogenesis in HUVECs. Compound 5 showed the most potent inhibition via downregulation of VEGF, p38 and ERK signaling pathways. These results suggested that the rare mushroom C. nipponica might be beneficial in antiangiogenesis therapy for cancer treatment.


Asunto(s)
Agaricales/química , Inhibidores de la Angiogénesis/farmacología , Células Endoteliales de la Vena Umbilical Humana/efectos de los fármacos , Neovascularización Patológica/tratamiento farmacológico , Inhibidores de la Angiogénesis/química , Inhibidores de la Angiogénesis/aislamiento & purificación , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Humanos , Estructura Molecular , Neovascularización Patológica/patología , Relación Estructura-Actividad
11.
Bioorg Med Chem Lett ; 27(18): 4389-4392, 2017 09 15.
Artículo en Inglés | MEDLINE | ID: mdl-28835347

RESUMEN

Sanguiin H-6 is a dimer of casuarictin linked by a bond between the gallic acid residue and one of the hexahydroxydiphenic acid units. It is an effective compound extracted from Rubus coreanus. It has an anticancer effect against several human cancer cells; however, its effect on breast cancer cells has not been clearly demonstrated. Thus, we aimed to investigate the anticancer effect and mechanism of action of sanguiin H-6 against two human breast carcinoma cell lines (MCF-7 and MDA-MB-231). We found that sanguiin H-6 significantly reduced cell viability in a concentration-dependent manner. It also increased the rates at which MCF-7 and MDA-MB-231 cells underwent apoptosis. Furthermore, sanguiin H-6 induced the cleavage of caspase-8, caspase-3, and poly(ADP-ribose) polymerase, which resulted in apoptosis. However, cleavage of caspase-9 was only detectable in MCF-7 cells. In addition, sanguiin H-6 increased the ratio of Bax to Bcl-2 in both MCF-7 and MDA-MB-231 cells. These findings suggest that sanguiin H-6 is a potent therapeutic agent against breast cancer cells. In addition, it exerts its anticancer effect in an estrogen-receptor-independent manner.


Asunto(s)
Antineoplásicos/farmacología , Taninos Hidrolizables/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/química , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Taninos Hidrolizables/síntesis química , Taninos Hidrolizables/química , Células MCF-7 , Estructura Molecular , Relación Estructura-Actividad
12.
Bioorg Med Chem Lett ; 27(13): 2881-2885, 2017 07 01.
Artículo en Inglés | MEDLINE | ID: mdl-28487074

RESUMEN

Cisplatin-induced nephrotoxicity is a serious adverse effect that limits the use of cisplatin in cancer patients. In the present study, we investigated the protective effect of lanostane triterpenoids (1-10) isolated from the ethanolic extract of Poria cocos Wolf against cisplatin-induced cell death in LLC-PK1 kidney tubular epithelial cells. Treatment of cisplatin induced significant cell death, which was suppressed by treatment with dehydroeburicoic acid monoacetate (1) and 3ß-acetoxylanosta-7,9(11),24-trien-21-oic acid (9). Compound 1 exhibited the highest efficacy among the tested compounds and was thus subjected to further mechanistic studies. The increase in the percentage of apoptotic cells induced by cisplatin reduced by 4.3% after co-treatment of cells with compound 1 (50 and 100µM). Furthermore, phosphorylation of the mitogen-activated protein kinases JNK, ERK, and p38, and caspase-3, which characterize oxidative stress-mediated apoptosis, increased significantly after treatment with cisplatin, and decreased after treatment with compound 1. These results indicate that the renoprotective effects of compound 1 may be mediated by its anti-apoptotic activity.


