Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 168
Filtrar
1.
Phytochemistry ; 222: 114074, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38604324

RESUMO

Ustiloxins I-M (1-5), five undescribed cyclopeptides bearing a 15-membered macrocyclic skeleton, were isolated from Cordyceps militaris. The structures of 1 and 5 were identified by spectroscopic and crystallographic methods, whereas the structures of 2-4 were assigned by spectroscopic and computational approaches. Biological evaluation of all the compounds toward human triple-negative breast cancer cells revealed that compounds 4 and 5 are toxic with IC50 values of 64.29 µM and 28.89 µM, respectively.


Assuntos
Cordyceps , Peptídeos Cíclicos , Cordyceps/química , Peptídeos Cíclicos/química , Peptídeos Cíclicos/isolamento & purificação , Peptídeos Cíclicos/farmacologia , Humanos , Estrutura Molecular , Ensaios de Seleção de Medicamentos Antitumorais , Linhagem Celular Tumoral , Antineoplásicos/farmacologia , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Relação Estrutura-Atividade , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga
2.
J Nat Prod ; 87(4): 1103-1115, 2024 Apr 26.
Artigo em Inglês | MEDLINE | ID: mdl-38600744

RESUMO

Twelve new alkaloids, scolopenolines A-L (1-7, 9-11, 13, 14), along with six known analogues, were isolated from Scolopendra subspinipes mutilans, identified by analysis of spectroscopic data and quantum chemical and computational methods. Scolopenoline A (1), a unique guanidyl-containing C14 quinoline alkaloid, features a 6/6/5 ring backbone. Scolopenoline B (2) is a novel sulfonyl-containing heterodimer comprising quinoline and tyramine moieties. Scolopenoline G (7) presents a rare C12 quinoline skeleton with a 6/6/5 ring system. Alkaloids 1, 8, 10, and 15-18 display anti-inflammatory activity, while 10 and 16-18 also exhibit anti-renal-fibrosis activity. Drug affinity responsive target stability and RNA-interference assays show that Lamp2 might be a potentially important target protein of 16 for anti-renal-fibrosis activity.


Assuntos
Alcaloides , Animais Peçonhentos , Quilópodes , Animais , Alcaloides/farmacologia , Alcaloides/química , Alcaloides/isolamento & purificação , Estrutura Molecular , Artrópodes/química , Fibrose/tratamento farmacológico , Rim/efeitos dos fármacos , Quinolinas/farmacologia , Quinolinas/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Humanos
3.
Bioorg Med Chem ; 97: 117544, 2024 01 01.
Artigo em Inglês | MEDLINE | ID: mdl-38071943

RESUMO

It's urgent to discover new antibiotics along with the increasing emergence and dissemination of multidrug resistant (MDR) bacterial pathogens. In the present investigation, morusin exhibited rapid bactericidal activity against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE) by targeting the phospholipid of bacterial inner membrane, increasing membrane rigidity and disrupting bacterial homeostasis together with the membrane permeability, which caused fundamental metabolic disorders. Furthermore, morusin can also accumulate ROS, suppress H2S production, and aggravate oxidative damage in bacteria. Importantly, morusin also inhibited the spread of wounds and reduced the bacterial burden in the mouse model of skin infection caused by MRSA. It's a chance to meet the challenge of existing antibiotic resistance and avoid the development of bacterial resistance, given the multiple targets of morusin.


Assuntos
Staphylococcus aureus Resistente à Meticilina , Morus , Animais , Camundongos , Antibacterianos/farmacologia , Testes de Sensibilidade Microbiana
4.
Phytochemistry ; 217: 113926, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-37981062

RESUMO

Six previously undescribed rigidly monoterpenoid indole alkaloids, alstolactines F-K (1-6), were isolated from Alstonia scholaris. Among them, a pair of cage-like epimers, 1 and 2, featuring a rare 6/5/6/6/7 ring system, represent the first example of C5→C20-olide, while compound 3 possesses unique degraded C18 and C19. The structures of the isolates were established by multiple spectroscopic analyses, quantum computational chemistry methods, and X-ray diffraction. Furthermore, the expression levels of proteins including NLRP3, TLR4, P-p65, NF-ĸB, Notch-2, IL-18, P-p38, and p38 in LPS-induced human normal hepatocyte (LO2) cells could be significantly downregulated by compounds 1-6, which showed potent anti-inflammatory bioactivity.


