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1.
Int J Biol Macromol ; 190: 463-473, 2021 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-34506859

RESUMO

Xanthine oxidase (XO) plays a vital role in inducing hyperuricemia and increasing the level of superoxide free radicals in blood, and is proved as an important target for gout. Chrysoeriol (CHE) is a natural flavone with potent XO inhibitory activity (IC50 = 2.487 ± 0.213 µM), however, the mechanism of interaction is still unclear. Therefore, a comprehensive analysis of the interaction between CHE and XO was accomplished by enzyme kinetics, isothermal titration calorimetry (ITC), multi-spectroscopic methods, molecular simulation and ADMET. The results showed that CHE acted as a rapid reversible and competitive-type XO inhibitor and its binding to XO was driven by hydrogen bonding and hydrophobic interaction. Moreover, CHE exhibited a strong fluorescence quenching effect through a static quenching procedure and induced conformational changes of XO. Its binding pattern with XO was revealed by docking study and the binding affinity to XO was enhanced by the interactions with key amino acid residues in the active pocket of XO. Further, CHE showed good stability and pharmacokinetic behavior properties in molecule dynamic simulation and ADMET prediction. Overall, this study shed some light on the mechanism of interaction between CHE and XO, also provided some valuable information concerning the future therapeutic application of CHE as natural XO inhibitor.

2.
Pharmacol Res ; 169: 105615, 2021 07.
Artigo em Inglês | MEDLINE | ID: mdl-33872808

RESUMO

Naturally occurring coumestans are known as a collection of plant-derived polycyclic aromatic secondary metabolites which are characterized by the presence of an oxygen heterocyclic four-ring system comprising a coumarin moiety and a benzofuran moiety sharing a CË­C bond. Recently, there is an increasing attention in excavating the medicinal potential of coumestans, particularly coumestrol, wedelolactone, psoralidin and glycyrol, in a variety of diseases. This review is a comprehensive inventory of the chemical structures of coumestans isolated from various plant sources during the period of 1956-2020, together with their reported biological activities. 120 molecules were collected and further classified as coumestans containing core skeleton, dimethylpyranocoumestans, furanocoumestans, O-glycosylated coumestans and others, which showed a wide range of pharmacological activities including estrogenic, anti-cancer, anti-inflammatory, anti-osteoporotic, organ protective, neuroprotective, anti-diabetic and anti-obesity, antimicrobial, immunosuppressive, antioxidant and skin-protective activities. Furthermore, this review focuses on the counteraction of coumestans against bone diseases and organ damages, and the involved molecular mechanisms, which could provide important information to better understand the medicinal values of these compounds. This review is intended to be instructive for the rational design and development of less toxic and more effective drugs with a coumestan scaffold.

3.
Dose Response ; 18(4): 1559325820939751, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33100936

RESUMO

Berberine (BBR), a major active component of Rhizoma coptidis, is one of the most promising agents for breast cancer adjuvant therapy. It is well accepted that BBR could exhibit remarkable anticancer efficacy with few side effects, and when treated with chemotherapeutic agents in combination, BBR could enhance the chemosensitivity of cancer cells. Our previous study reported that low-dose BBR (LDB) induced hormetic effect and attenuated the anticancer activity of chemotherapeutic agents. However, the underlying mechanisms are still unclear. In this study, we confirmed that LDB could promote cancer cell proliferation and antagonize the anti-breast cancer activities of chemotherapeutic agents. And the mechanisms were proved to be induction of autophagy and antioxidation by LDB. Our results showed that LDB could mildly induce reactive oxygen species, raise the level of autophagy by promoting the phosphorylation of adenosine monophosphate-activated protein kinase, and promote antioxidant enzymes expression through activating nuclear factor erythroid 2-related factor 2 in breast cancer cells. These findings revealed a potential negative impact of BBR on its adjuvant anti-breast cancer therapy, providing guidance for a safe and effective use of naturally originated medicines in the clinic.

