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1.
Food Sci Biotechnol ; 32(9): 1215-1223, 2023 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-37362808

RESUMO

Artemisia iwayomogi (AI) is a perennial herb found in Korea. Its ground parts are dried and used in food and traditional medicine for treating hepatitis, inflammation, cholelithiasis, and jaundice. In this study, the anti-obesity effects of single compounds isolated from AI extracts on adipose tissue were investigated. Results demonstrated that caffeoylquinic acid analogs strongly inhibited adipocyte differentiation from 3T3-L1 preadipocytes and reduced neutral lipids in differentiated adipocytes. Accordingly, lipid accumulation in adipocytes decreased, and lipid droplets became granulated. Caffeoylquinic acid analogs suppressed the expression of adipocyte differentiation marker genes, namely, Cebpa, Lep, and Fabp4, but it induced the expression of Ucp1, Ppargc1a, and Fgf21, which are browning biomarkers. Therefore, caffeoylquinic acid analogs from AI inhibited preadipocyte differentiation and induced adipose tissue browning, suggesting that these compounds could be promising therapeutic agents for obesity.

2.
J Med Food ; 25(3): 281-292, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-35320013

RESUMO

We evaluated the efficacy and safety of MS-10® for the treatment of menopausal symptoms. A double-blind randomized placebo-controlled clinical trial was performed in 71 premenopausal women for 4 and 12 weeks. A total of 12 individual menopausal symptom scores were assessed using the Kupperman index. MS-10 treatment effectively improved the symptoms by ∼48%. In addition, the quality of life of the women improved by 36% from four perspectives: vasomotor, psychosocial, physical, and sexual symptoms as evaluated using the menopause-specific quality of life (MenQoL) questionnaire. Our results show that MS-10 improves insulin-like growth factor-1 (IGF-1) and estrogen utilization through receptor activation, which are thought to have causative therapeutic effects on menopause and aging inhibition in women. Improvement of Enthotheline-1 (ET-1) in the blood after MS-10 intake led to an improvement in menopausal vascular symptoms. Improvements in bone formation and absorption markers such as osteocalcin, bone-specific alkaline phosphatase (BSALP), C-telopeptides of type I collagen (CTx), deoxypyridinoline (deoxyPYD), and N-telopeptides of type I collagen (NTx) in blood or urine indicate that MS-10 fundamentally improves bone health in women. By confirming the improvement of the psychological well-being index based on the improvement of stress hormone cortisol, MS-10 can solve causative psychological and physical stress-related symptoms. Moreover, various safety tests, such as those for female hormones, were confirmed. Therefore, it can be confirmed that MS-10 is a natural pharmaconutraceutical that causatively and safely improves health of women and aids in antiaging processes.


Assuntos
Cirsium , Envelhecimento Saudável , Menopausa , Extratos Vegetais , Thymus (Planta) , Cirsium/química , Feminino , Fogachos/tratamento farmacológico , Humanos , Extratos Vegetais/uso terapêutico , Qualidade de Vida , Thymus (Planta)/química
3.
J Med Food ; 25(2): 205-212, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-35148195

RESUMO

The extract of Clematis mandshurica Rupr. (CMR) inhibits the production of proinflammatory mediators from lipopolysaccharide-stimulated peritoneal macrophages and concanavalin A-stimulated splenocytes. Erigeron annuus Pers. (EAP) extract suppresses the production of reactive oxygen species (ROS) from preadipocytes. Furthermore, the mixture of the leaf extracts of CMR and EAP, YES-10®, protected against nerve injuries induced by ischemia/reperfusion, suggesting a ROS-scavenging action. These observations show the anti-inflammatory action of YES-10. Inflammatory cytokines can cause alterations in mental function, including depression, by influencing the neurotransmitter system. Thus, it was hypothesized that YES-10 could improve mental health, such as depression, anxiety, and sense of well-being. Seventy-two subjects were recruited and randomly divided into YES-10 or placebo groups (n = 36 per group). Each group was daily administered two capsules orally, containing 200 mg of YES-10 or placebo, for 4 weeks in a double-blinded manner and tested for levels of depression, anxiety, well-being, and mental fitness using the Beck Depression Inventory (BDI), Beck Anxiety Inventory (BAI), Psychosocial Well-being Index (PWI), and Mental Fitness Scale (MFS). In addition, the levels of cortisol (a stress hormone), interleukin-6 (IL-6) (an inflammatory cytokine), and 8-hydroxydeoxyguanosine (8-OHdG; a marker of oxidative stress) in the serum were measured. The BDI, BAI, PWI, and MFS scores decreased significantly, and the serum levels of cortisol, IL-6, and 8-OHdG were lowered significantly (P < .05), suggesting that YES-10 has the ability to improve mental health by relieving stress and by decreasing inflammation and oxidative stress.


