Effects of aqueous extract of Casearia sylvestris (Flacourtiaceae) on actions of snake and bee venoms and on activity of phospholipases A2.
The crude aqueous extract from the leaves of Casearia sylvestris, a plant found in Brazilian open pastures, was assayed for its ability to inhibit phospholipase A2 (PLA2) activity and some biological activities of bee and several snake venoms, and of a number of isolated PLA2s. The extract induced partial inhibition of the PLA2 activity of venoms containing class I, II and III PLA2s. When tested against the purified toxins, it showed the highest efficacy against class II PLA2s from viperid venoms, being relatively ineffective against the class I PLA2 pseudexin. In addition, C. sylvestris extract significantly inhibited the myotoxic activity of four Bothrops crude venoms and nine purified myotoxic PLA2s, including Lys-49 and Asp-49 variants. The extract was able to inhibit the anticoagulant activity of several isolated PLA2s, with the exception of pseudexin. Moreover, it partially reduced the edema-inducing activity of B. moojeni and B. jararacussu venoms, as well as of myotoxins MjTX-II and BthTX-I. The extract also prolonged the survival time of mice injected with lethal doses of several snake venoms and neutralized the lethal effect induced by several purified PLA2 myotoxins. It is concluded that C. sylvestris constitutes a rich source of PLA2 inhibitors.
Borges
M H
MH
Departamento de Genética e Bioquímica, Universidade Federal de Uberlândia, UFU, MG, Brazil.
Soares
A M
AM
Rodrigues
V M
VM
Andrião-Escarso
S H
SH
Diniz
H
H
Hamaguchi
A
A
Quintero
A
A
Lizano
S
S
Gutiérrez
J M
JM
Giglio
J R
JR
Homsi-Brandeburgo
M I
MI
D000818:Animals; D000925:Anticoagulants / Q000494:pharmacology; D000992:Antitoxins / Q000494:pharmacology*; D001514:Bee Venoms / Q000037:antagonists & inhibitors / Q000378:metabolism*; D003435:Crotalid Venoms / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004487:Edema / Q000188:drug therapy; D004591:Electrophoresis, Polyacrylamide Gel; D008297:Male; D051379:Mice; D010741:Phospholipases A / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D054467:Phospholipases A2; D010936:Plant Extracts / Q000494:pharmacology*; D019685:Rosales / Q000737:chemistry*; D012910:Snake Venoms / Q000037:antagonists & inhibitors / Q000378:metabolism*; D013997:Time Factors
D000925:Anticoagulants; D000992:Antitoxins; D001514:Bee Venoms; D003435:Crotalid Venoms; D010936:Plant Extracts; D012910:Snake Venoms; C078097:bothropstoxin; D010741:Phospholipases A; D054467:Phospholipases A2