4.
Chin Med ; 15: 79, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32765640

RESUMO

Background: Glycine tabacina (Labill.) Benth, one of the traditional Chinese herbal medicines, has been used for treatment of nephritis, osteoporosis, rheumatism, and menopausal syndrome. The aim of this study was to illuminate the therapeutic effect and mechanism of Glycine tabacina aqueous extract (GATE) in the treatment of nephrotic syndrome (NS). Methods: UHPLC-DAD-MS/MS was used to analyze the chemical profile of GATE. Adriamycin (ADR)-induced NS mouse model and network pharmacology methods were conducted to explore the protective effect and mechanism of GATE on NS treatment. Results: GATE administration significantly ameliorated symptoms of proteinuria and hyperlipidemia in NS mice, as evidenced by reduced excretion of urine protein and albumin, and decreased plasma levels of total cholesterol and triglyceride. Decreased blood urea nitrogen (BUN) and creatinine levels in NS mice suggested that GATE could prevent renal function decline caused by ADR. GATE treatment also inhibited ADR-induced pathological lesions of renal tissues as indicated by periodic acid Schiff staining. Six flavonoids of GATE were identified by using UHPLC-DAD-MS/MS. Network pharmacology analysis indicated that the protection of GATE in treating NS might be associated with the regulation of oxidative stress and inflammation. In addition, the in vivo experiment validated that treatment with GATE markedly decreased reactive oxygen species production, malonaldehyde level, and increased superoxide dismutase activity both in plasma and renal tissues. TNF-α level in plasma and protein expression in kidney were significantly decreased in GATE treatment groups. Conclusions: Combination of network pharmacology analysis and experimental verification revealed that GATE exerts anti-NS effect possibly through modulating oxidative stress and inflammation, suggesting the potential application of GATE or its derivatives in the prevention and treatment of NS and other related kidney diseases.

5.
J Agric Food Chem ; 68(39): 10664-10677, 2020 Sep 30.
Artigo em Inglês | MEDLINE | ID: mdl-32530618

RESUMO

Glycine tabacina (Labill.) Benth is an edible medicinal herb for rheumatoid arthritis (RA) treatment in folk medicine. Current phytochemical research on this dried herb led to the isolation of eight new coumestans, named glytabastan A-H (1-8), and twenty-three known compounds 9-31. Their structures were elucidated using spectroscopic methods. The antiarthritic activities of all isolates were evaluated, and the results showed that coumestans 1-6 and 8-10 could inhibit arthritic inflammation in vitro, while coumestans 1, 2, 9, and 10 significantly blocked the osteoclastogenesis induced by receptor activator of nuclear factor (NF) κB ligand (RANKL). Moreover, network pharmacological analysis revealed that the anti-RA effect of G. tabacina involved multitargets, multipathways such as PI3K/Akt and MAPK signaling pathways, and various biological processes such as inflammatory response and cytokine-mediated signaling pathways. These results suggested that this species and its novel coumestans could serve as potential antiarthritic agents for functional food or medicinal use.


Assuntos
Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Fabaceae/química , Animais , Artrite Reumatoide/tratamento farmacológico , Artrite Reumatoide/genética , Artrite Reumatoide/imunologia , Artrite Reumatoide/fisiopatologia , Medicamentos de Ervas Chinesas/isolamento & purificação , Humanos , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Macrófagos/efeitos dos fármacos , Macrófagos/imunologia , Camundongos , Osteoclastos/citologia , Osteoclastos/efeitos dos fármacos , Osteoclastos/imunologia , Osteogênese/efeitos dos fármacos , Fosfatidilinositol 3-Quinases/genética , Fosfatidilinositol 3-Quinases/imunologia , Ligante RANK/genética , Ligante RANK/imunologia , Células RAW 264.7 , Membrana Sinovial/efeitos dos fármacos , Membrana Sinovial/imunologia
6.
J Ethnopharmacol ; 258: 112855, 2020 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-32376366