Assuntos
Hidrocortisona , Interleucina-6 , Ansiedade , Citocinas , Depressão/tratamento farmacológico , Fadiga , Humanos
4.
Molecules ; 26(8)2021 Apr 12.
Artigo em Inglês | MEDLINE | ID: mdl-33921386

RESUMO

Acanthopanax henryi (Oliv.) Harms (Araliaceae), also known as Eleutherococcus henryi and Caoyewujia (Hengliwujia) in Chinese, is a widely used traditional Chinese herb with the effects of expelling wind and removing dampness, relaxing the muscles and stimulating the blood circulation, and regulating the flow of qi to alleviate pain in the theory of Traditional Chinese Medicine. Acanthopanax henryi (AH, thereafter) possesses ginseng-like activities and is known as ginseng-like herb. In the past decade, a great number of phytochemical and pharmacological studies on AH have been carried out. Several kinds of chemical compositions have been reported, including terpenoids (monoterpenoids, diterpenoids, and triterpenoid saponins), phenylpropanoids, caffeoyl quinic acid derivatives, flavonoids, lignans, sterols, fatty acids, etc., among which, triterpenoid saponins were considered to be the most active components. Considerable pharmacological experiments in vitro have demonstrated that AH possessed anti-neuroinflammatory, anti-adipogenic, anti-inflammatory, antibacterial, anti-cancer, anti-oxidation, anti-AChE, anti-BuChE, and antihyaluronidase activities. The present review is an up-to-date and comprehensive analysis of the botany, phytochemistry, and pharmacology of AH.


Assuntos
Eleutherococcus/química , Etnofarmacologia , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Pesquisa
5.
Molecules ; 26(2)2021 Jan 06.
Artigo em Inglês | MEDLINE | ID: mdl-33419109

RESUMO

Bidens pilosa L. (Asteraceae) has been used historically in traditional Asian medicine and is known to have a variety of biological effects. However, the specific active compounds responsible for the individual pharmacological effects of Bidens pilosa L. (B. pilosa) extract have not yet been made clear. This study aimed to investigate the anti-inflammatory phytochemicals obtained from B. pilosa. We isolated a flavonoids-type phytochemical, isookanin, from B. pilosa through bioassay-guided fractionation based on its capacity to inhibit inflammation. Some of isookanin's biological properties have been reported; however, the anti-inflammatory mechanism of isookanin has not yet been studied. In the present study, we evaluated the anti-inflammatory activities of isookanin using lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. We have shown that isookanin reduces the production of proinflammatory mediators (nitric oxide, prostaglandin E2) by inhibiting the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in LPS-stimulated macrophages. Isookanin also inhibited the expression of activator protein 1 (AP-1) and downregulated the LPS-induced phosphorylation of p38 mitogen-activated protein kinase (MAPK) and c-jun NH2-terminal kinase (JNK) in the MAPK signaling pathway. Additionally, isookanin inhibited proinflammatory cytokines (tumor necrosis factor-a (TNF-α), interleukin-6 (IL-6), interleukin-8 (IL-8), and interleukin-1ß (IL-1ß)) in LPS-induced THP-1 cells. These results demonstrate that isookanin could be a potential therapeutic candidate for inflammatory disease.


Assuntos
Anti-Inflamatórios , Bidens/química , Bioensaio , Chalconas , Macrófagos/metabolismo , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Chalconas/química , Chalconas/isolamento & purificação , Chalconas/farmacologia , Humanos , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Lipopolissacarídeos/toxicidade , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Macrófagos/patologia , Camundongos , Monocinas/metabolismo , Células RAW 264.7 , Células THP-1
6.
Molecules ; 27(1)2021 Dec 21.
Artigo em Inglês | MEDLINE | ID: mdl-35011239

RESUMO

Diabetes is a chronic metabolic disease that is a constant problem. Previous studies have reported that Benincasa cerifera Savi. extracts are effective in treating diabetes and its complications. Benincasae Exocarpium (BE) is a fruit peel of B. cerifera that has been reported to be used for the prevention and treatment of metabolic diseases such as hyperglycemia, obesity, and hyperlipidemia. However, there are not enough studies on the compounds and bioassays to support the efficacy of BE. The inhibitory activity of the BE extracts and fractions against advanced glycation end-products (AGE) formation and α-glucosidase activity was evaluated. These assays are relevant for the treatment of type 2 diabetes and its complications. Based on these results, compounds 1-11 were isolated through bioassay-guided isolation. In addition, we developed a high-performance liquid chromatography (HPLC) method that can simultaneously analyze these 11 compounds. Activity evaluation of the compounds was also conducted, and eight compounds exhibited significant activity. Among these, flavonoid compounds showed strong activity. A quantitative evaluation of eight bioactive compounds (2, 5-11) was conducted. In conclusion, this study demonstrated the potential of BE for prevention and treatment of type 2 diabetes and its complications.