Asunto(s)
Apoptosis/efectos de los fármacos , Basidiomycota/química , Cisplatino/antagonistas & inhibidores , Sustancias Protectoras/farmacología , Triterpenos/farmacología , Animales , Antineoplásicos/farmacología , Línea Celular , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Cisplatino/farmacología , Relación Dosis-Respuesta a Droga , Estructura Molecular , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación , Relación Estructura-Actividad , Porcinos , Triterpenos/química , Triterpenos/aislamiento & purificación
13.
Biotechnol Lett ; 39(3): 415-421, 2017 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-27885509

RESUMEN

OBJECTIVES: To determine the inhibitory activities of flavonoids against NS2B-NS3 protease of ZIKA virus (ZIKV NS2B-NS3pro) expressed in Escherichia coli BL21 (DE3) and their structure activity relationship. RESULTS: ZIKV NS2B-NS3pro was expressed in E. coli BL21(DE3) as a 35 kDa protein. It had a K m of 26 µM with the fluorogenic peptide Dabcyl-KTSAVLQSGFRKME-Edan. The purified ZIKV NS2B-NS3pro was used for inhibition and kinetic assays to determine the activities of 22 polyphenol compounds. These polyphenol compounds at 100 µM inhibited the activity of ZIKV NS2B-NS3pro by 6.2-88%. Seven polyphenol compounds had IC50 ranging from 22 ± 0.2 to 112 ± 5.5 µM. Myricetin showed a mixed type inhibitory pattern against ZIKV NS2B-NS3pro protease. Its IC50 value was 22 ± 0.2 µM with a K i value of 8.9 ± 1.9 µM. CONCLUSION: The chemical structure of a polyphenol compound and its inhibitory activity against ZIKV NS2B-NS3pro can be explored to develop highly selective inhibitors against ZIKV NS2B-NS3pro.


Asunto(s)
Flavonoides/química , Flavonoides/farmacología , Inhibidores de Proteasas/química , Inhibidores de Proteasas/farmacología , Proteínas no Estructurales Virales/antagonistas & inhibidores , Virus Zika/enzimología , Electroforesis en Gel de Poliacrilamida , Polifenoles/química , Polifenoles/farmacología , Relación Estructura-Actividad , Proteínas no Estructurales Virales/metabolismo
14.
Molecules ; 22(10)2017 Sep 21.
Artículo en Inglés | MEDLINE | ID: mdl-28934155

RESUMEN

The edible fungus Phellinus baumii Pilat (Hymenochaetaceae) has been used in Korean traditional medicines for strengthening health and prolonging life. An extract of the fruiting bodies of P. baumii was subjected to bioassay-guided fractionation based on its anti-inflammatory effects in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. The resulting fractions were chemically investigated, leading to isolation of three phenolic compounds (1-3), a sesquiterpene (4), two steroids (5-6), a fatty acid (7), and a cerebroside (8). Spectroscopic analyses including 1D and 2D NMR spectroscopy and LC/MS were used to determine their chemical structures. Compounds 2, 4, 5, 7 and 8 were identified in P. baumii for the first time. Since all compounds were isolated from active fractions with anti-inflammatory activity, their ability to inhibit LPS-stimulated nitric oxide (NO) production in RAW264.7 cells were evaluated in vitro. Compounds 1, 2, 3, 5 and 7 inhibited LPS-stimulated NO production, and compounds 1-3 had IC50 values <10 µM. Treatment of LPS-stimulated RAW264.7 cells with compounds 1-3 inhibited phosphorylation of IKKα and IκBα. In addition, treatment of compounds 1-3 reduced LPS-induced increases of nuclear factor-kappa B (NF-κB) p65, iNOS and COX-2 protein expressions. Collectively, compounds 1-3 inhibited NF-κB-dependent inflammation in RAW264.7 cells. Thus, P. baumii is a potential source of natural anti-inflammatory agents, and active compounds 1-3 could be promising lead compounds for the development of novel anti-inflammatory agents.