Assuntos
Alstonia , Alcaloides de Triptamina e Secologanina , Humanos , Alstonia/química , Lactonas , Alcaloides de Triptamina e Secologanina/química , Indóis , Hepatócitos , Alcaloides Indólicos , Estrutura Molecular
5.
Planta Med ; 2023 Oct 19.
Artigo em Inglês | MEDLINE | ID: mdl-37857337

RESUMO

Twelve lupanes including three new compounds named alstoscholarilups A-C (1: -3: ) were isolated from the leaves of Alstonia scholaris. Their structures were elucidated by spectroscopic analysis and ECD calculation. Structurally, compound 1: with a rare A ring-seco skeleton formed lactone and degraded C-3, while 2: with a 28-nor and 3: with a 29-nor-lupane skeleton supported the phytochemical diversity and novelty of the plant. Pharmacologically, compounds 4, 7: , and 10: reduced the serum uric acid (UA) levels of mice significantly.

6.
Phys Chem Chem Phys ; 25(35): 23836-23846, 2023 Sep 13.
Artigo em Inglês | MEDLINE | ID: mdl-37641860

RESUMO

We investigate the role of heterojunctions of few-layer black phosphorus (BP) with band gap inversion in governing the quantum transport behaviors. Numerical results show that in the armchair junction, electron tunneling probability occurs under approximately normal incidence with its magnitude T > 0.5. More interestingly, when different band gaps are taken into account on two sides of this junction, the maximum transmission appears away from the center of the valley, leading to the occurrence of anomalous Klein tunneling. Such a result tends to be independent of the width and height of the potential barrier. On the other hand, in the zigzag junction, electron transmission arises in a larger range of angles, and perfect electron transmission (T = 1.0) or reflection appears under specific band gap configurations. These findings provide a new understanding for the study of Klein tunneling and anomalous Klein tunneling based on tunable band gap BP or other two-dimensional Dirac semimetals.

7.
Phytochemistry ; 214: 113817, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-37549800

RESUMO

Nine pairs of undescribed enantiomers, (±)-styraxoids A-I (1-9), were isolated from the resin of Styrax tonkinensis, and their structures were assigned by spectroscopic and computational methods. Compounds (±)-1 are a pair of degraded lignans, and the remaining compounds (±)-(2-9) are phenylpropanoid skeletons. Compounds (±)-8 and (±)-9 feature a 1,3-dioxolane moiety. The biological evaluation showed that both enantiomers of 1 could inhibit LPS-induced INOS and COX-2 in RAW264.7 cells in a dose-dependent manner.


Assuntos
Lignanas , Styrax , Styrax/química , Anti-Inflamatórios/farmacologia , Lignanas/farmacologia , Resinas Vegetais/química
8.
Nefrología (Madrid) ; 43(3): 335-343, may.-jun. 2023. tab, graf
Artigo em Inglês | IBECS | ID: ibc-220038

RESUMO

Background: The associated factors of peritoneal small solute transport was not fully understood. This research aimed to investigate the connection between dialysate inflammatory markers (e.g. macrophage migration inhibitory factor, MIF) in peritoneal dialysis (PD) effluent and peritoneal solute transport rate (PSTR) properties. Subjects and design: A total of 80 stable PD patients in the First ShaoYang Hospital were enrolled in present study. Overnight PD effluent and serum inflammatory markers including MIF, MCP-1, VEGF, IL-6, TNFα and TGFβ were detected. Pearson correlation analysis and Logistic regression was performed to determine the risk factors for the increased PSTR. Results: A trend toward increased values of MIF, MCP-1 and IL-6 in PD effluent was observed in subjects with high PSTR when compared with those with low PSTR. The Pearson correlation test showed that D/P Cr exhibited positive correlations with dialysis effluent MIF (r=0.32, p=0.01), MCP-1 (r=0.47, p=0.01), IL-6 (r=0.48, p=0.01). Conversely, no significant correlation was found between D/P Cr and TGF-β (r=0.04, p=0.70), TNF-ɑ (r=0.22, p=0.05), VEGF (r=0.02, p=0.86) and serum inflammatory markers. In the unadjusted regression analysis, dialysis effluent MIF (OR 2.41), MCP-1 (OR 1.72), IL-6 (OR 1.55) were associated with high PSTR condition. Multivariate logistic regression analysis showed that the adjusted odds ratios (OR) of dialysis effluent MIF for high PSTR were 2.47 in all subjects (p=0.03). Conclusion: Elevated MIF, MCP-1 and IL-6 levels in PD effluent were associated with increased PSTR. Elevated dialysis effluent MIF levels was an independent risk factor for high PSTR in subjects with PD treatment. (AU)