Assuntos
Diabetes Mellitus Tipo 2/tratamento farmacológico , Frutas/química , Produtos Finais de Glicação Avançada/química , Hipoglicemiantes/química , Extratos Vegetais/química , Cromatografia Líquida de Alta Pressão , Avaliação Pré-Clínica de Medicamentos , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Flavonoides/química , Glucosidases/metabolismo , Produtos Finais de Glicação Avançada/farmacologia , Humanos , Hipoglicemiantes/farmacologia , Extratos Vegetais/farmacologia , Relação Estrutura-Atividade
7.
Molecules ; 25(24)2020 Dec 11.
Artigo em Inglês | MEDLINE | ID: mdl-33322478

RESUMO

Previous studies have reported that Hedyotis diffusa Willdenow extract shows various biological activities on cerebropathia, such as neuroprotection and short-term memory enhancement. However, there has been a lack of studies on the inhibitory activity on neurodegenerative diseases such as Alzheimer's disease (AD) through enzyme assays of H. diffusa. Therefore, H. diffusa extract and fractions were evaluated for their inhibitory effects through assays of enzymes related to AD, including acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), and ß-site amyloid precursor protein cleaving enzyme 1 (BACE1), and on the formation of advanced glycation end-product (AGE). In this study, ten bioactive compounds, including nine iridoid glycosides 1-9 and one flavonol glycoside 10, were isolated from the ethyl acetate and n-butanol fractions of H. diffusa using a bioassay-guided approach. Compound 10 was the strongest inhibitor of cholinesterase, BACE1, and the formation of AGEs of all isolated compounds, while compound 5 had the lowest inhibitory activity. Compounds 3, 6, and 9 exhibited better inhibitory activity than other compounds on AChE, and two pairs of diastereomeric iridoid glycoside structures (compounds 4, 8, and 6, 7) showed higher inhibitory activity than others on BChE. In the BACE1 inhibitory assay, compounds 1-3 were good inhibitors, and compound 10 showed higher inhibitory activity than quercetin, the positive control. Moreover, compounds 1 and 3 were stronger inhibitors of the formation of AGE than aminoguanidine (AMG), the positive control. In conclusion, this study is significant since it demonstrated that the potential inhibitory activity of H. diffusa on enzymes related to AD and showed the potential use for further study as a natural medicine for AD treatment on the basis of the bioactive components isolated from H. diffusa.


Assuntos
Acetilcolinesterase/metabolismo , Doença de Alzheimer/tratamento farmacológico , Secretases da Proteína Precursora do Amiloide/metabolismo , Ácido Aspártico Endopeptidases/metabolismo , Bioensaio/métodos , Hedyotis/metabolismo , Ácido Aspártico Endopeptidases/antagonistas & inibidores , Calibragem , Cromatografia Líquida de Alta Pressão , Flavonóis/química , Produtos Finais de Glicação Avançada , Glicosídeos/química , Humanos , Concentração Inibidora 50 , Glicosídeos Iridoides , Análise dos Mínimos Quadrados , Modelos Lineares , Simulação de Acoplamento Molecular , Componentes Aéreos da Planta/metabolismo , Extratos Vegetais/química , Ligação Proteica , Quercetina/química , Solventes , Espectrometria de Massas por Ionização por Electrospray , Estereoisomerismo
8.
Mol Med Rep ; 21(5): 2030-2040, 2020 05.
Artigo em Inglês | MEDLINE | ID: mdl-32186769

RESUMO

Glial cells are the resident immune cells of the central nervous system. Reactive glial cells release inflammatory mediators that induce neurotoxicity or aggravate neurodegeneration. Regulation of glial activation is crucial for the initiation and progression of neuropathological conditions. Constituents of the peach tree (Prunus persica L. Batsch), which has a global distribution, have been found to exert therapeutic effects in pathological conditions, such as rashes, eczema and allergies. However, the therapeutic potential of its aerial parts (leaves, fruits and twigs) remains to be elucidated. The present study aimed to evaluate the anti­inflammatory role of P. persica methanol extract (PPB) on lipopolysaccharide (LPS)­stimulated glial cells. High­performance liquid chromatography coupled with tandem mass spectrometry analysis showed that PPB contained chlorogenic acid and catechin, which have antioxidant properties. Western blot and reverse transcription polymerase chain reaction results indicated that PPB reduced the transcription of various proinflammatory enzymes (nitric oxide synthase and cyclooxygenase­2) and cytokines [tumor necrosis factor­α, interleukin (IL)­1ß and IL­6] in LPS­stimulated BV2 cells. In addition, PPB inhibited the activation of NF­κB and various mitogen­activated protein kinases required for proinflammatory mediator transcription. Finally, nitrite measurement and immunocytochemistry results indicated that PPB also suppressed nitrite production and NF­κB translocation in LPS­stimulated primary astrocytes. Thus, PPB may be used as a potential therapeutic agent for neurodegenerative diseases and neurotoxicity via the suppression of glial cell activation.


Assuntos
Anti-Inflamatórios/farmacologia , Lipopolissacarídeos/efeitos adversos , Neuroglia/efeitos dos fármacos , Extratos Vegetais/farmacologia , Prunus persica/química , Animais , Anti-Inflamatórios/uso terapêutico , Antioxidantes/farmacologia , Citocinas/metabolismo , Feminino , Mediadores da Inflamação , Interleucina-1beta/metabolismo , Interleucina-6/metabolismo , Masculino , Metanol , Quinases de Proteína Quinase Ativadas por Mitógeno/metabolismo , Proteínas Quinases Ativadas por Mitógeno/efeitos dos fármacos , Proteínas Quinases Ativadas por Mitógeno/metabolismo , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Nitritos/metabolismo , Extratos Vegetais/química , Ratos , Ratos Sprague-Dawley , Fator de Necrose Tumoral alfa/metabolismo
9.
J Nat Med ; 74(1): 142-152, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31463669

