ß-Escin: An Updated Review of Its Analysis, Pharmacology, Pharmacokinetics, and Toxicity.

[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.

Zoledronic acid ameliorates the effects of secondary osteoporosis in rheumatoid arthritis patients.

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.

[Comparison of analgesic effects between multimodal and patient-controlled intravenous analgesia in patients with rheumatoid arthritis in the perioperative period of total knee arthroplasty].

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.