Asunto(s)
Hongos/química , Fenoles/química , Animales , Antiinflamatorios , Ciclooxigenasa 2/metabolismo , Inflamación/metabolismo , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Espectroscopía de Resonancia Magnética , Ratones , FN-kappa B/metabolismo , Óxido Nítrico Sintasa de Tipo II/metabolismo , Células RAW 264.7
15.
Pharm Biol ; 55(1): 2205-2210, 2017 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-29115888

RESUMEN

CONTEXT: Antiacetylcholinesterase (AChE) drugs have been a main therapeutic treatment for Alzheimer's disease because increased AChE levels play a key role in reducing neurotransmission. OBJECTIVES: Extracts from 35 Korean plants were selected and screened for antioxidant and anti-cholinesterase activity to explore new sources derived from Korean natural resources that could be used as AD therapeutic agents. MATERIALS AND METHODS: The antioxidant effect of extracts from 35 selected Korean plants was determined using two most common free radical scavenging assays using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid (ABTS). Additionally, the effect of extracts, identified as antioxidants, on acetylcholinesterase inhibition was assessed by an acetylcholinesterase assay kit. RESULTS: Out of 36 extracts of 35 plants tested, Oenothera biennis L. (9.09 µg/mL), Saururus chinensis (Lour.) Baill. (9.52 µg/mL) and Betula platyphylla var. japonica (9.85 µg/mL) showed strong DPPH scavenging activity. Twelve other extracts also exerted moderate free radical scavenging activities with IC50 values ranging from 10 to 50 µg/mL. Antioxidant capacity detected by ABTS assay was only significant in O. biennis (23.40 µg/mL), while the other extracts were weak or unable to reduce the production of ABTS. Based on the antioxidant activities of these plant extracts, 19 extracts with IC50 values less than 100 µg/mL in DPPH assay were selected for further AChE inhibition assay. Among the extracts tested, the IC50 value for Prunella vulgaris var. lilacina NAKAI (18.83 µg/mL) in AChE inhibitory activity was the lowest, followed by O. biennis (20.09 µg/mL) and Pharbitis nil Chosy (22.79 µg/mL). CONCLUSIONS: Considering complex multifactorial etiology of AD, the extracts of P. vulgaris var. lilacina (aerial part), O. biennis (seed) and P. nil (seed) may be safe and ideal candidates for future AD modifying therapies.


Asunto(s)
Antioxidantes/farmacología , Inhibidores de la Colinesterasa/farmacología , Extractos Vegetales/farmacología , Plantas Medicinales/química , Acetilcolinesterasa/efectos de los fármacos , Acetilcolinesterasa/metabolismo , Antioxidantes/administración & dosificación , Antioxidantes/aislamiento & purificación , Inhibidores de la Colinesterasa/administración & dosificación , Inhibidores de la Colinesterasa/aislamiento & purificación , Depuradores de Radicales Libres/aislamiento & purificación , Depuradores de Radicales Libres/farmacología , Técnicas In Vitro , Concentración 50 Inhibidora , Extractos Vegetales/administración & dosificación , Extractos Vegetales/aislamiento & purificación , República de Corea
16.
Bioorg Med Chem Lett ; 25(22): 5367-71, 2015 Nov 15.
Artículo en Inglés | MEDLINE | ID: mdl-26410076

RESUMEN

Endothelial dysfunction is a key pathological feature of many inflammatory diseases, including sepsis. In the present study, a new caffeoyl glucoside (1) and two known caffeoylated compounds (2 and 3) were isolated from the fruits of Nandina domestica Thunb. (Berberidaceae). The compounds were investigated for their effects against lipopolysaccharide (LPS)-mediated endothelial inflammatory responses. At 20 µM, 1 and 2 inhibited LPS-induced hyperpermeability, adhesion, and migration of leukocytes across a human endothelial cell monolayer in a dose-dependent manner suggesting that 1 and 2 may serve as potential scaffolds for the development of therapeutic agents to treat vascular inflammatory disorders.