RESUMO

Cynandione A (CA), isolated from ethyl acetate extract of Cynanchum wilfordii (CW), is a bioactive phytochemical that has been found to be beneficial for the treatment of several diseases. Hepatic de novo lipogenesis is one of the main causes of non-alcoholic fatty liver disease (NAFLD), which is thought to be a hepatic manifestation of certain metabolic syndromes. However, it has not yet been reported if CA has any therapeutic value in these diseases. Here, we investigated whether CA can inhibit hepatic lipogenesis induced by liver X receptor α (LXRα) using an in vitro model. We found that the extract and ethyl acetated layer of CW decreased the mRNA levels of sterol regulatory element-binding protein-1c (SREBP-1c), which plays a crucial role in hepatic lipogenesis. Additionally, we observed that CA could suppress the level of SREBP-1c, which was increased using two commercial LXRα agonists, GW3954 and T0901317. Moreover, the enzymes that act downstream of SREBP-1c were also inhibited by CA treatment. To understand the mechanism underlying this effect, the levels of phosphorylated AMP kinase (pAMPK) were measured after CA treatment. Therefore, CA might increase the pAMPK level by inducing phosphorylation of liver kinase B1 (LKB1), which can then convert AMPK to pAMPK. Taken together, we conclude that CA has an alleviative effect on hepatic lipogenesis through the stimulation of the LKB1/AMPK pathway.


Assuntos
Proteínas Quinases Ativadas por AMP/metabolismo , Compostos de Bifenilo/farmacologia , Cynanchum/química , Lipogênese/efeitos dos fármacos , Proteínas Serina-Treonina Quinases/metabolismo , Quinases Proteína-Quinases Ativadas por AMP , Animais , Células Hep G2 , Humanos , Hidrocarbonetos Fluorados/farmacologia , Fígado/efeitos dos fármacos , Receptores X do Fígado/metabolismo , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Fosforilação , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Proteína de Ligação a Elemento Regulador de Esterol 1/genética , Sulfonamidas/farmacologia
10.
Biomed Res Int ; 2018: 7383869, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30581865

RESUMO

Hibiscus syriacus L. (Malvaceae) is an important ornamental shrub in horticulture and has been widely used as a medical material in Asia. The aim of this study was to assess the antidepressant and neuroprotective effects of a root bark extract of H. syriacus (HSR) and to investigate the underlying molecular mechanisms. Using an animal model of restraint stress, we investigated the effects of HSR on depressive-like behaviors and on the expression levels of serotonin, corticosterone, and neurotrophic factors in the brain. The mice were exposed to restraint stress for 2 h per day over a period of 3 weeks and orally treated with HSR (100, 200, or 400 mg/kg/day). We also examined the neuroprotective effect of HSR using corticosterone-treated human neuroblastoma SK-N-SH cells. The cells were incubated with the extract for 24 h, followed by corticosterone stimulation for 1 h, and then cell viability assay, cellular ATP assay, mitochondrial membrane potential (MMP) assay, cellular reactive oxygen species (ROS) assay, and western blotting were used to investigate the neuroprotective effects of HSR. Administration of HSR not only reduced the immobility times of the restraint-stressed mice in the forced swimming and tail suspension tests, but also significantly increased sucrose preference in the sucrose preference test. In addition, HSR significantly reduced the plasma levels of corticosterone and increased the brain levels of serotonin. The extract also increased the phosphorylation level of cyclic AMP response element-binding (CREB) protein and the expression level of brain-derived neurotrophic factor (BDNF). The in vitro assays showed that HSR pretreatment increased cell viability and ATP levels, recovered MMP, decreased ROS levels, and increased the expression of CREB and BDNF in corticosterone-induced neurotoxicity. Taken together, our data suggest that HSR may have the potential to control neuronal cell damage and depressive behaviors caused by chronic stress.


Assuntos
Antidepressivos/farmacologia , Depressão/tratamento farmacológico , Hibiscus/química , Fármacos Neuroprotetores/farmacologia , Extratos Vegetais/farmacologia , Animais , Comportamento Animal/efeitos dos fármacos , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Corticosterona/metabolismo , Proteína de Ligação ao Elemento de Resposta ao AMP Cíclico/metabolismo , Depressão/metabolismo , Modelos Animais de Doenças , Etanol/química , Elevação dos Membros Posteriores/fisiologia , Humanos , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Casca de Planta/química , Raízes de Plantas/química , Estresse Psicológico/tratamento farmacológico , Estresse Psicológico/metabolismo , Natação/fisiologia
11.
Molecules ; 23(9)2018 Aug 27.
Artigo em Inglês | MEDLINE | ID: mdl-30150550

