Some animals on the earth are poisonous. Venom is the "weapon" they use to defend themselves or attack. But intelligent humans turn some highly toxic substances into useful and even life-saving drugs, such as Botox. But beauty loving women all know that some wrinkles can be removed by injecting botox to paralyze facial muscles. In fact, Botox was first used in the treatment of ophthalmic diseases, such as crossed eyes and eyelid twitch, and now it is also used to prevent migraine.

Botox is only one of the most widely used toxic substances. Scientists are increasingly turning the deadliest substances in the animal kingdom into drugs, which can produce good therapeutic effects with only a small amount. The molecular weight of animal toxin polypeptide is relatively small compared with other toxins, and it has high specificity and molecular diversity. It is directly encoded by genes, with small dosage but strong toxicity. It is the key physiological component that acts on the target organism. Therefore, as a natural resource of drug research and development, animal toxin polypeptides are highly valued. A large number of drugs derived from animal toxin polypeptides have been approved by the US FDA for listing, and some polypeptides derived from animal toxins are in the clinical trial stage.

Snake toxin polypeptide drug

Snake venom is a mixture of enzyme and non enzyme protein / polypeptide. Many drugs derived from snake venom polypeptide have been used in clinical treatment.

A pentapeptide compound extracted from the venom of Agkistrodon halys Pallas is the enhancer of bradykinin. The oral drug captopril was synthesized by tailoring its structure and modifying its minimal pharmacophore ala Pro dipeptide. Captopril can reduce blood pressure by increasing the activity of bradykinin and inhibiting thrombin, which is a routine drug for the treatment of hypertension.Pharmacologists modified the structure of captopril, and successively developed enalapril, lisinopril, ramipril, fosinopril and other drugs.

Tirofiban, found in viper, is a protein peptide mimic of viper venom. It is an antiplatelet drug, also known as glycoprotein Ⅱ B / Ⅲ a inhibitor. Etifeba, another antiplatelet drug, is a synthetic cyclopeptide, which is almost listed at the same time as tirofiban. It imitates the components of the venom of the southeast Jurassic rattlesnake, and has a strong effect of disintegrin. Studies have shown that etifeba is slightly safer than tirofiban in patients with acute coronary syndrome, but there is no significant difference in efficacy.

Ximelagatra, an oral anticoagulant from Naja naja atra, is a vitamin K antagonist, which has been approved for marketing in some European countries and South American countries, but has not been approved for marketing by FDA, because the increase of alanine aminotransferase may lead to the increase of the hepatotoxicity of the drug. As a result, the development of the compound was halted and withdrawn from the market in 2006.

Cenderitide, from the venom of Green Mamba snake, is the first toxic natriuretic peptide (NP), which can inhibit the degradation of neutral endopeptidase to some extent. Preliminary clinical data show that cenderitide can improve renal function. A series of phase I and phase II trials have been completed in patients with heart failure treated with cenderitide, but the researchers are concerned that the adverse effects of the drug may outweigh the clinical benefits.

In addition, there are analgesic drugs refined from cobratoxin extracted from short-chain α - neurotoxin of cobra venom. Cardiotoxin Ⅲ (also known as cytotoxin Ⅲ) isolated from Taiwan cobra venom is used to prevent the migration and invasion of MDA-MB-231 breast cancer cells, as well as double chain snake venom thrombin for hemostasis.

Scorpion toxin polypeptide drug

In traditional Chinese medicine, scorpion is a kind of precious traditional Chinese medicine resource, which has the effects of calming the wind, relieving spasm, dredging collaterals, relieving pain and attacking toxin and dispersing the knot. It is mainly used for the diagnosis and treatment of convulsion, epilepsy, spasm, stroke, tetanus and other diseases. The venom of scorpion exists in the gland tissue of scorpion tail, and its components are complex, including neurotoxin, cytotoxic peptide, protease and other toxic components. These toxins combined with ion channel specificity can block the channel current or change the gating dynamics, thus changing the permeability of cell membrane.

The Chlorotoxin polypeptide found in scorpion venom can delay the activity of human glioma cells in vitro. The venom of Venezuelan scorpion has antibacterial and antiparasitic activities, which can inhibit the growth of Leishmania in vitro. Bengalin, the toxin protein of black scorpion, can induce apoptosis of human leukemic cells and improve the biochemical indexes of osteoporosis in female rats in vitro. α - neurotoxin found in scorpion venom can delay the deactivation of sodium channel at neuromuscular junction, while the deactivation of sodium channel may enhance the reflex of neuromuscular and airway contraction, which can theoretically treat sleep apnea.

Anemone toxin polypeptide drug

Anemone is one of the oldest poisonous animals. Like other members of the phylum spinifera, Anemone has many special spiny cells, which are widely distributed in the whole body of animals. SHK toxin isolated from sea anemone is an effective channel blocker, which plays an important role in the activation of human effector memory T cells (proliferation and cytokine production). SHK can treat T cell-mediated autoimmune diseases, such as multiple sclerosis and rheumatoid arthritis. Receptor blockers are also considered as targets for obesity, and SHK toxin has potential applications in the treatment of obesity and insulin resistance. Shk-186 is an analogue of SHK toxin, known as dalazatide drug, used to treat autoimmune diseases.

Hirudotoxin polypeptide drugs

Leech is an important traditional Chinese medicine, which is used to treat cerebral hemorrhage and other thrombus related diseases. Hirudin is an effective anticoagulant in the salivary glands of leeches. Hirudin can inhibit the formation of thrombus and prevent the coagulation of host blood. Pharmacology research shows that hirudin has the functions of anticoagulation, antithrombotic, anti atherosclerotic, anti platelet aggregation, anti-tumor, anti-inflammatory, improving Hemorheology and protecting cerebral ischemia-reperfusion injury.

Hirudin based anticoagulants include recombinant hirudin (lepirudin and Desirudin) and hirudin analogue bivalirudin. Lepirudin was approved by the FDA for the treatment of heparin related thrombocytopenia (HIT) and related thromboembolic diseases, but was withdrawn in 2012 for commercial reasons. Disirudin has been approved by FDA for the prevention of deep vein thrombosis or knee arthroplasty.

Bivalirudin has been approved by FDA for the treatment of unstable angina after percutaneous coronary intervention, with an increased risk of hit or hit. However, the use of these thrombin inhibitors has some disadvantages, such as bleeding, strong dependence on renal function, lack of antidotes and rebound hypercoagulability. Therefore, it is urgent to develop efficient and safe derivatives of hirudin.

Great achievements have been made in the clinical application of animal toxin polypeptide drugs, which makes more people realize the great potential of the research and development of animal toxin polypeptide drugs. At present, a large number of animal toxins have not been developed, and many problems of animal toxins in clinical treatment, such as the effectiveness and safety, need further verification. Therefore, drug development based on animal toxins also has great challenges.

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Chengdu Shengnuo Biotechnology Co., Ltd. has "Chengdu polypeptide drug engineering technology research center" in Chengdu, mainly engaged in polypeptide, polypeptide drug and beauty peptide research. Our zero defect has passed the FDA certification, and now it has become the first-class professional peptide drug and product development, technology transfer, technical service and peptide drug industry in the scale production and export of China's parks.