Antecedentes: Los factores asociados del transporte peritoneal de pequeños solutos no se conocen completamente. Esta investigación tuvo como objetivo investigar la conexión entre los marcadores inflamatorios del dializado (por ejemplo, el factor inhibidor de la migración de macrófagos [MIF]) en el efluente de diálisis peritoneal (DP) y las propiedades de la tasa de transporte de solutos peritoneal (PSTR). Sujetos y diseño: Se incluyó un total de 80 pacientes con DP estable en el primer Hospital de Shaoyang. Se detectaron efluentes de DP nocturnos y marcadores inflamatorios séricos, incluyendo MIF, MCP-1, VEGF, IL-6, TNF -ɑ, TGF -β. Se realizó un análisis de correlación de Pearson y regresión logística para determinar los factores de riesgo para la PSTR aumentada. Resultados: Se observó una tendencia hacia valores incrementados de MIF, MCP-1 e IL-6 en el efluente de DP en sujetos con PSTR alta, en comparación con aquellos con PSTR baja. La prueba de correlación de Pearson mostró que D/Pcr exhibe correlaciones positivas con el MIF del efluente diálisis (r = 0,32, p = 0,01), MCP-1 (r = 0,47, p = 0,01), IL-6 (r = 0,48, p = 0,01). Por el contrario, no se encontró una correlación significativa entre D/Pcr y TGF-β (r = 0,04, p = 0,70), TNF-ɑ (r = 0,22, p = 0,05), VEGF (r = 0,02, p = 0,86) y marcadores séricos de inflamación. En el análisis de regresión no ajustado, el MIF del efluente diálisis (OR 2,41), la MCP-1 (OR 1,72), la IL-6 (OR 1,55) se asociaron con una PSTR elevada. El análisis de regresión logística multivariante mostró que las odds ratios (OR) ajustadas del MIF del efluente diálisis para PSTR alta fueron de 2,47 en todos los sujetos (p = 0,03). Conclusión: Los niveles elevados de MIF, MCP-1 y IL-6 en el efluente de DP se asociaron con un aumento de la PSTR. Los niveles elevados del MIF del efluente diálisis fueron un factor de riesgo independiente para PSTR elevada en sujetos tratados con DP. (AU)


Assuntos
Humanos , Masculino , Feminino , Adulto Jovem , Adulto , Pessoa de Meia-Idade , Idoso , Diálise Peritoneal , Fatores Inibidores da Migração de Macrófagos , Proteínas Carreadoras de Solutos , Estudos Transversais , China
9.
Chem Commun (Camb) ; 59(16): 2271-2274, 2023 Feb 21.
Artigo em Inglês | MEDLINE | ID: mdl-36734477

RESUMO

Two unique windmill-like aziridine-containing indole alkaloids, possessing an unprecedented 6/5/5/6/6/5/3 rigid ring system and an unusual azabicyclo[3.1.0]hexane core, were isolated from Alstonia scholaris. Their structures were established by spectroscopy, X-ray diffraction, and electronic circular dichroism calculations. The novel compounds exhibited significant anti-inflammatory bioactivity in vitro and alleviated LPS-induced acute lung injury in mice.


Assuntos
Alstonia , Plantas Medicinais , Camundongos , Animais , Alstonia/química , Alcaloides Indólicos , Anti-Inflamatórios , Difração de Raios X , Estrutura Molecular , Folhas de Planta/química
10.
Fitoterapia ; 166: 105464, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-36848963

RESUMO

Three new steroidal alkaloids, veratrasines A - C (1-3), along with ten known analogues (4-13) were isolated from the roots of Veratrum stenophyllum. Their structures were elucidated by NMR and HRESIMS data and comparison with the reported data in the literatures. A plausible biosynthetic pathway for 1 and 2 were proposed. Compounds 1, 3, and 8 showed moderate cytotoxic activity against MHCC97H and H1299 cell lines.