RESUMO

Inhibition of the formation of advanced glycation end products (AGEs) is an attractive strategy in diabetes treatment. Taraxacum coreanum extracts were suggested to have antidiabetic effects. However, studies on the components of T. coreanum are lacking, and there is no report on the inhibitory effects of T. coreanum on the formation of AGEs. Therefore, T. coreanum extracts and fractions were tested for their inhibitory effects on α-glucosidase and AGEs formation in two systems (bovine serum albumin (BSA)⁻glucose and BSA⁻methylglyoxal (MGO)). Bioassay-guided isolation of compounds from T. coreanum led to six flavones (1⁻6) and four hydroxycinnamic acid derivatives (7⁻11). Compound 11 exhibited the highest inhibitory activity against α-glucosidase and AGEs formation and had the highest content in T. coreanum extract. All compounds except compound 9 showed a stronger inhibition than the positive control in the BSA-glucose and BSA-MGO system. In addition, T. coreanum showed a higher content of bioactive compounds and stronger inhibition of AGE formation and α-glucosidase activity than T. officinale. Our study demonstrated the preventive and therapeutic efficacy of T. coreanum and its potential use as a cost-effective phytopharmaceutical in complementary therapy against type-2 diabetes and its complications.


Assuntos
Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Taraxacum/química , Bioensaio , Ativação Enzimática/efeitos dos fármacos , Glucose/metabolismo , Produtos Finais de Glicação Avançada/metabolismo , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Estrutura Molecular , Extratos Vegetais/isolamento & purificação , alfa-Glucosidases/metabolismo
12.
Mol Med Rep ; 16(6): 9149-9156, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29039503

RESUMO

Acanthopanax gracilistylus (AGS) has long been used in traditional Chinese medicine for the treatment of various inflammatory diseases. 3­O­ß­D­glucopyranosyl 3α, 11α­dihydroxylup­20(29)­en­28­oic acid, acantrifoside A, acankoreoside D, acankoreoside B and acankoreoside A are major lupane­type triterpenoid saponins derived from AGS. In the present study, these five saponins were isolated from AGS by chromatography and their anti­inflammatory activities were investigated in lipopolysaccharide (LPS)­treated RAW264.7 macrophages. Cell viability was evaluated by MTT assay. Tumor necrosis factor (TNF)­α, interleukin (IL)­1ß and NF­κB p65 were measured by ELISA. The gene expression levels of TNF­α and IL­1ß was detected by reverse­transcription polymerase chain reaction. And high­mobility group box 1 (HMGB1) were analyzed by western blotting. The results demonstrated that these five saponins significantly suppressed LPS­induced expression of TNF­α and IL­1ß at the mRNA and protein level in RAW264.7 cells. Further analysis revealed that acankoreoside A and acankoreoside B were able to reduce the secretion of HMGB1 and NF­κB activity induced by LPS in RAW264.7 macrophages. Taken together, these results suggested that the anti­inflammatory activity of AGS­derived saponins may be associated with the downregulation of TNF­α and IL­1ß, and the 'late­phase' proinflammatory cytokine HMGB1, via negative regulation of the NF­κB pathway in RAW264.7 cells.


Assuntos
Proteína HMGB1/biossíntese , Interleucina-1beta/biossíntese , Lipopolissacarídeos/imunologia , Macrófagos/efeitos dos fármacos , Macrófagos/fisiologia , Saponinas/farmacologia , Triterpenos/farmacologia , Fator de Necrose Tumoral alfa/biossíntese , Animais , Sobrevivência Celular/efeitos dos fármacos , Regulação da Expressão Gênica , Interleucina-1beta/genética , Camundongos , NF-kappa B/metabolismo , Células RAW 264.7 , Fator de Necrose Tumoral alfa/genética
13.
Molecules ; 22(10)2017 Sep 29.
Artigo em Inglês | MEDLINE | ID: mdl-28961196

RESUMO

Due to the side effects of synthetic drugs, the therapeutic potential of natural products for Alzheimer's disease (AD) has gained interest. Morinda officinalis has demonstrated inhibitory effects on geriatric diseases, such as bone loss and osteoporosis. However, although AD is a geriatric disease, M. officinalis has not been evaluated in an AD bioassay. Therefore, M. officinalis extracts and fractions were tested for AD-related activity, including inhibition of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), ß-site amyloid precursor protein cleaving enzyme 1 (BACE1), and advanced glycation end-product (AGE) formation. A bioassay-guided approach led to isolation of 10 active compounds, eight anthraquinones (1-8), one coumarin (9), and one phytosterol (10), from n-hexane and ethyl acetate fractions of M. officinalis. The five anthraquinones (4-8) were stronger inhibitors of AChE than were other compounds. Compounds 3 and 9 were good inhibitors of BChE, and compounds 3 and 8 were good inhibitors of BACE1. Compounds 1-5 and 7-9 were more active than the positive control in inhibiting AGE formation. In addition, we first suggested a structure-activity relationship by which anthraquinones inhibit AChE and BACE1. Our findings demonstrate the preventive and therapeutic efficacy of M. officinalis for AD and its potential use as a natural alternative medicine.