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Glycine tabacina (Labill.) Benth has been used as a traditional Chinese herbal medicine for the treatment of rheumatoid arthritis (RA) and joint infection. It is also one of the sources of the renowned native herbal medicine 'I-Tiao-Gung' in Taiwan. AIM OF THE STUDY: This study aimed to investigate anti-arthritic effects and underlying mechanisms of dolichosin A (DoA), a coumestan compound isolated from G. tabacina, by the integration of network pharmacology and experimental pharmacology. MATERIALS AND METHODS: Putative therapeutic targets and potential pharmacological mechanisms of DoA for RA treatment were predicted by network pharmacology approach. The regulated network of DoA acting on RA was constructed using Cytoscape 3.7.1. Anti-arthritic effects of DoA and predicted mechanisms were further validated using IL-1ß-induced SW982 human synovial cell model and RANKL-induced osteoclastogenesis model. RESULTS: A regulatory network of DoA-targets-pathways-RA was successfully constructed using network pharmacology approach. In this network, 65 candidate targets of DoA related to its therapeutic effect on RA were identified and the functional enrichment analysis revealed that these candidate targets were significantly involved in 12 central signaling pathways such as PI3K/AKT pathway, MAPK pathway and osteoclast differentiation. Furthermore, we found that DoA could significantly inhibit IL-1ß-induced inflammation in SW982 human synovial cells, as evidenced by the decreased levels of pro-inflammatory mediators (TNF-α, IL-6 and COX-2) and MMP-3. DoA also suppressed RANKL-induced osteoclastogenesis in vitro, as evidenced by decreased number of TRAP-positive multinucleated osteoclasts and reduced TRAP activity. Further experimental mechanism evidence confirmed the predicted results of network pharmacology that the blockade of PI3K/AKT and MAPK pathways activation was closely associated with these regulated processes of DoA. CONCLUSIONS: Our results demonstrated that DoA exhibited strong anti-arthritic activity through suppressing PI3K/AKT and MAPK pathways activation in activated synovial cells and osteoclasts, suggesting its potential as a hopeful candidate for the development of novel agents for the prevention and treatment of RA.


Assuntos
Cumarínicos/farmacologia , Fabaceae/química , Inflamação/prevenção & controle , Osteogênese/efeitos dos fármacos , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antirreumáticos/isolamento & purificação , Antirreumáticos/farmacologia , Artrite Reumatoide/tratamento farmacológico , Artrite Reumatoide/fisiopatologia , Linhagem Celular Tumoral , Cumarínicos/isolamento & purificação , Humanos , Inflamação/patologia , Mediadores da Inflamação/metabolismo , Interleucina-1beta , Osteoclastos/efeitos dos fármacos , Osteoclastos/metabolismo , Ligante RANK , Sinoviócitos/efeitos dos fármacos , Sinoviócitos/patologia
7.
Carcinogenesis ; 41(6): 804-816, 2020 07 10.
Artigo em Inglês | MEDLINE | ID: mdl-31504230

RESUMO

Autophagy is an evolutionarily conserved mechanism to protect the cells from unfavorable environmental conditions. Inhibition of autophagy has been contemplated as a novel strategy to enhance anticancer efficacy of existing chemotherapeutic agents. We previously reported that pulsatilla saponin D (PSD) was a potent autophagy inhibitor. However, its anticancer potential as adjuvant and underlying mechanisms are still unknown. In this study, we identified that PSD induced the formation of autophagosome in MCF-7 and MDA-MB-231 breast cancer cells. However, PSD alone and particularly co-treatment with camptothecin remarkably increased p62 protein levels, indicating that PSD strongly inhibited the autophagic cargo degradation. The mechanistic study indicated that PSD profoundly abolished the co-localization of EGFP-LC3 and lysosomal-specific probe LysoTracker Red, suggesting that the autophagosome-lysosome fusion was blocked by PSD, which is similar to the action of chloroquine. In addition, PSD significantly increased lysosomal pH and inhibited the activation of lysosomal cathepsins in both breast cancer cell lines. Furthermore, the accrued p62 resulted in accumulation of ubiquitinated proteins owing to the interaction with p62 and delivery to the malfunctioned autophagosome by PSD. Finally, we demonstrated that PSD synergistically enhanced the anticancer activity of camptothecin (CPT) in cultured breast cancer cells and in mouse xenograft tumor models. Our results indicated that PSD inhibited autophagic flux via blocking autophagosome-lysosome fusion and lysosomal acidification, which may confer a synergistic anti-breast cancer activity of PSD and CPT.


