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人參達瑪烷皂苷Rg1能預防麻醉劑利多卡因的副作用

達瑪烷苷元的口服生物利用度研究表明:滴丸可以是增加吸收率的一種解決方法
達瑪烷苷元PPD和PPT是達瑪烷皂苷經過代謝後,去除側鏈糖基後的最終代謝產物,既往的研究已經表明,達瑪烷苷元比皂苷的活性增加5-10倍。 但是達瑪烷苷元是脂溶性的,難溶於水,因此,其口服的吸收率較低。中國醫科院江蘇分院研究發現:由於其難溶性和腸道吸收後的肝臟首過代謝效應,普通PPD 口服的生物利用度較低。因此,需要一種新型的製劑來增加達瑪烷苷元PPD的吸收率。 滴丸採用了固相分散和共溶技術,能夠大大提高難溶性物質的溶解度。在滴丸中,達瑪烷苷元PPD能夠以微小分子的形式均勻分散在製劑中(固相分...
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利多卡因,作為麻醉劑的物質,通常用於表面和脊髓麻醉。然而,研究表明,利多卡因可能誘發短暫神經症狀和馬尾綜合徵。

湖南長沙中南大學的研究人員發現:人參中的達瑪烷皂苷Rg1(皂苷Rg1)能夠顯著降低利多卡因誘發的的神經細胞凋亡。

這個研究利用Jurkat細胞,以及流式細胞儀和末端脫氧核苷酸轉移酶介導的缺口末端標記法(TUNEL )對此進行了評估。研究數據表明,培養Jurkat細胞在達瑪烷皂苷Rg1存在的情況下,防止了利多卡因誘導的細胞凋亡。

為了探討人參皂苷Rg1對細胞凋亡通路的影響,研究人員又進一步研究了胱天蛋白酶3基因的表達。結果表明,Rg1對利多卡因誘導的細胞凋亡的保護作用是通過改變BCL-2家族蛋白的水平和下調caspase-3來發揮的。

目前的研究表明,達瑪烷皂苷Rg1能夠對培養的Jurkat細胞提供保護,防止利多卡因誘導的細胞凋亡。並且,人參達瑪烷皂苷Rg1能夠阻斷胱天蛋白酶依賴的信號轉導,改變BCL-2家族的水平和下調caspase-3,從阻斷細胞凋亡的發生。

這個研究為達瑪烷皂苷Rg1在體內治療利多卡因引起的短暫神經系統症狀和馬尾綜合徵提供了理論基礎。

英文摘要如下:

Protective effect of ginsenoside Rg1 on lidocaine-induced apoptosis.
Mol Med Rep. 2013 Nov 21;
Authors: Li H, Xu J, Wang X, Yuan G
Abstract
Lidocaine, as an anesthetic substance, is often used for surface and spinal anesthesia. However , studies have shown that lidocaine may induce transient neurological symptoms and cauda equina syndrome. In the present study the effects of the ginsenoside Rg1 ( Rg1 ) on lidocaine‑induced apoptosis were assessed in Jurkat cells using flow cytometry and terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL). The data showed that incubation with Rg1 provides protection against lidocaine‑induced apoptosis in cultured Jurkat cells. In order to investigate the effect of Rg1 on the apoptosis pathway, caspase 3 gene expression was determined. The results suggested that the protective effect of Rg1 on lidocaine‑induced apoptosis is mediated by altering the level of B‑cell lymphoma‑2 (BCL‑2) family proteins and downregulating caspase‑3 expression. In conclusion, the present study demonstrated that incubation with Rg1 provides protection against lidocaine‑induced apoptosis in cultured Jurkat cells. In addition, the study demonstrated that Rg1 is a notable antiapoptotic molecule that is capable of blocking the caspase‑dependent signaling cascade in Jurkat cells, and that the protective effect of Rg1 on lidocaine‑induced apoptosis is mediated by altering levels of BCL‑2 family proteins and downregulating caspase‑3 expression. The present study provides the basis for understanding and evaluating the effect of Rg1 in the in vivo treatment of lidocaine-induced transient neurological symptoms and cauda equina syndrome by lidocaine.
PMID: 24270314 [PubMed - as supplied by publisher]

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