Assuntos
Bioensaio/métodos , Descoberta de Drogas , Morinda/química , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Doença de Alzheimer/tratamento farmacológico , Inibidores da Colinesterase/química , Inibidores da Colinesterase/isolamento & purificação , Inibidores da Colinesterase/farmacologia , Descoberta de Drogas/métodos , Humanos , Concentração Inibidora 50 , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Relação Estrutura-Atividade
14.
Int J Mol Sci ; 18(8)2017 Aug 12.
Artigo em Inglês | MEDLINE | ID: mdl-28805698

RESUMO

This study aimed to examine the protective effect of Artemisia iwayomogi extract (AI) against hypertriglyceridemia induced by a high-fat diet (HFD) in mice and to uncover the underlying molecular mechanisms. C57BL/6N mice were fed chow, HFD, HFD + 0.1% AI, HFD + 0.25% AI, or HFD + 0.5% AI for 10 weeks. The addition of 0.25% and 0.5% AI resulted in dose-dependent improvements in the major parameters of hypertriglyceridemia, including plasma triglyceride, free fatty acids, apolipoprotein B, and lipoprotein lipase, with parallel reductions in body weight gain, hepatic lipid accumulation, and insulin resistance. These beneficial effects were accompanied by the activation of adiponectin-adenosine monophosphate-activated protein kinase (AMPK) mediated signaling cascades in the liver, which downregulated molecules involved in lipogenesis and concurrently upregulated molecules related to fatty acid oxidation. The downregulation of molecules involved in very low density lipoprotein assembly, which was associated with improved hepatic insulin signaling, also appeared to contribute to the AI-induced attenuation of hypertriglyceridemia.


Assuntos
Proteínas Quinases Ativadas por AMP/metabolismo , Adiponectina/metabolismo , Artemisia , Hipertrigliceridemia/tratamento farmacológico , Lipoproteínas VLDL/metabolismo , Fígado/efeitos dos fármacos , Extratos Vegetais/uso terapêutico , Animais , Artemisia/química , Dieta Hiperlipídica/efeitos adversos , Ácidos Graxos/metabolismo , Hipertrigliceridemia/etiologia , Hipertrigliceridemia/metabolismo , Hipertrigliceridemia/patologia , Lipogênese/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Transdução de Sinais/efeitos dos fármacos
15.
Biomed Res Int ; 2017: 7375615, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28512639

RESUMO

Blocking the polyol pathway plays an important role preventing diabetic complications. Therefore, aldose reductase (AR) and advanced glycation endproducts (AGEs) formation has significant effect on diabetic complications. Artemisia iwayomogi has long been used as treatment of various diseases in Korea. However, no literatures have reported on AR and AGEs formation inhibitory activities of A. iwayomogi. For these reasons, we aimed to assess that A. iwayomogi had potential as anti-diabetic complications agents. We led to isolation of two coumarins (1 and 2), nine flavonoids (3-11), five caffeoylquinic acids (12-16), three diterpene glycosides (17-19), and one phenolic compound (20) from A. iwayomogi. Among them, hispidulin (4), 6-methoxytricin (6), arteanoflavone (7), quercetin-3-gentiobioside (10), 1,3-di-O-caffeoylquinic acid (13), and suavioside A (18) were first reported on the isolation from A. iwayomogi. Not only two coumarins (1 and 2), nine flavonoids (3-11), and five caffeoylquinic acids (12-16) but also extracts showed significant inhibitor on AR and AGEs formation activities. We analyzed contents of major bioactive compounds in Korea's various regions of A. iwayomogi. Overall, we selected Yangyang, Gangwon-do, from June, which contained the highest amounts of bioactive compounds, as suitable areas for cultivating A. iwayomogi as preventive or therapeutic agent in the treatment of diabetic complications.


Assuntos
Artemisia/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Polímeros/metabolismo , Aldeído Redutase/antagonistas & inibidores , Animais , Complicações do Diabetes/tratamento farmacológico , Complicações do Diabetes/metabolismo , Flavonas/química , Flavonas/farmacologia , Flavonoides/química , Flavonoides/farmacologia , Produtos Finais de Glicação Avançada/antagonistas & inibidores , Glicosídeos/química , Glicosídeos/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Ácido Quínico/análogos & derivados , Ácido Quínico/química , Ácido Quínico/farmacologia , Ratos , Ratos Sprague-Dawley , República da Coreia
16.
Sci Rep ; 7(1): 2251, 2017 05 22.
Artigo em Inglês | MEDLINE | ID: mdl-28533555

RESUMO

The present study aimed to investigate whether scopolin exhibits beneficial effects on high-fat diet (HFD)-induced hepatic steatosis in mice. The involvement of sirtuin 1 (SIRT1) as a molecular target for scopolin was also explored. Scopolin decreased the Km of SIRT1 for p53 and nicotinamide adenine dinucleotide without altering Vmax in a cell-free system. Scopolin alleviated oleic acid-induced lipid accumulation and downregulation of SIRT1 activity in HepG2 cells, and these beneficial effects of scopolin were abolished in the presence of SIRT1 inhibitor. Mice administered 0.02% scopolin for 8 weeks exhibited improved phenotypes of HFD-induced hepatic steatosis along with increased hepatic SIRT1 activity and protein expression. Scopolin resulted in increased deacetylation of sterol regulatory element-binding protein 1c with subsequent downregulation of lipogenic genes, and enhanced deacetylation of protein peroxisome proliferator-activated receptor-γ coactivator 1α with upregulation of fatty acid oxidation genes in livers. Scopolin also enhanced deacetylation of nuclear factor-kappa enhancer binding protein and liver kinase B1 (LKB1), facilitating LKB1/AMP-activated protein kinase signaling cascades. Scopolin attenuated hepatic steatosis through activation of SIRT1-mediated signaling cascades, a potent regulator of lipid homeostasis. Increased hepatic SIRT1 activity and protein expression appeared to be associated with these beneficial effects of scopolin.