Assuntos
Alcaloides , Veratrum , Veratrum/química , Estrutura Molecular , Raízes de Plantas , Esteroides , Alcaloides de Veratrum/química
11.
Chem Biodivers ; 20(3): e202201240, 2023 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-36799244

RESUMO

Jiangchuanmycin (1), a new indole containing pyrrolizidine, and six known peptides (2-7) were obtained from the fermentation broth of a Streptomyces isolate collected from a sediment sample of Xingyun Lake, Jiangchuan, China. Their structures were elucidated on the detailed analysis of the HR-ESI-MS, 1D and 2D NMR, ECD, and X-ray crystallographic data. Jiangchuanmycin (1) presented weak inhibitory effects on cell lines of H1299, MHCC97H, HCT116 with the IC50 values of 97.6 µM, 98.6 µM and 40.6 µM, respectively.


Assuntos
Antineoplásicos , Streptomyces , Streptomyces/química , Estrutura Molecular , Antineoplásicos/farmacologia , Antineoplásicos/química , Linhagem Celular Tumoral , Espectroscopia de Ressonância Magnética
12.
Nefrologia (Engl Ed) ; 43(3): 335-343, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36517360

RESUMO

BACKGROUND: The associated factors of peritoneal small solute transport was not fully understood. This research aimed to investigate the connection between dialysate inflammatory markers (e.g. macrophage migration inhibitory factor, MIF) in peritoneal dialysis (PD) effluent and peritoneal solute transport rate (PSTR) properties. SUBJECTS AND DESIGN: A total of 80 stable PD patients in the First ShaoYang Hospital were enrolled in present study. Overnight PD effluent and serum inflammatory markers including MIF, MCP-1, VEGF, IL-6, TNFα and TGFß were detected. Pearson correlation analysis and Logistic regression was performed to determine the risk factors for the increased PSTR. RESULTS: A trend toward increased values of MIF, MCP-1 and IL-6 in PD effluent was observed in subjects with high PSTR when compared with those with low PSTR. The Pearson correlation test showed that D/P Cr exhibited positive correlations with dialysis effluent MIF (r=0.32, p=0.01), MCP-1 (r=0.47, p=0.01), IL-6 (r=0.48, p=0.01). Conversely, no significant correlation was found between D/P Cr and TGF-ß (r=0.04, p=0.70), TNF-ɑ (r=0.22, p=0.05), VEGF (r=0.02, p=0.86) and serum inflammatory markers. In the unadjusted regression analysis, dialysis effluent MIF (OR 2.41), MCP-1 (OR 1.72), IL-6 (OR 1.55) were associated with high PSTR condition. Multivariate logistic regression analysis showed that the adjusted odds ratios (OR) of dialysis effluent MIF for high PSTR were 2.47 in all subjects (p=0.03). CONCLUSION: Elevated MIF, MCP-1 and IL-6 levels in PD effluent were associated with increased PSTR. Elevated dialysis effluent MIF levels was an independent risk factor for high PSTR in subjects with PD treatment.

13.
Chem Commun (Camb) ; 59(3): 326-329, 2023 Jan 03.
Artigo em Inglês | MEDLINE | ID: mdl-36511292

RESUMO

Veratrazine A (1), a steroidal alkaloid with a unique 6/5/5 triheterocyclic scaffold as the side chain, was isolated from Veratrum stenophyllum, and its structure was established via spectroscopic analyses and X-ray diffraction. A plausible biosynthetic pathway for 1 is proposed. Bioassy exhibits moderate anti-inflammatory activities in vitro and in vivo.


Assuntos
Alcaloides , Antineoplásicos , Veratrum , Alcaloides/farmacologia , Alcaloides/química , Extratos Vegetais/química , Veratrum/química , Esteroides/farmacologia , Anti-Inflamatórios , Estrutura Molecular
14.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-1009169