Assuntos
Protocolos de Quimioterapia Combinada Antineoplásica/farmacologia , Autofagia , Biomarcadores Tumorais/metabolismo , Neoplasias da Mama/tratamento farmacológico , Lisossomos/metabolismo , Proteínas de Ligação a RNA/metabolismo , Ubiquitina/metabolismo , Animais , Apoptose , Biomarcadores Tumorais/genética , Neoplasias da Mama/metabolismo , Neoplasias da Mama/patologia , Camptotecina/administração & dosagem , Proliferação de Células , Feminino , Regulação Neoplásica da Expressão Gênica , Humanos , Lisossomos/efeitos dos fármacos , Lisossomos/patologia , Camundongos , Camundongos Nus , Proteínas de Ligação a RNA/genética , Saponinas/administração & dosagem , Células Tumorais Cultivadas , Ubiquitinação , Ensaios Antitumorais Modelo de Xenoenxerto
8.
Nat Prod Res ; 34(7): 981-987, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30636441

RESUMO

A new isoflavone, milletenol A (1), along with four known flavonoids (2-5) were isolated from the seeds of Millettia pachycarpa. The structure of 1 was established by extensive spectroscopic methods while known compounds were identified by comparisons with literature data. Compound 1 and 2 showed significant anti-inflammatory activities against nitric oxide production in LPS-induced RAW264.7 macrophages. The state of CuSO4-stimulated inflammation was effectively alleviated by compound 1 in zebrafish. However, no significant cytotoxicity against human breast cancer cells was observed among all isolates.


Assuntos
Anti-Inflamatórios/isolamento & purificação , Isoflavonas/isolamento & purificação , Millettia/química , Sementes/química , Animais , Anti-Inflamatórios/farmacologia , Humanos , Isoflavonas/química , Isoflavonas/farmacologia , Lipopolissacarídeos , Macrófagos/efeitos dos fármacos , Camundongos , Óxido Nítrico/biossíntese , Células RAW 264.7 , Peixe-Zebra
9.
Inflammopharmacology ; 28(1): 289-297, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31446590

RESUMO

Rhynchosia minima root, a folk herbal medicine in southern China, is used to relieve itch and swelling. In this study, we examined the anti-inflammatory property of an ethanol fraction (EEF6) from R. minima root on lipopolysaccharide (LPS)-induced RAW 264.7 cells, as well as its underlying mechanism. The compound composition of EEF6 was determined by high-performance liquid chromatography-mass spectrometry. The result showed that five flavonoids compounds, 2',4',5,7-tetrahydroxyisoflavone, genistein-8-C-glucopyranoside, tricin, genistein, and daidzein, were identified in EEF6. In addition, EEF6 exhibited potent anti-inflammatory ability against LPS-stimulated RAW 264.7 cells via MAPK/NF-κB signaling pathways by decreasing the secretion of nitric oxide (NO), interleukin (IL)-6, TNF-α, and monocyte chemotactic protein (MCP)-1, inhibiting the translocation of p65 from cytoplasm to nucleus, and suppressing the phosphorylation of ERK, JNK, and p38. These results indicated that EEF6 could be a promising ingredient for inflammation management.


Assuntos
Anti-Inflamatórios/farmacologia , Fabaceae/química , Flavonoides/farmacologia , Inflamação/tratamento farmacológico , Raízes de Plantas/química , Transdução de Sinais/efeitos dos fármacos , Animais , Linhagem Celular , Citocinas/metabolismo , Genisteína/farmacologia , Inflamação/induzido quimicamente , Inflamação/metabolismo , Interleucina-6/metabolismo , Isoflavonas/farmacologia , Lipopolissacarídeos/farmacologia , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , NF-kappa B/metabolismo , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Fosforilação/efeitos dos fármacos , Células RAW 264.7 , Fator de Necrose Tumoral alfa/metabolismo
10.
Bioorg Chem ; 88: 102949, 2019 07.
Artigo em Inglês | MEDLINE | ID: mdl-31054435

