Abstract
Buthus martensii Karsch (BmK), is a kind of traditional Chinese medicine, which has been used for a long history for the treatment of many diseases, such as inflammation, pain and cancer. In this study, DKK-SP1/2/3 genes were screened and extracted from the cDNA library of BmK. The DKK-SP1/2/3 were expressed by using plasmid pSYPU-1b in E. coli BL21, and recombinant proteins were obtained by column chromatography. In the xylene-induced mouse ear swelling and carrageenan-induced rat paw swelling model, DKK-SP1 exerted a significant anti-inflammatory effect by inhibiting the expression of Nav1.8 channel. Meanwhile, the release of pro-inflammatory cytokines (COX-2, IL-6) was decreased significantly and the release of anti-inflammatory cytokines (IL-10) were elevated significantly. Moreover, DKK-SP1 could significantly decrease the Nav1.8 current in acutely isolated rat DRG neurons. In the acetic acid-writhing and ION-CCI model, DKK-SP2 displayed significant analgesic activity by inhibiting the expression of the Nav1.7 channel. Moreover, DKK-SP2 could significantly inhibit the Nav1.7 current in the hNav1.7-CHO cells.
Highlights
The scorpion is one of the oldest arthropods on earth, which has evolved for more than 400 million years [1]
Na+ channel toxins can be further divided into α-scorpion toxins and β-scorpion toxins [12]. α-scorpion toxins act on site 3 of the Na+
It is concluded that DKK-SP1 has a good anti-inflammatory effect, which may be achieved by reducing the expression of Nav1.8 protein and inhibiting Nav1.8 current
Summary
The scorpion is one of the oldest arthropods on earth, which has evolved for more than 400 million years [1]. Scorpion toxins are believed as the major component for its pharmacological actions [7]. Only 400 out of 100,000 toxins were discovered in the scorpion gland [8]. The scorpion toxins have consisted of 28 to 76 amino acid residues with 3–4 pairs of disulfide bonds. The scorpion toxins could recognize and activate ion channels receptors so as to change their permeability. According to their combined receptors, scorpion toxins can be divided into Na+ channel toxins [9], K+ channel toxins [10], Cl- channel toxins and Ca2+ channel toxins [11]. Α-scorpion toxins act on site 3 of the Na+ Na+ channel toxins can be further divided into α-scorpion toxins and β-scorpion toxins [12]. α-scorpion toxins act on site 3 of the Na+
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
