Abstract
Centipedes have been used as traditional medicine for thousands of years in China. Centipede venoms consist of many biochemical peptides and proteins. Factor Xa (FXa) is a serine endopeptidase that plays the key role in blood coagulation, and has been used as a new target for anti-thrombotic drug development. A novel FXa inhibitor, a natural peptide with the sequence of Thr-Asn-Gly-Tyr-Thr (TNGYT), was isolated from the venom of Scolopendra subspinipes mutilans using a combination of size-exclusion and reverse-phase chromatography. The molecular weight of the TNGYT peptide was 554.3 Da measured by electrospray ionization mass spectrometry. The amino acid sequence of TNGYT was determined by Edman degradation. TNGYT inhibited the activity of FXa in a dose-dependent manner with an IC50 value of 41.14 mg/ml. It prolonged the partial thromboplastin time and prothrombin time in both in vitro and ex vivo assays. It also significantly prolonged whole blood clotting time and bleeding time in mice. This is the first report that an FXa inhibiting peptide was isolated from centipedes venom.
Highlights
Factor Xa (FXa) is a serine endopeptidase that plays the key role in blood coagulation, and has been used as a new target for anti-thrombotic drug development
A novel FXa inhibitor, a natural peptide with the sequence of Thr-Asn-Gly-TyrThr (TNGYT), was isolated from the venom of Scolopendra subspinipes mutilans using a combination of sizeexclusion and reverse-phase chromatography
Fraction 2 was separated by reverse-phase high performance liquid chromatography (RP-HPLC) on a Lichrospher C18 column (Fig. 1b)
Summary
Y. Kong State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, People’s Republic of China. Li School of Pharmacy, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, People’s Republic of China. In China, centipedes have been used for thousands of years as a traditional Chinese medicine for treating the diseases, such as stroke-induced hemiplegia, apoplexy, epilepsy, tetanus, whooping cough, tuberculosis, scald burns, and pyocutaneous disease. They have been prescribed for treating cardiovascular diseases in Korea, China and other countries in East Asia for several hundred years (Pemberton 1999)
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