Acute toxicity, antinociceptive, and anti-inflammatory activities of the orally administered crotamine in mice

The chemistry of snake venom and its medicinal potential

“…This toxin is a small defensin purified from the venom of some populations of the South American neotropical rattlesnake (Crotalus durissus) 128 . Although the venom is very toxic, crotamine has low myotoxicity and neurotoxicity 129 . Crotamine is a very basic (with a pI of 10.3 and a charge of +8) amphipathic 42-residue peptide with three disulfide bridges and structural folds similar to those of human α-defensins and β-defensins 60,130 (Fig.…”

“…Crotamine has very high selectivity for actively proliferating cells 133 , such as cancer cells, making it a promising antitumour agent 132 . Its anti-melanoma activity was demonstrated in mice 134 without toxicity to healthy cells and it can even be administered orally 129,135 owing to its excellent resistance to proteolysis and its cell-penetrating ability. Among other bioactivities (TABlE 1), crotamine also exhibits antinociceptive activity (and is 500 times more potent than morphine (mol mol -1 )) 136 and antiinflammatory activity in in vivo mouse models and upon oral administration 129,135 without toxic side effects.…”

“…Its anti-melanoma activity was demonstrated in mice 134 without toxicity to healthy cells and it can even be administered orally 129,135 owing to its excellent resistance to proteolysis and its cell-penetrating ability. Among other bioactivities (TABlE 1), crotamine also exhibits antinociceptive activity (and is 500 times more potent than morphine (mol mol -1 )) 136 and antiinflammatory activity in in vivo mouse models and upon oral administration 129,135 without toxic side effects. Furthermore, its chemical and recombinant syntheses were recently reported [137][138][139] , which are fundamental steps required for upscaling crotamine production.…”

Shedding light on the toxicity of SARS-CoV-2-derived peptide in non-target COVID-19 organisms: A study involving inbred and outbred mice

“…Aiming to evaluate the effect of peptide fragment administration on parameters related to general activity, consciousness, motor coordination, muscle tone, reflexes, central and autonomic nervous system activities, a Hippocratic screening ( Malone, 1977 , Malone, 1983 ) was performed during 15 min, after intraperitoneal injection at 0.5, 1, 2, 4, 8, 12, 24 h. The following signs were evaluated: general activity, vocal frantic, irritability, touch response, tail grip response, contortion, posterior train position, straightening reflex, body tone, force to grasp, ataxia, auricular reflex, corneal reflex, tremors, convulsions, anesthesia, lacrimation, ptosis, urination, defecation, piloerection, hypothermia, breathing, cyanosis, hyperemia, and death. All these signs were evaluated by behavioral observation and systematic clinical examination of the mice, like examine the studies by Moreira et al (2021) and Brígido et al (2021) ). A score for Hippocratic screening was set from 0 (absent) to 4 (intense), according to the observation of animal activity parameters.…”

Pharmacological Activities of Rhododendron afghanicum; an Endemic Species of Khyber Pakhtunkhwa, Pakistan

“…The animals were divided into control and treatment groups randomly following the methodology of. [50] Various concentrations 30, 60 and 90 mg/kg were prepared from each fraction and administered subcutaneously to the albino mice. Drug administered animals were observed for the first four hours followed by the next 24 hours for any toxicity or harmful effect.…”