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首页> 外文期刊>Phytomedicine : >Inhibition of the myotoxic activity of Bothrops jararacussu venom and its two major myotoxins, BthTX-I and BthTX-II, by the aqueous extract of Tabernaemontana catharinensis A. DC. (Apocynaceae).
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Inhibition of the myotoxic activity of Bothrops jararacussu venom and its two major myotoxins, BthTX-I and BthTX-II, by the aqueous extract of Tabernaemontana catharinensis A. DC. (Apocynaceae).

机译：中华绒螯蟹（Tabernaemontana catharinensis A.DC）的水提取物对Bothrops jararacussu毒液及其两种主要肌毒素BthTX-I和BthTX-II的肌毒性活性的抑制作用。 （夹竹桃科）。

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Partial neutralization of the myotoxic effect of Bothrops jararacussu venom (BV) and two of its myotoxins [bothropstoxin-I (BthTX-I), catalytically inactive, and II (BthTX-II), showing low PLA2 activity], by the lyophilized aqueous extract of Tabernaemontana catharinensis (AE), was studied in rat isolated soleus muscle preparations (in vitro) and through i.m. injection in the gastrocnemius muscle (in vivo) by determination of creatine kinase (CK) activity and histopathological analysis. Incubation of soleus muscle for 1 h with BV or toxins (20 microg/ml) plus AE (400 microg/ml) added immediately after BV, BthTX-I or BthTX-II reduced CK levels by 53%, 37% and 56%, respectively. The myonecrotic effects of BV (20 microg/ml) upon soleus muscle was reduced 24%, 35% and 36% when AE (400 microg/ml) was added 1 h after BV and CK was evaluated 30 min, 1 and 2 h later, respectively. For BthTX-I these values were 46%, 48% and 47%, while for BthTX-II no inhibitory effect was detected. Histological analysis of soleus muscle after incubation with AE (400 microg/ml, 1 h) did not reveal any change in muscle fibers, but severe necrosis induced by BV or toxins (20 microg/ml) was clearly in evidence, and decreased significantly when soleus muscle was protected by AE. This protection was also observed when AE was administered 1 h after BV or BthTX-I, but not after BthTX-II. AE did not inhibit the catalytic PLA2 activity of BthTX-II or BV and did not change the PAGE pattern of BV, BthTX-I or BthTX-II. In vivo assays were performed in 100-g rats and maximal CK release was attained at a dose of 100 microg of BV, 3 h after injection. AE was not effective when injected 20 s after BV or toxins. However, injecting BV or toxins (100 microg), which were pre-incubated with AE (2 mg) caused an inhibition of 57%, 59% and 51%, respectively, with zero time pre-incubation, but was less effective with 1 h pre-incubation. This plant represents a potential source of promising myotoxin inhibitors.
机译：冻干水提取物部分中和了百日草（Broprops jararacussu）毒液（BV）及其两种肌毒素[催化活性不高的bothropstoxin-I（BthTX-I）和II（BthTX-II），显示出较低的PLA2活性]的肌毒性作用。在大鼠离体比目鱼肌制备物中（体外）和通过im进行了Tabernaemontana catharinensis（AE）的研究通过测定肌酸激酶（CK）活性和组织病理学分析，注射腓肠肌（体内）。在BV，BthTX-I或BthTX-II将CK水平降低53％，37％和56％后立即添加BV或毒素（20 microg / ml）加AE（400 microg / ml）的比目鱼肌孵育1小时，分别。在BV 1小时后添加AE（400 microg / ml）并在30分钟，1小时和2小时后评估CK时，BV（20微克/毫升）对比目鱼肌的坏死作用降低了24％，35％和36％ ， 分别。对于BthTX-I，这些值为46％，48％和47％，而对于BthTX-II，未检测到抑制作用。用AE（400 microg / ml，1 h）孵育后的比目鱼肌的组织学分析未显示肌肉纤维有任何变化，但BV或毒素（20 microg / ml）引起的严重坏死很明显，并且当比目鱼肌受到AE保护。当在BV或BthTX-I后1小时而不是BthTX-II后1小时给予AE时，也观察到这种保护作用。 AE不会抑制BthTX-II或BV的催化PLA2活性，也不会改变BV，BthTX-I或BthTX-II的PAGE模式。在注射后3小时，在100-g大鼠中进行体内测定，并且在100μgBV的剂量下获得最大的CK​​释放。 BV或毒素注射20 s后，AE无效。但是，注射预先与AE（2 mg）一起温育的BV或毒素（100 microg）会在零时间的预温育下分别产生57％，59％和51％的抑制作用，但在1次预温育下效果较差h预孵育。该植物代表有希望的肌毒素抑制剂的潜在来源。

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