Abstract
Copaifera spp. are Amazonian species widely studied and whose oleoresins are used by local people for various medicinal purposes. However, a detailed study of the activity of the main phytochemical components of these oleoresins remains to be done. Here, we studied the cytotoxicity and in vitro anti-inflammatory effects of six diterpene acids: copalic, 3-hydroxy-copalic, 3-acetoxy-copalic, hardwickiic, kolavic-15-metyl ester, and kaurenoic, isolated from the oleoresins of Copaifera spp. The diterpenes did not show cytotoxicity in normal cell lines, nor did they show significant changes in viability of tumoral line cells. The 3-hydroxy-copalic was able to inhibit the enzyme tyrosinase (64% ± 1.5%) at 250 µM. The kolavic-15-metyl ester at 200 µM showed high inhibitory effect on lipoxygenase (89.5% ± 1.2%). Among the diterpenes tested, only kaurenoic and copalic acids showed significant hemolytic activities with 61.7% and 38.4% at 100 µM, respectively. In addition, it was observed that only the copalic acid (98.5% ± 1.3%) and hardwickiic acid (92.7% ± 4.9%) at 100 mM inhibited nitric oxide production in macrophages activated by lipopolysaccharide. In this assay, the diterpenes did not inhibit tumor necrosis factor-α production. The acids inhibited the production of IL-6, 3-acetoxy-copalic (23.8% ± 8.2%), kaurenoic (11.2% ± 5.7%), kolavic-15-methyl ester (17.3% ± 4.2%), and copalic (4.2% ± 1.8%), respectively, at 25 µM. The kaurenoic, 3-acetoxy-copalic and copalic acids increased IL-10 production. This study may provide a basis for future studies on the therapeutic role of diterpenic acids in treating acute injuries such as inflammation or skin disorders.
Highlights
Copaifera species, known in Brazil as “copaíbeiras” or “copaíba”, are Amazonian plants best known and used by traditional Amazonian people for the pharmacological activity of the oleoresins that they contain
We evaluated the capacity of six diterpenic acids to interfere with the murine fibroblast 3T3-L1, human lymphocytes, and J774 murine macrophage viability
Our results showed that the diterpenic acids 3-acetoxy-copalic (23.8% ± 8.2%), kaurenoic (11.2% ± 5.7%), kolavic-15-methyl ester (17.3% ± 4.2%), and copalic (4.2% ± 1.9%) at 50 mM inhibited the production of Interleukin 6 (IL-6)
Summary
Known in Brazil as “copaíbeiras” or “copaíba”, are Amazonian plants best known and used by traditional Amazonian people for the pharmacological activity of the oleoresins that they contain. The species of the Copaifera genus are among the most studied in the world, due to their economic and ecological importance. Copaíba oleoresin is exuded from the tree trunks of certain. Copaifera species and has been demonstrated to be primarily composed of sesquiterpenes and diterpenes. The oleoresin has widespread cosmetic and medicinal purposes due to its emollient, bactericide, anti-inflammatory, and anti-melasma properties [1,2]. Ten species found in Brazil have been studied for their oleoresin, which has resulted in more than 100 sesquiterpenes and 40 diterpenes being identified [2,3]. Few studies have isolated and described their biological activities
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