RESUMO

This current study described the design and synthesis of a series of derivatives based on a natural pyranoisaflavone, which was obtained from the seeds of Millettia pachycarpa and displayed attractive BChE inhibition and high selectivity in our previous study. The inhibitory potential of all derivatives against two cholinesterases was evaluated. Only a few compounds demonstrated AChE inhibitory activity at the tested concentrations, while 26 compounds showed significant inhibition on BChE (the IC50 values varied from 9.34 µM to 0.093 µM), most of them presented promising selectivity to ward BChE. Prediction of ADME properties for 7 most active compounds was performed. Among them, 9g (IC50 = 222 nM) and 9h (IC50 = 93 nM) were found to be the most potent BChE inhibitors with excellent selectivity over AChE (SI ratio = 1339 and 836, respectively). The kinetic analysis demonstrated both of them acted as mixed-type BChE inhibitors, while the molecular docking results indicated that they interacted with both residues in the catalytic active site. A cytotoxicity test on PC12 cells showed that both 9g and 9h had a therapeutic safety range similar to tacrine. Overall, the results indicate that 9h could be a good candidate of BChE inhibitors.


Assuntos
Produtos Biológicos/farmacologia , Butirilcolinesterase/metabolismo , Carbamatos/antagonistas & inibidores , Inibidores da Colinesterase/farmacologia , Isoflavonas/farmacologia , Pironas/farmacologia , Animais , Produtos Biológicos/química , Produtos Biológicos/isolamento & purificação , Carbamatos/metabolismo , Sobrevivência Celular/efeitos dos fármacos , Inibidores da Colinesterase/química , Inibidores da Colinesterase/isolamento & purificação , Relação Dose-Resposta a Droga , Humanos , Isoflavonas/química , Isoflavonas/isolamento & purificação , Estrutura Molecular , Células PC12 , Pironas/química , Pironas/isolamento & purificação , Ratos , Relação Estrutura-Atividade
11.
Molecules ; 24(5)2019 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-30832224

RESUMO

Background: Polyphyllin VII (PP7), a steroidal saponin from Paris polyphylla, has been found to exert strong anticancer activity. Little is known about the anti-inflammatory property of PP7. In this study, the anti-inflammatory activity and its underlying mechanisms of PP7 were evaluated in lipopolysaccharide (LPS)-stimulated RAW264.7 cells and in multiple animal models. Methods: The content of nitric oxide (NO) was determined by spectrophotometry. The levels of prostaglandin E2 (PGE2) and cytokines were measured by enzyme-linked immunosorbent assay (ELISA) assay. The mRNA expression of pro-inflammatory genes was determined by qPCR. The total and phosphorylated protein levels were examined by Western blotting. The in vivo anti-inflammatory activities were evaluated by using mouse and zebrafish models. Results: PP7 reduced the production of NO and PGE2 and the protein and mRNA expressions of pro-inflammatory cytokines (TNF-α, IL-1ß, and IL-6) and enzymes (inducible NO synthase [iNOS], cyclooxygenase-2 [COX-2], and Matrix metalloproteinase-9 [MMP-9]) in LPS-induced RAW264.7 cells by suppressing the NF-κB and MAPKs pathways. Notably, PP7 markedly inhibited xylene-induced ear edema and cotton pellet-induced granuloma formation in mice and suppressed LPS and CuSO4-induced inflammation and toxicity in zebrafish embryos. Conclusion: This study demonstrates that PP7 exerts strong anti-inflammatory activities in multiple in vitro and in vivo models and suggests that PP7 is a potential novel therapeutic agent for inflammatory diseases.


