ABSTRACT
The anti-inflammatory and antiproliferative activities of 4ß-cinnamoyloxy,1ß,3α-dihydroxyeudesm-7,8-ene (1) and of three derivatives, namely diacetate (2), hydrogenate (3) and diacetate hydrogenate (4) were evaluated. All derivatives exert an anti-inflammatory effect significantly lower than that exerted by 1. Otherwise, both the lead compound and 2-4 showed a comparable antiproliferative activity on human tumor cell lines. The investigation of the mechanism of action accountable for cytotoxicity highlighted the capacity to impair mitochondrial functions through two different pathways, depending on chemical structure. In particular, the lead compound 1 and derivative 3 are able to induce mitochondrial permeability transition, while derivatives 2 and 4 inhibit Complex II in the respiratory chain.
Subject(s)
Anti-Inflammatory Agents/pharmacology , Mitochondria/metabolism , Verbesina/chemistry , Humans , Molecular StructureABSTRACT
From Byrsonima crassifolia (L.) H.B.K. a tropical tree widely distributed in Mexico, Central and South America, which has been used medicinally since prehispanic times, we report here the antibacterial activities of organic extracts of roots and stems. The ethyl acetate of roots was the most active against Klebsiella pneumoniae, Pseudomonas aeruginosa, Salmonella typhi, Shigella flexneri, Staphylococcus aureus, Staphylococcus epididermis, Streptococcus pneumoniae and Micrococcus luteus.
Subject(s)
Anti-Bacterial Agents/pharmacology , Plant Extracts/pharmacology , Plants, Medicinal/chemistry , Bacteria/drug effects , Microbial Sensitivity TestsABSTRACT
Hypertension is a very widespread condition which is not strictly considered as an illness but if not countered, progressively causes damage to all tissues and loss in their functionality. For this reason the find of new antihypertensive agents is prominent and medicinal plants and their derivatives are valuable for the purpose. The genus Casimiroa (Rutaceae) includes plants from Central America and Mexico; among these, Casimiroa edulis Llave et Lex. and Casimiroa pubescens Ramirez are the most relevant species, even for their medicinal uses. The decoction of leaves and seeds is traditionally taken as a tea mainly to lower blood pressure. The object of this research was the study of vascular activity of coumarinic and flavonoid compounds isolated from seeds of Casimiroa spp. in comparison with Casimiroa edulis and Casimiroa pubescens extracts. The phenolic compounds isolated from Casimiroa were herniarin (Her), imperatorin (Imp), 8-geranyloxypsoralen (GOP) and 5,6,2',3',4'-pentamethoxyflavone (PMF). All these compounds induced vasorelaxation on rat arterial tissues although with different effectiveness. To study the cellular mechanisms of the vasorelaxation exhibited by imperatorin, we used selective inhibitors of different receptors and enzymes, such as atropine, pyrilamine, nifedipine, L-NAME and DETC. In a further step of this research, we evaluated the radical-scavenging activity of Casimiroa extracts and isolated compounds by means of DPPH assay. In general, we observed that the scavenging activities increased in a concentration-dependent manner for all substances. The phenolic compounds highlight a synergism of vasodilation and antioxidant activity which may be very useful in the management of cardiovascular diseases. Among the evaluated compounds, imperatorin shows a significant vasorelaxant activity even higher than acetylcholine and similar to nitrite, and also useful antiradical capabilities. All these properties suggest its possible role against hypertension and vasculopathies, even if in vivo studies are needed to determine the actual applications.
Subject(s)
Antihypertensive Agents/analysis , Casimiroa/chemistry , Free Radical Scavengers/analysis , Furocoumarins/pharmacology , Vasodilator Agents/analysis , Animals , Antihypertensive Agents/pharmacology , Drug Evaluation, Preclinical , Flavones/isolation & purification , Flavones/pharmacology , Furocoumarins/isolation & purification , Heterocyclic Compounds, 3-Ring/isolation & purification , Heterocyclic Compounds, 3-Ring/pharmacology , In Vitro Techniques , Male , Plant Extracts/chemistry , Plant Extracts/pharmacology , Rats, Wistar , Seeds/chemistry , Umbelliferones/isolation & purification , Umbelliferones/pharmacologyABSTRACT
From the aerial parts of Decatropis bicolor, heraclenin (1), seselin (2), psoralen (3), imperatorin (4), skimmianine (5), and heraclenol (6), were isolated. This is the first time that coumarin-like compounds are isolated from Decatropis genus. The anti-inflammatory properties of compounds 1-6 were examined against the ear edema in mice produced by TPA. The results suggest that the anti-inflammatory activity of each compound depends of its individual substitution on the aromatic ring rather than the coumarin skeleton itself.