RESUMO

OBJECTIVE@#To investigate the correlation between the medial meniscal indentation index (MDI) and medial tibiofemoral articular cartilage damage more than 3 degrees in patients aged 40 to 60 years old with suspected or complicated knee osteoarthritis at non-weight-bearing position, and to determine the predictive threshold.@*METHODS@#From June 2016 to June 2020, a total of 308 patients who underwent initial knee arthroscopic exploration for chronic knee pain were collected. The age ranged from 36 to 71 years old with an average of(56.40±1.82) years old, including 105 males and 203 females. And patients with extra-articular malformations (abnormal force lines), a history of trauma, inflammatory arthritis and other specific arthritis were excluded. Finally, 89 eligible cases were obtained, aged from 42 to 60 years old with an average of (59.50±0.71) years old, including 45 males and 44 females. The degree of cartilage damage in the medial compartment of the knee joint was recorded, which was divided into two groups(≥degree 3 and<degree 3) according to Outer-Bridge classification system. The possible risk factors were determined by univariate analysis in the age, gender, affected sides, body mass index (BMI), synovial thickening grade, meniscus injury and MDI of 2 groups. Then, the independent risk factors for cartilage injury of more than grade 3 were determined by further binary Logistic regression analysis. If MDI was taken as an independent risk factor, receiver operating characteristic (ROC) analysis was performed to confirm whether it had diagnostic value for cartilage damage of above degree 3 and calculate the critical value of MDI.@*RESULTS@#A total of 89 eligible patients were obtained. Univariate analysis showed age, BMI, MDI and meniscus injury may be the independent risk factors for cartilage damage of more than 3 degrees, further binary Logistic regression analysis confirmed that MDI[OR=1.66, 95%CI(1.64, 1.69), P=0.01]and BMI [OR=1.58, 95%CI(1.17, 2.15), P=0.03] were independent risk factors for cartilage injury of more than degree 3 in enrolled patients. ROC analysis showed that MDI had more diagnostic value than BMI, and the critical value was 0.355 with a sensitivity of 89.1% and a specificity of 88.2%.@*CONCLUSION@#In doubt or accompanied by 40 to 60 years old patients with knee osteoarthritis, the MDI measured by non-weight-bearing knee MRI has predictive value for cartilage injury of more than degree 3 in medial tibiofemoral joint, and the critical value for diagnosis of cartilage injury of more than degree 3 is 0.355.


Assuntos
Masculino , Feminino , Humanos , Adulto , Pessoa de Meia-Idade , Idoso , Osteoartrite do Joelho/cirurgia , Cartilagem Articular/cirurgia , Articulação do Joelho/cirurgia , Menisco , Meniscos Tibiais/cirurgia , Doenças das Cartilagens , Imageamento por Ressonância Magnética/efeitos adversos
15.
Tissue Cell ; 79: 101944, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36179454

RESUMO

Macrophages have been reported to play important roles in tissue repair and regeneration. While it is known that macrophages are present in the dental pulp, their role in dental pulp regeneration is not fully understood. In the present study, we investigated the effects of different phenotype macrophages conditioned medium on the cellular behaviors of hDPSCs and their extracellular matrix (cell sheets) in vitro. Moreover, twenty-four root fragments inserted with cell sheets cultured with different conditioned media were placed into the back subcutaneous space of 6-8-week-old male BALB/c nude mouse. The regenerated tissues in the root fragments were assessed via histologic analysis after 8 weeks of transplantation. M2 macrophages could promote the proliferation, migration, and osteogenic differentiation of hDPSCs. Dental pulp-like tissue with an odontoblast-like layer lining the dentinal surface and well-arranged collagen fibers was harvested in root fragment combined with M2 conditioned medium cultured cell sheet, whereas a large amount of calcium salt deposition and disorganization of collagen fibers were observed in root fragments combined with M1 conditioned medium cultured cell sheet. Therefore, promoting the transformation of M1 into M2 macrophage in dental pulp tissue regeneration may be a potential way for dental pulp regeneration via functional healing.


Assuntos
Osteogênese , Células-Tronco , Camundongos , Animais , Masculino , Meios de Cultivo Condicionados/farmacologia , Meios de Cultivo Condicionados/metabolismo , Polpa Dentária , Regeneração , Diferenciação Celular , Macrófagos , Colágeno/metabolismo , Células Cultivadas
16.
Nat Prod Bioprospect ; 12(1): 23, 2022 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-35701630

RESUMO

Steroidal alkaloids possess the basic steroidal skeleton with a nitrogen atom in rings or side chains incorporated as an integral part of the molecule. They have demonstrated a wide range of biological activities, and some of them have even been developed as therapeutic drugs, such as abiraterone acetate (Zytiga®), a blockbuster drug, which has been used for the treatment of prostate cancer. Structurally diverse natural steroidal alkaloids present a wide spectrum of biological activities, which are attractive for natural product chemistry and medicinal chemistry communities. This review comprehensively covers the structural classification, isolation and various biological activities of 697 natural steroidal alkaloids discovered from 1926 to October 2021, with 363 references being cited.