Asunto(s)
Berberidaceae/química , Ácidos Cafeicos/química , Endotelio/efectos de los fármacos , Frutas/química , Glucósidos/química , Lipopolisacáridos , Extractos Vegetales/farmacología , Animales , Ácidos Cafeicos/farmacología , Adhesión Celular/efectos de los fármacos , Movimiento Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Endotelio/inmunología , Glucósidos/farmacología , Humanos , Inflamación/tratamiento farmacológico , Espectroscopía de Resonancia Magnética , Estructura Molecular , Extractos Vegetales/química
17.
J Nat Prod ; 78(4): 803-10, 2015 Apr 24.
Artículo en Inglés | MEDLINE | ID: mdl-25835537

RESUMEN

Veratrum nigrum is recognized as a medicinal plant used for the treatment of hypertension, stroke, and excessive phlegm. Chemical investigation of the roots and rhizomes led to the isolation of five new steroidal alkaloids, jervine-3-yl formate (1), veramarine-3-yl formate (2), jerv-5,11-diene-3ß,13ß-diol (3), (1ß,3ß,5ß)-1,3-dihydroxyjervanin-12(13)-en-11-one (4), and veratramine-3-yl acetate (5). Compounds 1 and 5 exhibited potent inhibitory activity (11.3 and 4.7 µM, respectively) against protein tyrosine phosphatase 1B (PTP1B), which has emerged as a viable target for treatment of type 2 diabetes mellitus. On the basis of their PTP1B inhibitory activity, the compounds were evaluated for their potential to enhance glucose uptake in C2C12 skeletal muscle cells. The insulin-stimulated glucose uptake was enhanced upon treatment with compounds 1 and 5 (10 µM) by 49.9 ± 6.5% and 56.0 ± 9.7%, respectively, in a more potent manner than that with the positive control rosiglitazone (47.3 ± 3.4% at 30 µM). These results suggest that steroidal alkaloids serve as practical antidiabetes mellitus leads capable of enhancing glucose uptake.


Asunto(s)
Alcaloides/aislamiento & purificación , Alcaloides/farmacología , Glucosa/metabolismo , Plantas Medicinales/química , Esteroides/aislamiento & purificación , Esteroides/farmacología , Veratrum/química , Alcaloides/química , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Estructura Molecular , Músculo Esquelético/metabolismo , Raíces de Plantas/química , Proteína Tirosina Fosfatasa no Receptora Tipo 1/antagonistas & inhibidores , República de Corea , Rizoma/química , Rosiglitazona , Estereoisomerismo , Esteroides/química , Tiazolidinedionas/farmacología
18.
Biotechnol Bioprocess Eng ; 19(1): 70-75, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-32218679

RESUMEN

Neuraminidase (NA) is one of the two glycoproteins on the surface of influenza virus, which cleaves terminal sialic acid residues and facilitates the release of virions from infected cells. The recombinant NA from H5N1 influenza virus strain A/Vietnam/1203/04 was expressed in Pichia pastoris X33 as a 45 kDa protein that displayed a K m of 9.96 ± 1.26 µM with fluorogenic substrate, 2'-(4-methylumbelliferyl)-α-D-N-acetyl neuraminic acid. Partially purified NA was used for the inhibition and kinetic assays with eight flavonoid compounds and gallic acid. Among them, gallocatechin gallate (GCG) showed the best inhibition against NA with the IC50 of 8.98 ± 0.46 µM and showed a competitive inhibition pattern with K i value of 8.34 ± 0.25 µM. In molecular docking experiments, GCG displayed a binding energy of -13.71 kcal/mol to the active site of NA and the galloyl moiety was required for NA inhibition activity.

