Abstract
The present study reports a bioassay-guided isolation of β-caryophyllene from the essential oil of Aquilaria crassna. The structure of β-caryophyllene was confirmed using FT-IR, NMR and MS. The antimicrobial effect of β-caryophyllene was examined using human pathogenic bacterial and fungal strains. Its anti-oxidant properties were evaluated by DPPH and FRAP scavenging assays. The cytotoxicity of β-caryophyllene was tested against seven human cancer cell lines. The corresponding selectivity index was determined by testing its cytotoxicity on normal cells. The effects of β-caryophyllene were studied on a series of in vitro antitumor-promoting assays using colon cancer cells. Results showed that β-caryophyllene demonstrated selective antibacterial activity against S. aureus (MIC 3 ± 1.0 µM) and more pronounced anti-fungal activity than kanamycin. β-Caryophyllene also displayed strong antioxidant effects. Additionally, β-caryophyllene exhibited selective anti-proliferative effects against colorectal cancer cells (IC50 19 µM). The results also showed that β-caryophyllene induces apoptosis via nuclear condensation and fragmentation pathways including disruption of mitochondrial membrane potential. Further, β-caryophyllene demonstrated potent inhibition against clonogenicity, migration, invasion and spheroid formation in colon cancer cells. These results prompt us to state that β-caryophyllene is the active principle responsible for the selective anticancer and antimicrobial activities of A. crassnia. β-Caryophyllene has great potential to be further developed as a promising chemotherapeutic agent against colorectal malignancies.
Highlights
Aquilaria crassna (Thymelaeaceae) has been used in diverse Chinese and Southeast Asian traditional medicine systems to treat infectious and inflammatory diseases, arthritis and cardiac disorders
A number of studies have confirmed that the essential oil is an active component of A. crassna stem bark [18,19], but very little is known about the active principle(s) responsible for the pharmacological properties of the plant
The present study clearly demonstrated that the essential oil extracted from A. crassna using the hydrodistillation method showed remarkable antiproliferative properties against human colorectal cancer cells
Summary
Aquilaria crassna (Thymelaeaceae) has been used in diverse Chinese and Southeast Asian traditional medicine systems to treat infectious and inflammatory diseases, arthritis and cardiac disorders. The plant, locally known in Indonesia as gaharu or agarwood, contains biologically active essential oils which have been used for various medicinal purposes by a number of civilizations due to their phytochemically rich and pharmacologically active aromatic compounds [1]. It has been widely used by Arabs and Japanese to treat digestive, neurodegenerative and sedative disorders [2,3]. An essential oil mixture from A. crassna bark was subjected to bioactivity-guided fractionation and repeated column chromatography to afford β-caryophyllene as an active principle. To elucidate the mechanism of action and to characterize the mode of cytotoxicity induced by β-caryophyllene in human colorectal cancer cells, a series of in vitro assays, such as Hoechst 33342, rhodamine 123, colony formation, migration and invasion assays were performed
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