Assuntos
Cumarínicos/farmacologia , Dieta Hiperlipídica , Fígado Gorduroso/etiologia , Fígado Gorduroso/metabolismo , Glucosídeos/farmacologia , Transdução de Sinais/efeitos dos fármacos , Sirtuína 1/metabolismo , Animais , Cromatografia Líquida de Alta Pressão , Cumarínicos/química , Dieta Hiperlipídica/efeitos adversos , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Ativação Enzimática/efeitos dos fármacos , Fígado Gorduroso/tratamento farmacológico , Fígado Gorduroso/patologia , Glucosídeos/química , Metabolismo dos Lipídeos/efeitos dos fármacos , Lipogênese/efeitos dos fármacos , Espectroscopia de Ressonância Magnética , Camundongos
17.
Biosci Biotechnol Biochem ; 81(7): 1305-1313, 2017 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-28345393

RESUMO

We investigated the anti-inflammatory effects of 3α-hydroxy-lup-20(29)-en-23, 28-dioic acid (HLEDA)-a lupane-type triterpene isolated from leaves of Acanthopanax gracilistylus W. W.Smith (AGS), as well as the underlying molecular mechanisms in lipopolysaccharide (LPS)-induced RAW264.7 cells. Our results demonstrated that HLEDA concentration-dependently reduced the production of nitric oxide (NO), significantly suppressed LPS-induced expression of TNF-α and IL-1ß at the mRNA and protein levels in RAW264.7 cells. Further analysis revealed that HLEDA could reduce the secretion of High Mobility Group Box 1 (HMGB1). Additionally, the results showed that HLEDA efficiently decreased nuclear factor-kappaB (NF-κB) activation by inhibiting the degradation and phosphorylation of IκBα. These results suggest that HLEDA exerts anti-inflammatory properties in LPS-induced macrophages, possibly through inhibition of the NF-κB signaling pathway, which mediates the expression of pro-inflammatory cytokines. These results warrant further studies that would concern candidate therapy for diseases, such as fulminant hepatitis and rheumatology of triterpenoids in AGS.


Assuntos
Anti-Inflamatórios/farmacologia , Medicamentos de Ervas Chinesas/química , Proteína HMGB1/antagonistas & inibidores , Interleucina-1beta/antagonistas & inibidores , Macrófagos/efeitos dos fármacos , Triterpenos/farmacologia , Fator de Necrose Tumoral alfa/antagonistas & inibidores , Animais , Anti-Inflamatórios/isolamento & purificação , Linhagem Celular , Relação Dose-Resposta a Droga , Eleutherococcus , Expressão Gênica , Proteína HMGB1/genética , Proteína HMGB1/metabolismo , Inflamação , Interleucina-1beta/genética , Interleucina-1beta/metabolismo , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Macrófagos/citologia , Macrófagos/metabolismo , Camundongos , Inibidor de NF-kappaB alfa/antagonistas & inibidores , Inibidor de NF-kappaB alfa/genética , Inibidor de NF-kappaB alfa/metabolismo , Óxido Nítrico/antagonistas & inibidores , Óxido Nítrico/biossíntese , Fosforilação/efeitos dos fármacos , Triterpenos/isolamento & purificação , Fator de Necrose Tumoral alfa/genética , Fator de Necrose Tumoral alfa/metabolismo
18.
Molecules ; 22(3)2017 Mar 11.
Artigo em Inglês | MEDLINE | ID: mdl-28287485

RESUMO

The search for natural inhibitors with anti-diabetes properties has gained increasing attention. Among four selected Smilacaceae family plants, Smilax china L. stems (SCS) showed significant in vitro anti-glycation and rat lens aldose reductase inhibitory activities. Bioactivity-guided isolation was performed with SCS and four solvent fractions were obtained, which in turn yielded 10 compounds, including one phenolic acid, three chlorogenic acids, four flavonoids, one stilbene, and one phenylpropanoid glycoside; their structures were elucidated using nuclear magnetic resonance and mass spectrometry. All solvent fractions, isolated compounds, and stem extracts from plants sourced from six different provinces of South Korea were next tested for their inhibitory effects against advanced glycation end products, as well as aldose reductase. α-Glucosidase, and lipase assays were also performed on the fractions and compounds. Since compounds 3, 4, 6, and 8 appeared to be the superior inhibitors among the tested compounds, a comparative study was performed via high-performance liquid chromatography with photodiode array detection using a self-developed analysis method to confirm the relationship between the quantity and bioactivity of the compounds in each extract. The findings of this study demonstrate the potent therapeutic efficacy of SCS and its potential use as a cost-effective natural alternative medicine against type 2 diabetes and its complications.


