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1.
Zhongguo Gu Shang ; 37(3): 242-50, 2024 Mar 25.
Artículo en Chino | MEDLINE | ID: mdl-38515410

RESUMEN

Osteoporotic fractures represent the most severe complications of osteoporosis,characterized by insidious onset,high mortality and disability rates,and a steadily increasing incidence,imposing a significant socioeconomic burden. Western medicine has advantages in diagnosis and surgical interventions,while traditional Chinese medicine excels in holistic management and the restoration of bodily equilibrium. The integration of both traditional Chinese medicine (TCM) and western medicine emerges as an effective therapeutic strategy for osteoporotic fractures. In order to propagate the concept of integrated diagnosis and treatment,foster the advancement of integrated medical techniques for osteoporotic fractures,and establish standardized and normative protocols for disease prevention,diagnosis,and treatment,a consensus expert group,led by Geriatric Branch of Chinese Geriatrics Society,the Young Osteoporosis Group of Orthopedics Branch of Chinese Medical Association,Osteoporosis Group of Orthopedics Branch of Chinese Physician Association,and Osteoporosis Professional Committee of the Shanghai Society of Integrated Traditional Chinese and Western Medicine,was established. This group engaged in deliberations and formulated the "Expert Consensus on Integrated Traditional Chinese and Western Medicine Diagnosis and Treatment of Osteoporotic Fractures" elucidating the concept of integrated medicine and offering recommendations in the domains of prevention,diagnosis,and treatment,with the aspiration of ameliorating the prognosis of osteoporotic fractures and enhancing the quality of life for these patients.


Asunto(s)
Osteoporosis , Fracturas Osteoporóticas , Humanos , Anciano , Fracturas Osteoporóticas/diagnóstico , Fracturas Osteoporóticas/terapia , Consenso , Calidad de Vida , China , Medicina Tradicional China , Osteoporosis/diagnóstico , Osteoporosis/terapia
2.
Fitoterapia ; 175: 105917, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38508501

RESUMEN

The aim of this work is to explore the effects of herbal medicine on secondary metabolites of microorganisms during fermentation. Clonostachys rogersoniana was found to metabolize only small amounts of polyketide glycosides rogerson B and C on fresh potatoes, but after replacing the medium to the medicinal plant Rubus delavayi Franch., the type and content of the metabolized polyketones showed significant changes. The sugars and glycosides in R. delavayi are probably responsible for the changes in secondary metabolites. Six polyketide glycosides including a new metabolite, rogerson F, and two potential antitumor compounds, TMC-151C and TMC-151D, were isolated from the extract of R. delavayi fermented by C. rogersoniana. In addition, 13C labeling experiments were used to trace the biosynthesis process of these compounds. TMC-151C and TMC-151D showed significant cytotoxic activity against PANC-1, K562 and HCT116 cancer cells but had no obvious cytotoxic activity against BEAS-2B human normal lung epithelial cells. The yields of TMC-151C and TMC-151D reached 14.37 ± 1.52 g/kg and 1.98 ± 0.43 g/kg, respectively, after fermentation at 28 °C for 30 days. This is the first study to confirm that herbal medicine can induce microbes to metabolize active compounds. And the technology of fermenting medicinal materials can bring more economic value to medicinal plants.


Asunto(s)
Fermentación , Hypocreales , Policétidos , Policétidos/metabolismo , Policétidos/farmacología , Humanos , Línea Celular Tumoral , Hypocreales/metabolismo , Antineoplásicos Fitogénicos/farmacología , Estructura Molecular , Glicósidos/farmacología , Glicósidos/aislamiento & purificación , Plantas Medicinales/química , Metabolismo Secundario , China
3.
Phytochemistry ; 216: 113871, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37777165

RESUMEN

Five undescribed eudesmane sesquiterpenoids, artemilavanins A-E, and one undescribed rearranged eudesmane sesquiterpenoid, artemilavanin F, were isolated from the 95% ethanol extract of the aerial parts of Artemisia lavandulaefolia DC., along with ten known compounds. The structures and configurations of undescribed compounds were mainly elucidated by spectroscopic analyses and single-crystal X-ray diffraction analysis. Among all isolated compounds, artemilavanin F exhibited inhibitory activity on PANC-1 pancreatic cancer cells with IC50 of 9.69 ± 2.39 µM. Artemilavanin F inhibited PANC-1 cell proliferation by induction of G2/M cell cycle arrest and apoptosis mediated by downregulation of cyclin-dependent kinases and accumulation of reactive oxygen species. Moreover, artemilavanin F inhibited the colony formation, cell migration and sphere formation of PANC-1 cells, indicating the suppression of stem-cell-like phenotype of PANC-1 cells. Further results confirmed that the expression of cancer stem cell markers such as Bmi1, CD44, CD133 were inhibited by artemilavanin F. Downregulation of epithelial-mesenchymal transition (EMT) markers such as N-cadherin and Oct-4 indicated the potential of artemilavanin F in prevention of metastasis.


Asunto(s)
Artemisia , Neoplasias Pancreáticas , Sesquiterpenos de Eudesmano , Sesquiterpenos , Artemisia/química , Neoplasias Pancreáticas/tratamiento farmacológico , Sesquiterpenos de Eudesmano/farmacología , Sesquiterpenos de Eudesmano/análisis , Sesquiterpenos de Eudesmano/química , Componentes Aéreos de las Plantas/química , Sesquiterpenos/química , Estructura Molecular , Neoplasias Pancreáticas
4.
J Virol ; 97(9): e0079023, 2023 09 28.
Artículo en Inglés | MEDLINE | ID: mdl-37607058

RESUMEN

Bats carry genetically diverse severe acute respiratory syndrome-related coronaviruses (SARSr-CoVs). Some of them utilize human angiotensin-converting enzyme 2 (hACE2) as a receptor and cannot efficiently replicate in wild-type mice. Our previous study demonstrated that the bat SARSr-CoV rRsSHC014S induces respiratory infection and lung damage in hACE2 transgenic mice but not wild-type mice. In this study, we generated a mouse-adapted strain of rRsSHC014S, which we named SMA1901, by serial passaging of wild-type virus in BALB/c mice. SMA1901 showed increased infectivity in mouse lungs and induced interstitial lung pneumonia in both young and aged mice after intranasal inoculation. Genome sequencing revealed mutations in not only the spike protein but the whole genome, which may be responsible for the enhanced pathogenicity of SMA1901 in wild-type BALB/c mice. SMA1901 induced age-related mortality similar to that observed in SARS and COVID-19. Drug testing using antibodies and antiviral molecules indicated that this mouse-adapted virus strain can be used to test prophylactic and therapeutic drug candidates against SARSr-CoVs. IMPORTANCE The genetic diversity of SARSr-CoVs in wildlife and their potential risk of cross-species infection highlights the importance of developing a powerful animal model to evaluate the antibodies and antiviral drugs. We acquired the mouse-adapted strain of a bat-origin coronavirus named SMA1901 by natural serial passaging of rRsSHC014S in BALB/c mice. The SMA1901 infection caused interstitial pneumonia and inflammatory immune responses in both young and aged BALB/c mice after intranasal inoculation. Our model exhibited age-related mortality similar to SARS and COVID-19. Therefore, our model will be of high value for investigating the pathogenesis of bat SARSr-CoVs and could serve as a prospective test platform for prophylactic and therapeutic candidates.


Asunto(s)
Quirópteros , Ratones , Coronavirus Relacionado al Síndrome Respiratorio Agudo Severo , Animales , Ratones/virología , Quirópteros/virología , Coronavirus Relacionado al Síndrome Respiratorio Agudo Severo/clasificación , Coronavirus Relacionado al Síndrome Respiratorio Agudo Severo/efectos de los fármacos , Coronavirus Relacionado al Síndrome Respiratorio Agudo Severo/genética , Coronavirus Relacionado al Síndrome Respiratorio Agudo Severo/patogenicidad , Ratones Endogámicos BALB C , COVID-19/mortalidad , Síndrome Respiratorio Agudo Grave/tratamiento farmacológico , Síndrome Respiratorio Agudo Grave/mortalidad , Pase Seriado , Antivirales/farmacología , Antivirales/uso terapéutico , Anticuerpos Antivirales/farmacología , Anticuerpos Antivirales/uso terapéutico , Zoonosis Virales/tratamiento farmacológico , Zoonosis Virales/transmisión , Zoonosis Virales/virología , Enfermedades Pulmonares Intersticiales/tratamiento farmacológico , Enfermedades Pulmonares Intersticiales/virología , Envejecimiento , Evaluación Preclínica de Medicamentos
5.
Zhen Ci Yan Jiu ; 48(6): 592-9, 2023 Jun 25.
Artículo en Chino | MEDLINE | ID: mdl-37385791

RESUMEN

OBJECTIVE: To observe the effect of acupuncture at "Houxi"(SI3) and "Huantiao"(GB30) on high mobility group box 1(HMGB1) protein and mRNA in spinal nerve trunk(SNT) of rats with lumbar disc herniation(LDH), so as to explore the mechanisms of acupuncture at this paired points on the treatment for LDH. METHODS: SD rats were randomly divided into sham operation, model, conventional acupuncture(CA) and paired points(PP) groups (with 8 rats in each group). The LDH model was established by injection of autologous suspension made from rats' own nucleus pulsus into the epidural space. Rats in the CA group received acupuncture treatment at bilateral "Weizhong"(BL40), "Dachangshu"(BL25) and "Shenshu"(BL23), while rats in the PP group received acupuncture at bilateral SI3 and GB30, 30 min each time, once daily for 14 consecutive days. The thermal pain threshold of bilateral hind feet of rats was detected by thermal pain stimulator. The contents of serum IL-1ß, IL-6 and IL-8 of rats were detected by ELISA. Western blot and immunofluorescence were used to detect the expression of HMGB1 protein in the lumbar(L)5 SNT of rats. The relative expression of HMGB1 mRNA in L5 SNT was determined by qPCR. HE staining was used to observe the morphological changes of L5 SNT. RESULTS: Compared with the sham operation group, the thermal pain threshold of bilateral hind feet in the model group was decreased (P<0.05); compared with the model group, the thermal pain threshold of bilateral hind feet in the CA group and the PP group were increased (P<0.05). The expressions of HMGB1 protein and mRNA in L5 SNT, and the contents of serum IL-1ß, IL-6 and IL-8 of rats in the model group were significantly increased(P<0.000 1, P<0.001) in contrast to the sham operation group. The expressions of HMGB1 protein and mRNA in L5 SNT, and the levels of serum IL-1ß, IL-6 and IL-8 were significantly decreased (P<0.01, P<0.000 1, P<0.001, P<0.05) in the CA and PP group, in comparison with those of the model group. Compared with the CA group, the above indexes of rats in the PP group recovered more significantly (P<0.05,P<0.001, P<0.01,P<0.000 1). The histomorphological results showed scattered and various-sized nerve fibers, vacuolation, a large number of disintegrating myelin sheath and lysed Schwann cells in the model group. Myelin sheaths regeneration, regularly-arranged nerve fibers were seen in the CA group and the PP group, with more obvious histopathological recovery observed in the PP group than the CA group. CONCLUSION: Acupuncture intervention inhibites the expressions of HMGB1 protein and mRNA in rats with LDH, and further reduces the production of IL-1ß, IL-6 and IL-8, which is beneficial to inflammatory response inhibition and pain alleviation. The therapeutic effect of the PP group is more obvious than that of the CA group.


Asunto(s)
Terapia por Acupuntura , Proteína HMGB1 , Desplazamiento del Disco Intervertebral , Animales , Ratas , Ratas Sprague-Dawley , Proteína HMGB1/genética , Desplazamiento del Disco Intervertebral/genética , Desplazamiento del Disco Intervertebral/terapia , Interleucina-6/genética , Interleucina-8 , Dolor , Nervios Espinales
6.
Mol Biol Rep ; 50(3): 2883-2892, 2023 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-36538170

RESUMEN

Tea, which is mainly produced using the young leaves and buds of tea plants (Camellia sinensis (L.) O. Kuntze), is one of the most common non-alcoholic beverages consumed in the world. The standard of tea mostly depends on the variety and quality of tea plants, which generally grow in subtropical areas, where the warm and humid conditions are also conducive to the occurrence of diseases. In fighting against pathogens, plants rely on their sophisticated innate immune systems which has been extensively studied in model plants. Many components involved in pathogen associated molecular patterns (PAMPs) triggered immunity (PTI) and effector triggered immunity (ETI) have been found. Nevertheless, the molecular regulating network against pathogens (e.g., Pseudopestalotiopsis sp., Colletotrichum sp. and Exobasidium vexans) causing widespread disease (such as grey blight disease, anthracnose, and blister blight) in tea plants is still unclear. With the recent release of the genome data of tea plants, numerous genes involved in tea plant immunity have been identified, and the molecular mechanisms behind tea plant immunity is being studied. Therefore, the recent achievements in identifying and cloning functional genes/gene families, in finding crucial components of tea immunity signaling pathways, and in understanding the role of secondary metabolites have been summarized and the opportunities and challenges in the future studies of tea immunity are highlighted in this review.


Asunto(s)
Camellia sinensis , Camellia sinensis/genética , Camellia sinensis/metabolismo , Inmunidad de la Planta/genética , Hojas de la Planta/genética , Hojas de la Planta/metabolismo , Té/metabolismo , Regulación de la Expresión Génica de las Plantas
7.
Zhongguo Zhong Yao Za Zhi ; 47(21): 5855-5862, 2022 Nov.
Artículo en Chino | MEDLINE | ID: mdl-36472004

RESUMEN

To comprehensively evaluate the quality of commercial Ginseng Radix et Rhizoma Rubra, 43 batches of commercial Ginseng Radix et Rhizoma Rubra were collected to determine the content of nine ginsenosides Rg_1, Re, Rb_1, Rk_3, Rh_4, 20(S)-Rg_3, 20(R)-Rg_3, Rk_1, and Rg_5 by high performance liquid chromatography(HPLC). The quality of the commercial Ginseng Radix et Rhizoma Rubra was evaluated by correlation analysis, principal component analysis, factor analysis, analysis of variance(ANOVA), and cluster heatmap analysis. The content determination indicated that the content of common ginsenosides in commercial Ginseng Radix et Rhizoma Rubra were higher while that of rare ginsenosides were lower. Multivariate statistical analysis revealed that ginsenosides Rg_1 and Rb_1 were significantly positively correlated with rare ginsenosides, and Rg_1, Rb_1 and rare ginsenosides played an important role in evaluating the quality of commercial Ginseng Radix et Rhizoma Rubra. In combination with the processing principle and current quality situation of Ginseng Radix et Rhizoma Rubra, it is recommended to improve the content limit of Rb_1 in the existing quality standards.


Asunto(s)
Medicamentos Herbarios Chinos , Ginsenósidos , Panax , Ginsenósidos/análisis , Rizoma/química , Raíces de Plantas/química , Cromatografía Líquida de Alta Presión
8.
Expert Opin Investig Drugs ; 31(11): 1151-1167, 2022 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-36437752

RESUMEN

INTRODUCTION: Since the approval of sorafenib for systemic treatment of advanced hepatocellular carcinoma (HCC), many tyrosine kinase inhibitors (TKIs) and immune checkpoint inhibitors (ICIs) have shown efficacy and tolerability as first-line treatments. On the other hand, these first-line therapies are associated with low objective response and drug resistance. Many drugs have been successfully tested for second-line treatment of advanced HCC. While the rapid proliferation of second-line treatments for advanced HCC brings hope to patients, it also complicates clinical decision-making. AREAS COVERED: This review aims to facilitate decisions by summarizing the latest guidelines for second-line treatment of HCC in various countries or regions. We then review existing second-line treatment options and discuss challenges that should be addressed in the future. A literature search was conducted in April 2022 of PubMed/Medline, Cochrane library, and abstracts of international cancer meetings. EXPERT OPINION: There is no standard second-line treatment, especially for the case of sequential treatment after atezolizumab plus bevacizumab (atezo+bev) and further studies focused on sequential treatment are warranted in this setting. The design of clinical trials, different etiologies, and complications or quality of life (QoL) are interesting issues in the second-line setting.


Asunto(s)
Carcinoma Hepatocelular , Neoplasias Hepáticas , Humanos , Carcinoma Hepatocelular/tratamiento farmacológico , Calidad de Vida , Neoplasias Hepáticas/tratamiento farmacológico , Sorafenib , Administración Cutánea
9.
Dalton Trans ; 51(23): 8938-8944, 2022 Jun 13.
Artículo en Inglés | MEDLINE | ID: mdl-35642650

RESUMEN

Cancer is still one of the most life-threatening diseases in the world. Among the various cancer therapeutic strategies, photothermal therapy (PTT) has attracted considerable attention due to its high treatment efficacy, low invasive burden, and minor side effects. Microporous metal-organic frameworks (MOFs) are potential materials for photothermal tumor treatment thanks to their high surface areas, suitable pore geometry, and easy functionalization. Through designating organic linkers, encapsulating PTT agents and fabricating MOF hybrids, MOF-based treatment platforms have great potential in PTT. In this review, we mainly summarize the recent advances of MOFs in photothermal combined cancer therapy. The present challenges and possible future prospects in this field are also explored.


Asunto(s)
Estructuras Metalorgánicas , Neoplasias , Humanos , Estructuras Metalorgánicas/uso terapéutico , Neoplasias/tratamiento farmacológico , Fototerapia , Terapia Fototérmica , Porosidad
10.
Acta Pharmacol Sin ; 43(5): 1299-1310, 2022 May.
Artículo en Inglés | MEDLINE | ID: mdl-34381182

RESUMEN

Osteoarthritis (OA) is the most common arthritis with a rapidly increasing prevalence. Disease progression is irreversible, and there is no curative therapy available. During OA onset, abnormal mechanical loading leads to excessive osteoclastogenesis and bone resorption in subchondral bone, causing a rapid subchondral bone turnover, cyst formation, sclerosis, and finally, articular cartilage degeneration. Moreover, osteoclast-mediated angiogenesis and sensory innervation in subchondral bone result in abnormal vascularization and OA pain. The traditional Chinese medicine Panax notoginseng (PN; Sanqi) has long been used in treatment of bone diseases including osteoporosis, bone fracture, and OA. In this study we established two-dimensional/bone marrow mononuclear cell/cell membrane chromatography/time of flight mass spectrometry (2D/BMMC/CMC/TOFMS) technique and discovered that diterbutyl phthalate (DP) was the active constituent in PN inhibiting osteoclastogenesis. Then we explored the therapeutic effect of DP in an OA mouse model with anterior cruciate ligament transaction (ACLT). After ACLT was conducted, the mice received DP (5 mg·kg-1·d-1, ip) for 8 weeks. Whole knee joint tissues of the right limb were harvested at weeks 2, 4, and 8 for analysis. We showed that DP administration impeded overactivated osteoclastogenesis in subchondral bone and ameliorated articular cartilage deterioration. DP administration blunted aberrant H-type vessel formation in subchondral bone marrow and alleviated OA pain assessed in Von Frey test and thermal plantar test. In RANKL-induced RAW264.7 cells in vitro, DP (20 µM) retarded osteoclastogenesis by suppressing osteoclast fusion through inhibition of the ERK/c-fos/NFATc1 pathway. DP treatment also downregulated the expression of dendritic cell-specific transmembrane protein (DC-STAMP) and d2 isoform of the vacuolar (H+) ATPase V0 domain (Atp6v0d2) in the cells. In conclusion, we demonstrate that DP prevents OA progression by inhibiting abnormal osteoclastogenesis and associated angiogenesis and neurogenesis in subchondral bone.


Asunto(s)
Osteoartritis , Osteoclastos , Animales , Ligamento Cruzado Anterior/metabolismo , Ratones , Factores de Transcripción NFATC/metabolismo , Osteoartritis/tratamiento farmacológico , Osteoartritis/etiología , Osteoartritis/metabolismo , Osteoclastos/metabolismo , Dolor/metabolismo , Ácidos Ftálicos
11.
Fitoterapia ; 152: 104875, 2021 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-33675886

RESUMEN

One new limonoid, named 19-hydroxy methyl isoobacunoate diosphenol (1); one new degraded limonoid, named 9α-methoxyl dictamdiol (9); two new quinolone alkaloids, 1-methyl-3-[(7E,9E,12Z)-7,9,12-pentadecadienyl]-4(1H)-quinolone (11) and 1-methyl-3-[(7E,9E,11E)-7,9,11-pentadecadienyl]-4(1H)-quinolone (12), along with eight known compounds, evodol (2), 7ß-acetoxy-5-epilimonin (3), rutaevine (4), 6ß-acetoxy-5-epilimonin (5), limonin (6), obacunone (7), clauemargine L (8), hiiranlactone E (10) were isolated from the fruits of Evodia rutaecarpa (Juss.) Benth.. Structures of the four new compounds were elucidated on the basis of extensive spectroscopic techniques, including 1D and 2D NMR techniques. Compounds 3, 5, 9, 11 and 12 showed obviously cytotoxic activity against six human tumor lines, while compounds 11, 12 displayed anti-platelet aggregation induced by ADP at 50 µM and 100 µM.


Asunto(s)
Alcaloides/farmacología , Antineoplásicos Fitogénicos/farmacología , Evodia/química , Limoninas/farmacología , Quinolonas/farmacología , Alcaloides/aislamiento & purificación , Antineoplásicos Fitogénicos/aislamiento & purificación , Plaquetas/efectos de los fármacos , Línea Celular Tumoral , China , Frutas/química , Humanos , Limoninas/aislamiento & purificación , Estructura Molecular , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Agregación Plaquetaria/efectos de los fármacos , Quinolonas/aislamiento & purificación
12.
Zhongguo Zhen Jiu ; 39(11): 1177-80, 2019 Nov 12.
Artículo en Chino | MEDLINE | ID: mdl-31724353

RESUMEN

OBJECTIVE: To observe the clinical efficacy of SU Jia-fu's Wenjing Tongdu external treatment combined with long-snake moxibustion at the governor vessel for neurogenic bladder after spinal cord injury. METHODS: A total of 64 patients with neurogenic bladder after spinal cord injury were randomly divided into an observation group and a control group, 32 cases in each group. The patients in the control group were treated with routine acupuncture and rehabilitation of bladder function; based on the treatment in the control group, the patients in the observation group were treated with SU Jia-fu's Wenjing Tongdu external treatment combined with long-snake moxibustion at the governor vessel, twice a week for 8 weeks. Urodynamic test, including residual urine volume (RUV), maximum flow rate of urination (Qmax), bladder pressure at filling phase (Pves), maximum detrusor pressure (Pdet-max) and maximum urinary bladder volume (VMCC), was performed before and after 8-week treatment. RESULTS: The urodynamic indexes in the two groups were improved compared with before treatment (P<0.01, P<0.05); after treatment, VMCC in the observation group was significantly higher than the control group (P<0.01), while RUV and Pves in the observation group were significantly lower than the control group (P<0.05). After treatment, there was no significant difference in Qmax and Pdet-max between the two groups (P>0.05). CONCLUSION: Based on routine acupuncture and rehabilitation of bladder function, SU Jia-fu's Wenjing Tongdu external treatment combined with long-snake moxibustion at the governor vessel could effectively improve urodynamic indexes, reduce residual urine, reduce bladder pressure and increase the maximum capacity of bladder, thereby improving bladder compliance and bladder function.


Asunto(s)
Moxibustión , Traumatismos de la Médula Espinal , Vejiga Urinaria Neurogénica , Terapia por Acupuntura , Animales , Humanos , Moxibustión/métodos , Traumatismos de la Médula Espinal/complicaciones , Vejiga Urinaria Neurogénica/etiología , Vejiga Urinaria Neurogénica/terapia , Urodinámica
13.
Pak J Pharm Sci ; 32(6): 2565-2572, 2019 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-31969287

RESUMEN

Some patients experience lesser degrees of platelet inhibition, which is known as clopidogrel resistance (CR). The goal of our study was to investigate the effects of Xuefu Zhuyu decoction on CR in coronary artery disease patients and whether P2Y12 polymorphisms and its methylation were related to drug response or not. 49 patients diagnosed with CR were randomly divided into control and treatment groups. Platelet functions were measured using Verify-Now P2Y12 assay. By restriction fragment length polymorphism-polymerase chain reaction, the single-nucleotide polymorphisms of rs2046934 and rs6785930 were genotyped. Using bisulphite pyrosequencing assay, we investigated the association of the P2Y12 gene DNA methylation levels and the effects of Xuefu Zhuyu decoction on CR. The results showed that the decoction improved CR (P=0.005), and the patients with the TT genotype in rs2046934 received substantial benefits from Xuefu Zhuyu Decoction, in both P2Y12 reaction units (PRU) and inhibition percentage (PPRU= 0.016; Pinhibition percentage = 0.028). And patients with lower methylation levels of CpG1 were more likely to be TT carriers in rs2046934 (CpG1TT Vs. CpG1TC+CC (%): 39.47±6.20 vs.45.70±8.47, P=0.044). In conclusion, our study indicated that Xuefu Zhuyu decoction might be useful for overcoming CR and the polymorphism of rs2046934 might influence the drug effect.


Asunto(s)
Clopidogrel/farmacología , Metilación de ADN/efectos de los fármacos , Medicamentos Herbarios Chinos/farmacología , Inhibidores de Agregación Plaquetaria/farmacología , Receptores Purinérgicos P2Y12/genética , Plaquetas/efectos de los fármacos , Estudios de Casos y Controles , Resistencia a Medicamentos/efectos de los fármacos , Femenino , Humanos , Masculino , Persona de Mediana Edad , Polimorfismo de Nucleótido Simple/genética
14.
Zhongguo Zhong Yao Za Zhi ; 42(14): 2655-2658, 2017 Jul.
Artículo en Chino | MEDLINE | ID: mdl-29098818

RESUMEN

Triptolide is an active component in traditional Chinese medicine Tripterygium wilfordii. Currently, triptolide has been used to treat various diseases, including lupus, cancer, rheumatoid arthritis and nephritic syndrome. Its main pharmacology efficacies include anti-inflammation, anti-tumor, and immunity suppression. Recent studies have also demonstrated triptolide's protective effect on cardiovascular diseases and osteoporosis. This paper summarizes the pharmacological efficacy of triptolide based on the advance in studies of triptolide.


Asunto(s)
Diterpenos/farmacología , Medicamentos Herbarios Chinos/farmacología , Fenantrenos/farmacología , Tripterygium/química , Compuestos Epoxi/farmacología
15.
BMC Vet Res ; 13(1): 178, 2017 Jun 15.
Artículo en Inglés | MEDLINE | ID: mdl-28619095

RESUMEN

BACKGROUND: Marbofloxacin is a veterinary fluoroquinolone with high activity against Pasteurella multocida. We evaluated it's in vivo activity against P. multocida based on in vivo time-kill data in swine using a tissue-cage model. A series of dosages ranging from 0.15 to 2.5 mg/kg were administered intramuscularly after challenge with P. multocida type B, serotype 2. RESULTS: The ratio of the 24 h area under the concentration-time curve divided by the minimum inhibitory concentration (AUC24TCF/MIC) was the best PK/PD index correlated with the in vivo antibacterial effectiveness of marbofloxacin (R2 = 0.9279). The AUC24TCF/MIC necessary to achieve a 1-log10 CFU/ml reduction and a 3-log10 CFU/ml (90% of the maximum response) reduction as calculated by an inhibitory sigmoid Emax model were 13.48 h and 57.70 h, respectively. CONCLUSIONS: Marbofloxacin is adequate for the treatment of swine infected with P. multocida. The tissue-cage model played a significant role in achieving these PK/PD results.


Asunto(s)
Antibacterianos/uso terapéutico , Fluoroquinolonas/uso terapéutico , Infecciones por Pasteurella/tratamiento farmacológico , Pasteurella multocida , Enfermedades de los Porcinos/tratamiento farmacológico , Animales , Antibacterianos/farmacocinética , Fluoroquinolonas/farmacocinética , Masculino , Pruebas de Sensibilidad Microbiana , Porcinos
16.
Fitoterapia ; 117: 79-83, 2017 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-28040532

RESUMEN

The ethanol extract of the aerial parts of Alstonia yunnanensis Diels afforded five new monoterpenoid indole alkaloids, alstiyunnanenines A-E (1-5), along with one known compound, alstoniascholarine I (6). The structures of the isolated compounds were established based on 1D and 2D (1H-1H COSY, HMQC, and HMBC) NMR spectroscopy, in addition to high resolution mass spectrometry. The isolated compounds were tested in vitro for cytotoxic potential using eight tumor cell lines. As a result, alkaloids 4-6 exhibited cytotoxicities against all tested tumor cell lines, especially against osteosarcoma cell lines (SOSP-9607, MG-63, Saos-2, M663) with IC50 values<6µM.


Asunto(s)
Alstonia/química , Antineoplásicos Fitogénicos/química , Alcaloides de Triptamina Secologanina/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Línea Celular Tumoral , Humanos , Estructura Molecular , Componentes Aéreos de las Plantas/química , Extractos Vegetales/química , Alcaloides de Triptamina Secologanina/aislamiento & purificación
17.
Fitoterapia ; 115: 148-154, 2016 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-27769820

RESUMEN

A series of new Lycopodium alkaloids, namely 1-epi-malycorin A (1), 1-epi-17S-hydroxymalycorin A (2), 6α-hydroxyphlegmariurine A (3), 2S,4R-dihydroxyfawcettimine (4), and 16-hydroxylycodine (5), together with 24 known ones, have been isolated from the club moss Phlegmariurus henryi. The structures of the new compounds were determined by extensive spectroscopic analysis, including 1D and 2D NMR, as well as X-ray crystallographic analysis. Among them, the absolute configurations of 1, 2, and 4 and the structure of 3 were confirmed on the basis of the single-crystal X-ray diffraction analysis. 1-Epi-17S-hydroxymalycorin A (2) was a unique C19N-type Lycopodium alkaloid consisting of a serratinine skeleton with 1,2-propanediol unit. 2S,4R-dihydroxyfawcettimine (4) was a 2,4-dihydroxy derivative of fawcettimine. 16-Hydroxylycodine (5) was the oxidative product of lycodine with an unusual hydroxymethyl group at C-15. All new compounds were evaluated for in vitro acetylcholinesterase (AChE) inhibitory activity and cytotoxicity against four human cancer cell lines.


Asunto(s)
Alcaloides/química , Lycopodiaceae/química , Alcaloides/aislamiento & purificación , Línea Celular Tumoral , Inhibidores de la Colinesterasa/química , Humanos , Indolizinas/química , Indolizinas/aislamiento & purificación , Estructura Molecular , Componentes Aéreos de las Plantas/química
18.
Phytochemistry ; 129: 68-76, 2016 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-27452450

RESUMEN

Phytochemical investigation of the flowers of Inula japonica led to isolation of nine sesquiterpenoids, inujaponins A-I, as well as eighteen known ones. These sesquiterpenoids belong to six skeletal-types, including eudesmane, 1,10-seco-eudesmane, germacrane, guaiane, 4,5-seco-guaiane, and pseudoguaiane sesquiterpenoids. Their structures were established by extensive spectroscopic analysis. The absolute configurations of inujaponin A, eupatolide, and deacetylovatifolin were determined by Cu-Kα X-ray crystallographic analysis. Most of the isolated compounds exhibited potent cytotoxicity against HL-60, SMMC-7721, A-549, MCF-7, and SW-480 cancer cell lines, with IC50 values ranging from 1.57 to 22.58 µM. Some selected compounds also possessed significant inhibitory activity against LPS-induced NO production in RAW264.7 macrophages with IC50 values ranging from 1.42 to 8.99 µM.


Asunto(s)
Flores/química , Inula/química , Sesquiterpenos de Eudesmano/aislamiento & purificación , Animales , Cristalografía por Rayos X , Células HL-60 , Humanos , Concentración 50 Inhibidora , Lipopolisacáridos/farmacología , Macrófagos/efectos de los fármacos , Ratones , Conformación Molecular , Estructura Molecular , Óxido Nítrico/biosíntesis , Sesquiterpenos/química , Sesquiterpenos/aislamiento & purificación , Sesquiterpenos/farmacología , Sesquiterpenos de Eudesmano/química , Sesquiterpenos de Eudesmano/farmacología , Sesquiterpenos de Guayano/química , Sesquiterpenos de Guayano/aislamiento & purificación , Sesquiterpenos de Guayano/farmacología
19.
Org Lett ; 18(8): 1876-9, 2016 Apr 15.
Artículo en Inglés | MEDLINE | ID: mdl-27014919

RESUMEN

Hyperjapones A-E (1-5), novel terpenoid polymethylated acylphloroglucinols (TPAPs) with unusual architectures, were characterized from Hypericum japonicum. Their structures and absolute configurations were determined by comprehensive spectroscopic data and X-ray diffractions. Compound 1 was obtained as a racemic mixture and was separated by a column coated with cellulose tris(4-methylbenzoate) after attempts with various chiral materials. Compounds 1, 2, and 4 exhibited moderate antitumor activities in vitro.


Asunto(s)
Antineoplásicos Fitogénicos/química , Celulosa/análogos & derivados , Hypericum/química , Floroglucinol/química , Extractos Vegetales/química , Terpenos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Antineoplásicos Fitogénicos/farmacología , Benzoatos , Línea Celular Tumoral , Celulosa/química , Humanos , Espectroscopía de Resonancia Magnética , Estructura Molecular , Extractos Vegetales/aislamiento & purificación , Policétidos , Terpenos/aislamiento & purificación , Terpenos/farmacología , Difracción de Rayos X
20.
Artículo en Inglés | MEDLINE | ID: mdl-26989425

RESUMEN

Woad root has been used for the prevention of influenza for hundreds of years in many Asian countries. In this study, the antiviral modes of clemastanin B (CB), epigoitrin, phenylpropanoid portion (PEP), and the mixture of phenylpropanoids, alkaloids, and organic acid portions (PEP + ALK + OA) from wood root extract against influenza virus A FM1 were investigated. The results revealed that CB, epigoitrin, PEP, and PEP + ALK + OA exert their anti-influenza activity via inhibiting the virus multiplication, prophylaxis, and blocking the virus attachment. The primary mode of action of PEP and PEP + ALK + OA is the inhibition of virus replication. The inhibitory effect on virus attachment and multiplication is the main modes for epigoitrin. All the compounds or chemical portions from woad root extract tested in this study do not have direct virucidal activity. Our results provided the comprehensive analysis of the antiviral mechanism of wood root extract.

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