Triterpenoid saponins, new metalloprotease snake venom inhibitors isolated from Pentaclethra macroloba.
We report here the antiproteolytic and antihemorrhagic properties of triterpenoid saponin inhibitors, named macrolobin-A and B, from Pentaclethra macroloba, against Bothrops snake venoms. The inhibitors were able to neutralize the hemorrhagic, fibrin(ogen)olytic, and proteolytic activities of class P-I and P-III metalloproteases isolated from B. neuwiedi and B. jararacussu venoms. Clotting and fibrinogenolytic activities induced by snake venoms and isolated thrombin-like enzymes were partially inhibited. Furthermore, the potential use of these inhibitors to complement antivenom therapy as an alternative treatment and/or used as molecular models for development of new therapeutical agents in the treatment of snake bite envenomations needs to be evaluated in future studies.
da Silva
Jocivânia O
JO
Departamento de Análises Clínicas, Toxicológicas e Bromatológicas, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, FCFRP, Universidade de São Paulo, USP, Ribeirão Preto-SP, Brazil.
Fernandes
Renata S
RS
Ticli
Fábio K
FK
Oliveira
Clayton Z
CZ
Mazzi
Maurício V
MV
Franco
João J
JJ
Giuliatti
Silvana
S
Pereira
Paulo S
PS
Soares
Andreimar M
AM
Sampaio
Suely V
SV
D000818:Animals; D031175:Baccharis / Q000737:chemistry; D001777:Blood Coagulation / Q000187:drug effects; D002240:Carbohydrate Sequence; D002942:Circular Dichroism; D003435:Crotalid Venoms / Q000201:enzymology / Q000633:toxicity; D005337:Fibrin / Q000737:chemistry; D005340:Fibrinogen / Q000737:chemistry; D006470:Hemorrhage / Q000139:chemically induced / Q000517:prevention & control; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D008969:Molecular Sequence Data; D010741:Phospholipases A / Q000037:antagonists & inhibitors / Q000633:toxicity; D010936:Plant Extracts / Q000737:chemistry; D010944:Plants / Q000737:chemistry*; D012503:Saponins / Q000302:isolation & purification / Q000494:pharmacology*; D015842:Serine Proteinase Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D012910:Snake Venoms / Q000201:enzymology* / Q000633:toxicity*; D013056:Spectrophotometry, Ultraviolet; D014315:Triterpenes / Q000302:isolation & purification / Q000494:pharmacology*
D003435:Crotalid Venoms; D010936:Plant Extracts; D012503:Saponins; D015842:Serine Proteinase Inhibitors; D012910:Snake Venoms; D014315:Triterpenes; C523182:macrolobin A; C523183:macrolobin B; D005337:Fibrin; D005340:Fibrinogen; D010741:Phospholipases A