Assuntos
Anti-Inflamatórios/farmacologia , Inflamação/tratamento farmacológico , Óxido Nítrico/genética , Saponinas/farmacologia , Animais , Anti-Inflamatórios/química , Ciclo-Oxigenase 2/genética , Dinoprostona/genética , Modelos Animais de Doenças , Ensaio de Imunoadsorção Enzimática , Regulação da Expressão Gênica/efeitos dos fármacos , Humanos , Inflamação/induzido quimicamente , Inflamação/patologia , Interleucina-1beta/genética , Interleucina-6/genética , Lipopolissacarídeos/toxicidade , MAP Quinase Quinase 1/genética , Camundongos , NF-kappa B/genética , Óxido Nítrico Sintase Tipo II/genética , Células RAW 264.7/efeitos dos fármacos , Saponinas/química , Transdução de Sinais/efeitos dos fármacos , Fator de Necrose Tumoral alfa/genética , Peixe-Zebra/embriologia , Peixe-Zebra/genética
12.
Bioorg Med Chem Lett ; 29(10): 1194-1198, 2019 05 15.
Artigo em Inglês | MEDLINE | ID: mdl-30910460

RESUMO

Millettia pachycarpa Benth, a widely used anthelminthic drug in folk, is rich in flavonoids with various bioactivities. This study aimed to identify active flavonoids with anti-Alzheimer's disease (AD) effect from its seeds by a bioassay-guided isolation. A novel rotenoid with unusual oxidative ring-opening skeleton (10) and nine known flavonoids (1-9) were obtained, and their structures were elucidated by NMR and HR-ESIMS analysis. Among all isolates, 7 and 8 showed selective butyrylcholinesterase (BChE) inhibitory activities (IC50 = 2.34 and 11.49 µM, respectively), while 3 was classified as a dual-action inhibitor against acetylcholinesterase (AChE) and BChE (IC50 AChE = 17.14 µM, IC50 BChE = 5.68 µM). Further kinetic study revealed that 3, 7, and 8 were mixed-type BChE inhibitors, but 3 was a competitive AChE inhibitor. Their strong binding affinities to BChE were confirmed by fluorescence quenching analysis. Additionally, 3 and 8 exhibited potent inhibitory effects against ß-amyloid peptide aggregation. These results revealed M. pachycarpa could be a valuable source for anti-AD leads development, and compounds 3, 7 and 8 were worthy of further study as multifunctional or specific agents for AD treatment.


Assuntos
Peptídeos beta-Amiloides/metabolismo , Inibidores da Colinesterase/química , Flavonoides/química , Millettia/química , Acetilcolinesterase/química , Acetilcolinesterase/metabolismo , Butirilcolinesterase/química , Butirilcolinesterase/metabolismo , Inibidores da Colinesterase/metabolismo , Flavonoides/metabolismo , Cinética , Millettia/metabolismo , Extratos Vegetais/química , Sementes/química , Sementes/metabolismo , Relação Estrutura-Atividade
13.
J Ethnopharmacol ; 237: 20-27, 2019 Jun 12.
Artigo em Inglês | MEDLINE | ID: mdl-30880257

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: The whole plant of Glycine tabacina (Labill.) Benth has been used as a traditional herbal medicine to treat rheumatism, ostealgia and nephritis in China. It is also one of the sources of the renowned native herbal medicine 'I-Tiao-Gung' in Taiwan. AIM OF THE STUDY: This study aimed to investigate the anti-arthritic effect of ethanol extract of G. tabacina (GTE) in a collagen-induced arthritis (CIA) rat model. MATERIALS AND METHODS: The chemical profile of GTE was analyzed by HPLC-UV. The CIA was induced in male Wistar rats by intradermal injection of bovine type II collagen at tail root, back and ankle joints. The rats were orally administrated daily with GTE (1.11, 2.22 and 4.44 g dry weight of herb powder per kg body weight) from day 0 and continued for 30 days. Swelling volume and thickness of paw, arthritis index, X-radiographs and histopathological changes were examined to assess the severity of arthritis. Furthermore, the levels of pro-inflammatory cytokines, such as interleukin1ß (IL-1ß), IL-6 and tumor necrosis factor α (TNF-α), total superoxide dismutase (T-SOD) activity and malonaldehyde (MDA) level were measured to preliminarily explore the possible mechanisms. RESULTS: Oral administration of GTE significantly ameliorated the arthritic symptoms in CIA rat model, as indicated by the effects on paws swelling and arthritis index. X-radiographic analysis and histopathological examinations demonstrated that GTE effectively protected the bone and cartilage of joints from erosion, lesion and deformation. The efficacy of GTE treatment on CIA was comparable to that of indomethacin (positive drug). Besides, the overproduction of IL-1ß, IL-6 and TNF-α was remarkably inhibited in the serum of all GTE treatment groups. The restoration of serum T-SOD activity and MDA level proved that GTE administration alleviated the oxidative stress in CIA rats. CONCLUSIONS: GTE exhibited strong anti-CIA activity through inhibiting pro-inflammatory cytokines and oxidation in rats, suggesting its potential preventive and therapeutic effects on rheumatoid arthritis (RA).