17.
Chem Biodivers ; 19(5): e202200064, 2022 May.
Artigo em Inglês | MEDLINE | ID: mdl-35333437

RESUMO

Actinomycetes have being regarded as a treasure reservoir of various bioactive secondary metabolites and devoted many antibiotics in clinicals. Amycolatopsis sp. YNNP 00208 was isolated from a soil sample collected in Gaoligong Mountain area, Yunnan Province, China. Chemical investigation of its fermentation broth led to a new amide, baoshanmycin (1), and a new furanone derivative, 3-(1,3-dihydroxybutyl)-4-methylfuran-2(H)-one (2), together with eight known compounds, including two amides (3-4), four cyclic dipeptides (5-8), and two deoxyribonucleosides (9-10). Their structures were established on basis of the 1D- and 2D-NMR spectroscopic data, along with the HR-ESI-MS experiments. Baoshanmycin (1) showed moderate antimicrobial activities against Candida albicans, and weak activities against Staphylococcus aureus, multi-drug resistant Staphylococcus aureus, Bacillus subtilis, Listeria monocytogenes, fluconazole-resistant Candida albicans. Baoshanmycin (1) presented strong antioxidant activity and moderate anti-acetylcholinesterase activity. The other compound 3-(1,3-dihydroxybutyl)-4-methylfuran-2(H)-one (2) and the known compounds (3-10) showed moderate antioxidant activity.


Assuntos
Actinobacteria , Staphylococcus aureus Resistente à Meticilina , Actinobacteria/metabolismo , Amycolatopsis , Antibacterianos/química , Antioxidantes/metabolismo , China , Staphylococcus aureus Resistente à Meticilina/metabolismo , Testes de Sensibilidade Microbiana , Solo
18.
J Ethnopharmacol ; 290: 115049, 2022 May 23.
Artigo em Inglês | MEDLINE | ID: mdl-35150817

RESUMO

ETHNOPHARMACOLOGY RELEVANCE: One folk use of Alstonia scholaris (L.) R. Br. in "Dai" ethno-medicine system is to treat gouty arthritis, which might be caused by hyperuricemia, but anti-hyperuricemic investigation of A. scholaris were rarely reported. AIM OF THE STUDY: To verify anti-hyperuricemic property of A. scholaris, and explore its bioactive compounds in vivo and in vitro. MATERIALS AND METHODS: The anti-hyperuricemic bioactivity of the non-alkaloids fraction and compounds were evaluated with potassium oxonate (PO) induced hyperuricemia mice model in vivo, and monosodium urate (MSU) induced human renal tubular epithelial cells (HK-2) was selected to test in vitro, respectively, with benzobromarone as the positive control. 11 triterpenoids were isolated by phytochemical methods and their structures were elucidated by spectroscopic analysis and ECD calculation. RESULTS: The non-alkaloids fraction of A. scholaris decreased the serum uric acid (UA) level in mice model significantly at the doses of 100 mg/kg and 200 mg/kg, and then nine ursane- and two oleanane-triterpenoids including four new compounds (1-3 and 10) were isolated from the bioactive fraction, in which compounds 1, 4, 5, 6 and 10 exhibited better anti-hyperuricemic tendency in vitro by promoting the excretion of UA in MSU-induced HK-2 cell model at a concentration of 5 µM. Furthermore, compounds 1 and 4 were proved to reduce the serum UA level in mice significantly at 5 mg/kg in vivo. CONCLUSIONS: The results supported the traditional use of A. scholaris in treating gouty arthritis, and also provided new bioactive triterpenoids for further chemical and pharmacological investigation.


Assuntos
Alstonia/química , Hiperuricemia/patologia , Extratos Vegetais/farmacologia , Ácido Úrico/sangue , Animais , Linhagem Celular , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Humanos , Hiperuricemia/induzido quimicamente , Masculino , Camundongos , Camundongos Endogâmicos ICR , Ácido Oxônico/farmacologia
19.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-940528