19.
J Glob Infect Dis ; 16(1): 27-32, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38680753

RESUMEN

Introduction: The coronavirus disease 2019 (COVID-19) pandemic may have influenced the prevalence and seasonality of acute respiratory viral infections. The aim of the study was to investigate the prevalence of all viruses causing acute viral respiratory infections before and after social distancing measures were lifted. Methods: Cross-sectional study where outpatients and inpatients at Kyunghee University Hospital were examined. From January 2021 to December 2022, respiratory samples were analyzed using multiplex reverse transcriptase real-time polymerase chain reaction. Results: Of 3953 samples obtained, 412 (10.42%) were positive for acute respiratory viral infection, and 502 viruses were detected. The number of viral infections increased from 184 in 2021 to 318 in 2022. Human metapneumovirus was detected from August to November 2022. Human bocavirus (HBoV) was frequently detected from April to June 2021; however, in 2022, HBoV was frequently detected from July to October. Human parainfluenza virus 3 was rarely detected after its initial frequent detection from October to December 2021 but was continuously observed after frequent detection in September 2022. Co-infection occurred in 78 (18.9%) cases. The most common combination of simultaneous infections was human rhinovirus-HBoV (n = 30, 38.5%). Conclusions: During the COVID-19 pandemic, the incidence of acute respiratory viral infection decreased significantly but increased in 2022 when measures were lifted. The prevalence and seasonality of respiratory viral infections have changed since the pandemic. Our findings contribute to the prediction of an effective response to changes in the prevalence of respiratory viruses.

20.
Clin Spine Surg ; 37(4): 115-123, 2024 May 01.
Artículo en Inglés | MEDLINE | ID: mdl-38637931

RESUMEN

STUDY DESIGN: A retrospective, single-center study. OBJECTIVE: The aim of this study is to evaluate the efficacy and safety of a newly developed extensive dome-like laminoplasty using en bloc resection of the C2 inner lamina in patients with severe cord compression behind the C2 body. SUMMARY OF BACKGROUND DATA: A surgery for severe cord compression behind C2 body is challenging for spinal surgeons. To date, there has been no established solution for severe cord compression behind the C2 body. MATERIALS AND METHODS: Patients with severe cord compression behind the C2 body who underwent posterior surgery consecutively were enrolled. Extensive dome-like laminoplasty that was newly developed was performed to remove en bloc removal of the C2 inner lamina were performed. Preoperative and postoperative canal diameters behind the C2 and mean removed area of the C2 inner lamina were measured using MRI and CT scan. Clinical and radiographic parameters were assessed preoperative and postoperative periods. In addition, perioperative complications were analyzed. RESULTS: A total of 36 patients underwent extensive dome-like laminoplasty and their diagnoses were ossification of the posterior longitudinal ligament (OPLL, 66.7%) and congenital stenosis with spondylosis (33.3%). The mean canal diameter behind the C2 increased from 9.85 (2.28) mm preoperatively to 19.91 (3.93) mm at the last follow-up ( P <0.001). Clinically, neck and arm visual analog scale, Japanese Orthopaedic Association score, and neck disability index significantly improved at postoperative 1 month ( P <0.05), and the scores were maintained until the last follow-up. No meaningful radiographic changes occurred after the surgeries. During the procedures, there were no particular complications, but one patient showed deteriorated myelopathic symptoms and underwent additional C1-C2 decompressive surgery. CONCLUSIONS: After extensive dome-like laminoplasty, surgical outcomes are satisfactory, and complications are rare. This technique may be a viable option for patients with severe cord compression behind the C2 body. LEVEL OF EVIDENCE: Level IV.


Asunto(s)
Laminoplastia , Compresión de la Médula Espinal , Humanos , Laminoplastia/métodos , Masculino , Femenino , Compresión de la Médula Espinal/cirugía , Compresión de la Médula Espinal/diagnóstico por imagen , Persona de Mediana Edad , Resultado del Tratamiento , Anciano , Vértebras Cervicales/cirugía , Vértebras Cervicales/diagnóstico por imagen , Adulto , Imagen por Resonancia Magnética , Estudios Retrospectivos
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