Assuntos
Anti-Inflamatórios/uso terapêutico , Artrite Experimental/tratamento farmacológico , Fabaceae , Extratos Vegetais/uso terapêutico , Animais , Articulação do Tornozelo/efeitos dos fármacos , Articulação do Tornozelo/patologia , Anti-Inflamatórios/farmacologia , Artrite Experimental/imunologia , Artrite Experimental/patologia , Citocinas/sangue , Articulação do Joelho/efeitos dos fármacos , Articulação do Joelho/patologia , Masculino , Malondialdeído/sangue , Oxirredução , Fitoterapia , Extratos Vegetais/farmacologia , Ratos Wistar , Superóxido Dismutase/sangue
14.
J Asian Nat Prod Res ; 21(12): 1170-1176, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30585518

RESUMO

Two new stilbenoids bletilol D (1) and bletilol E (2), together with five known compounds were isolated from Bletilla striata. Three of them (3, 4, and 7) were obtained from this genus for the first time. Their structures were elucidated by spectroscopic methods and comparing with data reported in literatures. The cytotoxic activities of compounds 1-7 against MCF-7 (human breast cancer) and A549 (human lung carcinoma) cell lines were evaluated by MTT assay. Compound 2 showed weak cytotoxicity against MCF-7 and A549 cell lines with IC50 values of 36.32 ± 1.17 and 36.48 ± 1.12 µM, respectively, and 5 exhibited weak cytotoxicity against MCF-7 cell line with IC50 value of 57.09 ± 2.03 µM.


Assuntos
Orchidaceae , Estilbenos , Humanos , Estrutura Molecular
15.
Biochim Biophys Acta Gen Subj ; 1862(8): 1751-1759, 2018 08.
Artigo em Inglês | MEDLINE | ID: mdl-29763643

RESUMO

BACKGROUND: Polysaccharides, one of the active ingredients in herbal medicine, are proved to enhance innate immunity against infections. The aim of this study is to explore the immunoregulatory ability of polysaccharides from Rhynchosia minima root in vitro and in vivo. METHODS: Polysaccharide fractions of R. minima root were obtained by chromatographic column. The content of NO was measured by spectrophotometry. The levels of cytokines (tumor necrosis factor-α, TNF-α; interleukin-6, IL-6; and monocyte chemoattractant protein-1, MCP-1) were determined by enzyme-linked immuno-sorbent assay (ELISA) kits. The translocation of p65 into the nucleus was imaged by confocal microscopy. The mRNA expression of TNF-α, IL-6, and MCP-1 was determined by quantitative real-time PCR. T-lymphocyte subgroups of spleen from immunosuppressive mouse were evaluated by flow cytometry. RESULTS: PRM3 remarkably enhanced the phagocytic ability of macrophages and promoted the release of NO and the secretion of cytokines (TNF-α, IL-6, and MCP-1) from macrophages. Simultaneously, PRM3 potently activated NF-κB signaling pathway via Toll-like receptor 4 (TLR4). In addition, PRM3 obviously increased the levels of serum cytokines, markedly up-regulated the percentages of CD3+ and CD4+ T lymphocytes and the CD4+/CD8+ ratio of splenocytes, and effectively attenuated cyclophosphamide induced immunosuppression in mice. CONCLUSIONS: PRM3 profoundly enhanced the immune function in vitro and in vivo through TLR4-NF-κB pathway and is a promising candidate of immunopotentiator which could be applied in functional foods or drugs. GENERAL SIGNIFICANCE: This study reported a polysaccharide PRM3 from R. minima root exhibited potent immunoenhancing activity and significantly alleviated cyclophosphamide-induced immunosuppression through TLR4-NF-κB pathway.