RESUMO

ObjectiveTo establish an integrated method of fingerprint qualitative, multi-component quantitative analysis and chemometrics, and to evaluate the quality attributes and differences of Aurantii Fructus from different production areas and origins. MethodAnalysis was performed on COSMOSIL 5C18-MS-Ⅱ column (4.6 mm×250 mm, 5 μm) with the mobile phase of acetonitrile-0.2% phosphoric acid solution for gradient elution (0-4 min, 19%A; 4-5 min, 19%-21%A; 5-18 min, 21%A; 18-19 min, 21%-28%A; 19-27 min, 28%A; 27-28 min, 28%-40%A; 28-36 min, 40%A; 36-37 min, 40%-50%A; 37-42 min, 50%-60%A; 42-46 min, 60%-95%A; 46-55 min, 95%-100%A), the flow rate was 1 mL·min-1, the column temperature was 30 ℃, the detection wavelength was set at 320 nm, and the injection volume was 10 μL. High performance liquid chromatography (HPLC) fingerprints of Aurantii Fructus from different production areas and origins were established. Then, the quality of 26 batches of samples was evaluated by cluster analysis (CA), principal component analysis (PCA) and orthogonal partial least squares discriminant analysis (OPLS-DA). A method for the determination of 12 components was developed and verified, and a thermal map-based CA of Aurantii Fructus from different production areas and origins was carried out based on the content difference of samples. ResultThe fingerprint and determination methods were well verified. The similarity of HPLC fingerprint of 12 batches of Aurantii Fructus was 0.85-0.996, 20 common peaks were calibrated and 14 of them were assigned. The resolution and linear relationship of 12 components in quantitative analysis were good. The recovery rates were 99.2%-101.0% with RSD≤2.0%. The results of CA, PCA and OPLS-DA indicated that the differentiation of Aurantii Fructus in different production areas was great, and there were differences among different cultivars. ConclusionThe qualitative analysis of fingerprint and quantitative analysis of multiple indexes based on the same chromatographic analysis conditions are convenient, accurate and reliable, and combined with chemometrics, the identification and quality analysis of Aurantii Fructus from different production areas and origins can be realized, which can provide reference for quality control and evaluation of Aurantii Fructus.

20.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-935830

RESUMO

Objective: To investigate the effect of exosomes from mild-inflammation- stimulated human dental pulp stem cells (hDPSC) combined with stromal cell-derived factor-1 (SDF-1) on dental pulp regeneration in rats. Methods: Primary hDPSCs were isolated, cultured and then stimulated by using lipopolysaccharide (LPS). The exosomes from the hDPSCs with (L-EXO) or without (N-EXO) LPS were extracted by overspeed differential centrifugation and were identified by transmission electron microscopy and Western blotting. Forty SD rats, aged 6-8 weeks, were equally divided into S group (SDF-1 alone), L+S group (L-EXO combined with SDF-1), N+S group (N-EXO combined with SDF-1) and blank control group (no substance implanted into the root canal) by random number table method. Bilateral mandibular first molars were used as the experimental teeth to establish pulpless root canal models and different contents were implanted into the root canals according to the groups. All rats were over-anesthetized and sacrificed at the 30th day after content implantation. Bilateral mandibular tissues were taken for histological evaluation by means of HE, Masson and immunohistochemical stainings. Results: The HE staining showed new pulp-like tissue in the root canals of all three experimental groups. The amount of new tissues and the number of cells in the tissues were greatest in L+S group and least in S group. Masson staining showed that the mineralized tissue in L+S group was arranged longitudinally along the root canal wall and the collagen fibers were arranged in an orderly fashion, while those in N+S group showed an irregular and disordered distribution. Quantitative analysis of the area of neovascularization in each group showed that the density of vessels in the L+S group [(2.03±0.65)%] was significantly higher than that in the S group [(0.65±0.05)%] and the N+S group [(1.06±0.38)%] respectively (F=5.879, P<0.05). Immunohistochemical staining showed that the expression of CXC chemokine receptor 4 (CXCR4) was significantly lower in S and L+S groups than in N+S group, with a statistically significant difference (F=8.633, P<0.01). Conclusions: Exosomes secreted by hDPSCs combined with SDF-1 might increase the amount of new tissue in the root canal and the density of blood vessels in the tissue. L-EXO showed a stronger effect than N-EXO did. The combination of L-EXO with SDF-1 might result in more regular arrangement of mineralized tissue and collagen fibers in the regenerative tissues.


Assuntos
Animais , Humanos , Ratos , Diferenciação Celular , Polpa Dentária , Exossomos , Lipopolissacarídeos , Ratos Sprague-Dawley , Regeneração , Células-Tronco , Células Estromais
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA