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1.
Am J Chin Med ; 51(8): 2095-2120, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37865870

RESUMEN

[Formula: see text]-Escin is an oleanane-type pentacyclic triterpenoid saponin extracted from the seeds of Aesculus hippocastanum (AH), which is more widely distributed. [Formula: see text]-Escin sodium has been approved by the American FDA for clinical usage. This paper is intended to summarize an updated and comprehensive review of the pharmacological activities, pharmacokinetic properties, toxicity, and analytical methods of [Formula: see text]-escin. Studies have shown that [Formula: see text]-escin has significant antitumor, antiviral, anti-inflammatory, and other activities alongside less adverse effects and higher safety than other compounds. The review shows that the pharmacological effects of [Formula: see text]-escin involve mechanisms such as ATM/[Formula: see text]H2AX, RhoA/Rock, GSK-3[Formula: see text]/[Formula: see text]-Catenin, HER2/HER3/Akt, and PI3K/Akt signaling pathways, and Cyclin A, p21[Formula: see text], survivin, Bcl-2, Mcl-1, Caspases, TGF-[Formula: see text], MMPs, and TNF-[Formula: see text] among other inflammatory factors. [Formula: see text]-Escin has significant cytotoxicity; the use of the chitosan/xanthan gum-based polyelectrolyte complexes PA1 and PC-11 to modify it not only to reduces its toxicity, but also improves its drug efficacy. Because of this, these compounds may become a new research hotspot. [Formula: see text]-Escin in vivo metabolism can be converted by the CYP1A2 enzyme in the intestinal flora to produce [Formula: see text]-escin, deacylated, deglycosylated, and 21[Formula: see text]-[Formula: see text]-crotonoyl-protoescin, and the binding rate of the plasma proteins is higher than 90%. These are mainly metabolized by the liver, kidneys, and other organs, and excreted in the form of urine and feces. The number of reports on the specific mediators of the metabolism of [Formula: see text]-escin and their mechanisms and metabolites is relatively small; furthermore, the results are vague. Therefore, a complete and in-depth exploration of the pharmacokinetic characteristics of [Formula: see text]-escin is needed to provide a more complete and effective theoretical reference for the study of its pharmacodynamic activity.


Asunto(s)
Escina , Extractos Vegetales , Escina/farmacología , Extractos Vegetales/farmacología , Glucógeno Sintasa Quinasa 3 , Fosfatidilinositol 3-Quinasas , Proteínas Proto-Oncogénicas c-akt
2.
Front Pharmacol ; 14: 1164784, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37649892

RESUMEN

Enterovirus 71 (EV71) commonly causes symptoms such as hand, foot, and mouth disease (HFMD) in infants and children and may lead to neurological disease and even death in severe cases. Appropriate vaccines for the prevention of HFMD are available in the clinic; however, they present different and serious adverse effects that cannot guarantee compliance and efficacy. The purpose of this study was to analyze the potential mechanism of Bryum billardieri Schwaegr. (BBS) against EV71 and analyze its potential active components. A previous in vitro antiviral assay was used to determine the best extraction method for the active site of BBS against EV71, and the results showed that the antiviral activity of BBS was more pronounced in the fraction that was extracted by aqueous extraction and alcoholic precipitation and then obtained by purification on a silica gel column (dichloromethane:methanol = 0:100). In addition, the therapeutic effects of BBS on EV71-infected mice were further investigated by in vivo pharmacological experiments. BBS reduced the lung index, viral titer, and degree of EV71-induced lung, brain, and skeletal muscle damage. The mechanism of anti-EV71 activity of BBS was also investigated by using ELISA and qRT-PCR, and it was found that BBS exerted its action mainly by regulating the expression of TLR3, TLR4, TNF-α, IL-2, and IFN-γ by modulating the activation of NF-κB and JAK2/STAT1 signaling pathways. Finally, the chemical structures of the active monomers in BBS were determined by using UPLC-MS and NMR techniques. The study revealed that one of the monomers on which BBS exerts its antiviral activity is saponarin. In conclusion, the results of this study suggest that BBS is considered a natural anti-EV71 product with enormous potential, and saponarin would be its non-negligible active monomer.

3.
Biomed Res Int ; 2022: 1213278, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36119926

RESUMEN

Objective: This research aims to investigate and analyze the impact of alendronate sodium (ALN) plus elcatonin (EC) in treating postoperative bone pain (BP) in patients with osteoporotic fractures (OPFs). Methods: One hundred and thirty-eight cases of OPFs admitted between July 2018 and July 2021 were selected, of which 68 cases receiving ALN were set as the control group and 70 cases receiving ALN plus EC were set as the research group. Intercomparisons were performed in terms of BP, curative effect, complication rate, and serum bone metabolism indexes such as bone Gla protein (BGP), parathyroid hormone (PTH), and bone alkaline phosphatase (BALP). Results: Better postoperative BP relief, higher overall response rate, and lower complication rate were identified in the research group versus the control group. On the other hand, the research group presented with increased BGP and BALP after treatment, higher than those in the control group, while the posttreament PTH decreased obviously and was lower versus the control group. Conclusions: For OPF patients, ALN plus EC contributes to significantly reduced postoperative BP, improved clinical efficacy, higher treatment safety, and better bone metabolism, which has high clinical application value.


Asunto(s)
Alendronato , Fracturas Osteoporóticas , Alendronato/uso terapéutico , Fosfatasa Alcalina , Calcitonina/análogos & derivados , Humanos , Osteocalcina , Fracturas Osteoporóticas/complicaciones , Fracturas Osteoporóticas/tratamiento farmacológico , Fracturas Osteoporóticas/cirugía , Dolor Postoperatorio/tratamiento farmacológico , Hormona Paratiroidea
4.
J Orthop Surg Res ; 14(1): 421, 2019 Dec 10.
Artículo en Inglés | MEDLINE | ID: mdl-31823822

RESUMEN

BACKGROUND: Secondary osteoporosis may occur in patients with rheumatoid arthritis (RA), causing irreversible joint damage and disability. Bisphosphonates, the recently developed bone resorption inhibitors, have demonstrated significant therapeutic effects on senile and postmenopausal osteoporosis. This study evaluated the efficacy and safety of zoledronic acid (ZOL), with or without methotrexate (MTX), for the prevention and treatment of bone destruction in RA patients. METHODS: We recruited 66 RA patients with symptoms of secondary osteoporosis. They were randomized into three treatment groups-combined treatment with MTX and ZOL, ZOL monotherapy, or MTX monotherapy-in two consecutive 6-month periods. The participants were followed for 12 months. At the end of each treatment period, improvement in disease activity, bone destruction, and fracture risk were evaluated. RESULTS: Combined treatment with ZOL and MTX had significantly better clinical efficacy compared with either ZOL or MTX monotherapy (P < 0.05). The combination significantly improved the lumbar spine and hip BMD and reduced FRAX scores, suggesting that ZOL combined with MTX reduces bone loss and risk of hip fracture in RA patients with secondary osteoporosis. CONCLUSION: ZOL has a synergistic effect when combined with MTX, inhibiting RA disease activity, reducing fracture risk, and improving quality of life in RA patients with secondary osteoporosis. TRIAL REGISTRATION: Chinese Clinical Trial Registry, ChiCTR1800019290. Registered 3 November 2018-Retrospective registered, http://www.chictr.org.cn/showproj.aspx?proj = 31758.


Asunto(s)
Artritis Reumatoide/diagnóstico por imagen , Artritis Reumatoide/tratamiento farmacológico , Conservadores de la Densidad Ósea/uso terapéutico , Osteoporosis/diagnóstico por imagen , Osteoporosis/tratamiento farmacológico , Ácido Zoledrónico/uso terapéutico , Artritis Reumatoide/complicaciones , Densidad Ósea/efectos de los fármacos , Densidad Ósea/fisiología , Conservadores de la Densidad Ósea/farmacología , Femenino , Estudios de Seguimiento , Humanos , Masculino , Persona de Mediana Edad , Osteoporosis/etiología , Ácido Zoledrónico/farmacología
5.
Zhongguo Gu Shang ; 30(4): 356-359, 2017 Apr 25.
Artículo en Chino | MEDLINE | ID: mdl-29349988

RESUMEN

OBJECTIVE: To compare the analgesic effect between multimodal and patient-controlled intravenous analgesia(PCIA) in patients with rheumatoid arthritis(RA) in the perioperative period of knee joint replacement. METHODS: From June 2015 to June 2016, 40 RA patients undergoing total knee arthroplasty were randomly divided into two groups. There were 20 patients in PCIA group, including 3 males and 17 females, with an average age of(59.6±2.3) years old, who received controlled instillation of sufentanil analgesia controlled by an intravenous analgesia pump. There were 20 patients in multiple model analgesia group, including 2 males and 18 females, with an average age of(56.3±1.3) years old, who were treated with continuous femoral nerve block, local injection of knee joint and combined buprenorphine patches. The VAS score and the incidence of adverse reactions and HSS score were compared between the two groups after operation. The advantages and disadvantages of the two modes of analgesia were evaluated. RESULTS: On the 6 th and 24 th hours after surgery, the VAS scores of the multimodal analgesia group were significantly lower than those of the PCIA group(P<0.01). On the 48 th hour after surgery, the VAS scores was significantly lower in the multimodal analgesia group than those in PCIA group(P<0.000 1), both in the state of motion and at rest. On the 1 st week after surgery, the HSS score of the multimodal analgesia group was significantly higher than that in the PCIA group(P<0.000 1). The pain score and the degree of activity in HSS score of the multimodal analgesia group were better than those in PCIA group (P<0.05). The functional score of multimodal analgesia group was significantly better than that of PCIA group(P<0.01). But there was no significant difference in muscle strength scores between two groups. CONCLUSIONS: Multimodal analgesia is an ideal analgesic plan for total knee arthroplasty TKA patients with RA in perioperative period, which has good effects and little adverse reaction.


Asunto(s)
Analgesia Controlada por el Paciente , Anestesia Intravenosa , Anestésicos Intravenosos/administración & dosificación , Artritis Reumatoide/cirugía , Artroplastia de Reemplazo de Rodilla , Manejo del Dolor/métodos , Sufentanilo/administración & dosificación , Femenino , Humanos , Masculino , Persona de Mediana Edad , Bloqueo Nervioso , Periodo Perioperatorio
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