Assuntos
Fabaceae/química , Regulação da Expressão Gênica/efeitos dos fármacos , Macrófagos/imunologia , NF-kappa B/metabolismo , Raízes de Plantas/química , Polissacarídeos/farmacologia , Receptor 4 Toll-Like/metabolismo , Animais , Células Cultivadas , Citocinas/metabolismo , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , Camundongos Endogâmicos C57BL , Camundongos SCID , Polissacarídeos/química , Polissacarídeos/isolamento & purificação , Transdução de Sinais/efeitos dos fármacos
16.
Nat Prod Commun ; 11(5): 621-2, 2016 May.
Artigo em Inglês | MEDLINE | ID: mdl-27319133

RESUMO

Ten flavonoids (1-10), including a new glycoside (nevadensin-7-sambubioside, 7), together with a phenylpropanoid glycoside (11) were isolated from Lysionotus pauciflorus. Their structures were elucidated by a combination of spectroscopic methods and comparing with literature data. Five compounds (1, 3, 4, 8, and 9) were obtained from the family Gesneriaceae for the first time. The new compound was evaluated in vitro for anticholinesterase activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), but was found to be inactive.


Assuntos
Flavonoides/isolamento & purificação , Magnoliopsida/química , Flavonoides/química , Estrutura Molecular
17.
Nat Prod Res ; 30(17): 1945-9, 2016 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-26407107

RESUMO

The anticholinesterase and antioxidant effects of five different extracts of Piper nigrum were evaluated. Twenty-one known alkamides were isolated from active ethyl acetate extract and investigated for their cholinesterase inhibitory and antioxidant effects. Among them, piperine (2), piperettine (5) and piperettyline (20) exhibited dual inhibition against AChE and BChE, and feruperine (18) was the most potent selective inhibitor of BChE. Molecular docking simulation was performed to get insight into the binding interactions of the ligands and enzymes. In addition, N-trans-feruloyltyramine (3) contributed to the strongest DPPH radical-scavenging activity. The self-induced Aß aggregation inhibition of 2, 5 and 18 was further evaluated. Results indicated that some alkamides could be multifunctional lead candidates for Alzheimer's disease therapy.


Assuntos
Antioxidantes/farmacologia , Inibidores da Colinesterase/farmacologia , Piper nigrum/química , Extratos Vegetais/farmacologia , Doença de Alzheimer/tratamento farmacológico , Antioxidantes/química , Inibidores da Colinesterase/química , Frutas/química , Humanos , Simulação de Acoplamento Molecular
18.
Nat Prod Commun ; 9(8): 1125-6, 2014 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-25233587

RESUMO

A new acorane sesquiterpene glucoside, 1R,3S,4R,5R,10R-3,10-dihydroxyacoronene-3-O-beta-D-gluc-oside (1), was isolated from the EtOAc-soluble partition of the ethanol extract of Lysionotus pauciflorus, together with six known compounds, namely p-hydroxybenzoic acid (2), vanillic acid (3). caffeic acid (4). beta-hydroxypropiosyringone (5), alpha,beta-dihydroxypropiosyringone (6), and lyoniresinol (7). The structure of the new compound was elucidated on the basis of spectroscopic methods, including 1D and 2D NMR, and high-resolution MS analysis. The absolute configuration of 1 was determined from CD spectra. When evaluated against several bacterial and fungal strains, and human cancer cell lines, compound 1 and its aglycone were inactive.


Assuntos
Glucosídeos/química , Magnoliopsida/química , Extratos Vegetais/química , Sesquiterpenos/química , Espectroscopia de Ressonância Magnética , Estrutura Molecular
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