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1.
Biomed Pharmacother ; 78: 248-256, 2016 Mar.
Article in English | MEDLINE | ID: mdl-26898449

ABSTRACT

Chamomile (Matricaria chamomilla L., Asteraceae) is a medicinal plant widely used as remedy for pain and gastric disorders. The association of non-steroidal anti-inflammatory drugs (NSAIDs) with medicinal plant extracts may increase its antinociceptive activity, permit the use of lower doses and limit side effects. The aim was to isolate and identify the main chemical constituents of Matricaria chamomilla ethanolic extract (MCE) as well as to explore their activity as cyclooxygenase (COX) inhibitors in silico; besides, to examine the interaction between MCE and diclofenac on nociception in the formalin test by isobolographic analysis, and to determine the level of gastric injury in rats. Three terpenoids, α-bisabolol, bisabolol oxide A, and guaiazulene, were isolated and identified by (1)H NMR. Docking simulation predicted COX inhibitory activity for those terpenoids. Diclofenac, MCE, or their combinations produced an antinociceptive effect. The sole administration of diclofenac and the highest combined dose diclofenac-MCE produced significant a gastric damage, but that effect was not seen with MCE alone. An isobologram was constructed and the derived theoretical ED35 for the antinociceptive effect was significantly different from the experimental ED35; hence, the interaction between diclofenac and MCE that mediates the antinociceptive effect is synergist. The MCE contains three major terpenoids with plausible COX inhibitory activity in silico, but α-bisabolol showed the highest affinity. Data suggest that the diclofenac-MCE combination can interact at the systemic level in a synergic manner and may have therapeutic advantages for the clinical treatment of inflammatory pain.


Subject(s)
Cyclooxygenase 2 Inhibitors/isolation & purification , Cyclooxygenase 2 Inhibitors/pharmacology , Diclofenac/pharmacology , Matricaria/chemistry , Molecular Docking Simulation , Nociception/drug effects , Plant Extracts/pharmacology , Stomach/pathology , Animals , Cyclooxygenase 2 Inhibitors/chemistry , Drug Interactions , Drug Synergism , Male , Motor Activity/drug effects , Plant Extracts/chemistry , Proton Magnetic Resonance Spectroscopy , Rats, Wistar , Reference Standards , Stomach/drug effects , Thermodynamics
2.
Molecules ; 16(3): 2107-18, 2011 Mar 02.
Article in English | MEDLINE | ID: mdl-21368722

ABSTRACT

Lectins comprise a heterogeneous class of proteins that recognize the carbohydrate moieties of glycoconjugates with high specificity. Numerous studies have shown that lectins are capable of recognizing specific carbohydrate moieties displayed by malignant cells or tissues. The present work was performed to investigate the effects of tepary bean (Phaseolus acutifolius) lectins on proliferation, colony formation, and alteration of DNA synthesis of human malignant cells. Tepary bean lectin showed dose dependent  effects on the inhibition of viability as well as on colony formation in two human malignant cells lines (C33-A, Sw480); By contrast, tepary bean lectin only showed significant effects on DNA synthesis on Sw480 cells. Our results provide evidence of the anti- proliferative and cytotoxic effects of the tepary bean lectins on C33-A and Sw480 cells lines.


Subject(s)
Adenocarcinoma/pathology , Colonic Neoplasms/pathology , Lectins/pharmacology , Neoplasms, Glandular and Epithelial/pathology , Uterine Cervical Neoplasms/pathology , Cell Proliferation/drug effects , Drug Screening Assays, Antitumor , Electrophoresis, Polyacrylamide Gel , Female , Humans
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