Assuntos
Aldeído Redutase/antagonistas & inibidores , Ácido Clorogênico/química , Produtos Finais de Glicação Avançada/antagonistas & inibidores , Glicosídeos/química , Hidroxibenzoatos/química , Smilax/química , Estilbenos/química , Aldeído Redutase/metabolismo , Animais , Ácido Clorogênico/isolamento & purificação , Ácido Clorogênico/farmacologia , Etanol/química , Flavonoides/química , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Produtos Finais de Glicação Avançada/metabolismo , Glicosídeos/isolamento & purificação , Glicosídeos/farmacologia , Glicosilação/efeitos dos fármacos , Hidroxibenzoatos/isolamento & purificação , Hidroxibenzoatos/farmacologia , Cristalino/química , Cristalino/enzimologia , Lipase/antagonistas & inibidores , Lipase/metabolismo , Metanol/química , Estrutura Molecular , Extratos Vegetais/química , Caules de Planta/química , Ratos , Ratos Sprague-Dawley , Solventes/química , Estilbenos/isolamento & purificação , Estilbenos/farmacologia , alfa-Glucosidases/metabolismo
19.
Arch Pharm Res ; 40(2): 204-213, 2017 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-28012047

RESUMO

In a previous study, Quercetin-3-O-ß-D-glucuronopyranoside (QGC) has anti-oxidative and anti-inflammatory effects in vivo. QGC is a flavonoid glucoside extracted from Rumex Aquaticus. We investigated the downstream target proteins involved in IL-1ß-stimulated ROS production and the ability of QGC to inhibit ROS production. Cell viability was determined using the MTT reduction assay. Western blot analysis was performed with antibodies to investigate the activation of three MAPKs, NF-κB, and phosphorylated IκB-α (pIB), and the expression of COX-2. 2',7'-dichlorofluorescin diacetate was used to detect the generation of intracellular ROS species. When the cells were exposed to media containing IL-1ß for 18 h, cell viability was not affected. QGC did not reduce the COX-2 expression induced by IL-1ß. However; QGC attenuated the production of intracellular ROS induced by IL-1ß. IL-1ß increased the expression of ERK, p38 MAPK, and pIB, and nuclear translocation of NF-κB were recovered by the ROS scavenger N-acetyl-L-cysteine (NAC) and QGC, but not by the NADPH oxidase inhibitor diphenylene iodonium. Pretreatment of cells with the ERK inhibitor PD98059, the p38 MAPK inhibitor SB202190, NAC, and QGC attenuated nuclear translocation of NF-κB and activation of pIB. QGC has a scavenging effect on cytokine-induced ROS production, thereby preventing its downstream effects, nuclear translocation of NF-κB, and activation of pIB is mediated by activation of ERK and p38 MAPK, although QGC does not inhibit IL-1ß-stimulated COX-2 expression in feline esophageal epithelial cells. The data suggest that QGC exerts anti-oxidative effects and inhibitory effects against esophageal epithelial cells signals by the action of IL-1ß treatment.


Assuntos
Antioxidantes/farmacologia , Células Epiteliais/efeitos dos fármacos , Interleucina-1beta/metabolismo , Quercetina/análogos & derivados , Espécies Reativas de Oxigênio/metabolismo , Acetilcisteína/farmacologia , Animais , Gatos , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Ciclo-Oxigenase 2/metabolismo , Mucosa Esofágica/citologia , Flavonoides/farmacologia , Fluoresceínas/metabolismo , Quinase I-kappa B/metabolismo , Imidazóis/farmacologia , Proteínas Quinases Ativadas por Mitógeno/metabolismo , NF-kappa B/metabolismo , Fosforilação , Piridinas/farmacologia , Quercetina/farmacologia , Rumex/química , Transdução de Sinais
20.
J Sep Sci ; 39(12): 2252-62, 2016 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-27121301

RESUMO

Triterpenoid saponins are difficult to analyze using high-performance liquid chromatography coupled to UV/vis spectrophotometry due to their lack of chromophores. This study describes the first analytical method for the determination of 15 triterpenoid saponins from the leaves, stems, root bark, and fruits of Acanthopanax henryi, using a high-performance liquid chromatography with charged aerosol detection coupled with electrospray ionization mass spectrometry method. The separation was carried out on a Kinetex XB-C18 column with an acetonitrile/water gradient as the mobile phase, followed by charged aerosol detection. The operating conditions of charged aerosol detection were set at 24 kPa for nitrogen pressure and 100 pA for the detection range. Liquid chromatography with electrospray ionization mass spectrometry is described for the identification of compounds in plant samples. The electrospray ionization mass spectrometry method involved the use of the [M + Na](+) and [M + NH4 ](+) ions for compounds 1-15 in the positive ion mode with an extracted ion chromatogram. The developed method was fully validated in terms of linearity, sensitivity, precision, repeatability, and recovery, then subsequently applied to evaluate the quality of A. henryi.


Assuntos
Aerossóis/análise , Eleutherococcus/química , Saponinas/análise , Triterpenos/análise , Cromatografia Líquida , Espectrometria de Massas por Ionização por Electrospray
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