Anxiolytic effect of the heartwood of Haematoxylum campechianum L. and sappanchalcone in an in vivo model in mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Haematoxylum campechianum L., is a well-known plant in the southeast region of Mexico, where it is named as "palo tinto" or "palo de Campeche", in English there are vernacular names such as "redwood", "bloodwood tree" or "campeachy wood". Traditional medicine refers its use for the treatment of different disorders including depression. AIM OF THE STUDY: Considering the traditional use of this plant for the alleviation of depression, the aim of this study was the evaluation of the anxiolytic effect of the methanolic and hydroalcoholic extracts from the heartwood of Haematoxylum campechianum L., and the sappanchalchone (Sapp). Additionally, it is presented the characterization of the new compound 4-hydroxyhematoxylol (2) isolated from the hydroalcoholic extract. MATERIAL AND METHODS: The anxiolytic effect of the extracts and Sapp was evaluated by using the Elevated Plus Maze (EPM) additionally the sedative effect was assessed with the Open Field Test (OFT). The chemical characterization of Sapp and 2 was performing by 1D and 2D NMR experiments. RESULTS: The EPM test showed that the administration of the plant extracts increased the percentage of time spent in open arms (76.32 ± 6.35 and 66.68 ± 20.64%, respectively for the methanolic and hydroalcoholic extracts), whereas the administration of Sapp increased the percentage of time spent in open arms by 60.07 ± 14.28%, these results are similar to Diazepam (DZP, positive control) which caused an increment of 74.06 ± 23.42%. For the OFT, all of the doses evaluated for both extracts and Sapp diminished the number of rearing (R) and total corssing (TC) behavior in a similar way to the positive control (DZO) and statistically different with respect to the vehicle. CONCLUSION: The results obtained showed that the polar extracts from the heartwood of Haematoxylum campechianum L. possess both anxiolytic and sedative effect and that the chalcone-type compound Sapp, isolated from the methanolic extract, is partially responsible of these activities.

Homoisoflavonoids and Chalcones Isolated from Haematoxylum campechianum L., with Spasmolytic Activity.

Haematoxylum campechianum is a medicinal plant employed as an astringent to purify the blood and to treat stomach problems such as diarrhea and dysentery. A bio-guided chemical fractionation of the methanolic extract obtained from this plant allowed for the isolation of five compounds: two chalcones known as sappanchalcone (1); 3-deoxysappanchalcone (2); three homoisoflavonoids known as hematoxylol A (3); 4-O-methylhematoxylol (4); and, hematoxin (5). The spasmolytic activity was determined in an in vitro model (electrically induced contractions of guinea pig ileum), and allowed to demonstrate that the methanolic extract (EC50 = 62.11 ± 3.23) fractions HcF7 (EC50 = 61.75 ± 3.55) and HcF9 (EC50 = 125.5 ± 10.65) and compounds 1 (EC50 = 16.06 ± 2.15) and 2 (EC50 = 25.37 ± 3.47) of Haematoxylum campechianum present significant relaxing activity as compared to papaverine (EC50 = 20.08 ± 2.0) as a positive control.