Conformational Analysis and Biological Activity of Leptocarpin and Leptocarpin Acetate

Abstract

Letters a group of PAHs are present in the plant extract and contributed to the light-mediated antiviral activity. We believe that the source of the PAHs was not from contamination in the purification procedure. With separation and analytical techniques capable of purifying trace components, it is more of a possibility that impurities from materials used in the processing can be accumj.ilated and be found in an identifiable quantity. The major solvent used in this procedure consisted of a mixture of hexanes. The impurities remaining from the evaporation of four liters of hexanes under reduced pressure were submitted for NMR and the spectrum obtained was not complex enough to indicate the presence of PAHs. Polycycic aromatic hydrocarbons have been found in foliage as well as in crops (6). PAils are generated by the incomplete combustion of fossil fuels and are found throughout the environment. If the occurrence of 245-261.

Leptocarpin Suppresses Proliferation, Migration, and Invasion of Human Osteosarcoma by Targeting Type-1 Insulin-Like Growth Factor Receptor (IGF-1R)

“…LTC is a sesquiterpene lactone, a major component of the Asteraceae family [ 25 ]. According to Martinez et al [ 12 ], LTC exhibits high cytotoxicity on human liver adenocarcinoma (SK-Hep-1) and HeLa cells. Therefore, LTC has anti-cancer and anti-tumor effects [ 26 – 28 ].…”

“…Asteraceae, which produces many bioactive compounds such as polyacetylenes, diterpenes, and sesquiterpene lactones [ 8 ], expresses various clinical activities, including anti-tumor, anti-ulcer, anti-inflammatory, neurocytotoxic, and cardiotonic activities [ 9 , 10 ], as well as the ability to influence critical biological processes such as cell signaling, cell proliferation, apoptosis, and mitochondrial metabolism [ 11 ]. Leptocarpin (LTC) is the one of the major components of Leptocarpha rivularis , which belongs to the Asteraceae family and was been widely used as a folk remedy [ 12 – 14 ]. In our study, LTC was used as an anti-tumor drug to treat MG63 cells.…”

Enhancement of Cytotoxic Activity by Encapsulation in Pluronic Polymer Micelles: Leptocarpha Rivularis Extracts Against Human Cancer Cell Lines

“…As discussed above, SQL exhibit cytotoxic activity against various cancer cell lines, and therefore the activity of these extracts must be related to their SQL content. In previous work, it has been found that L. rivularis contains a high percentage of SQL, and leptocarpin amounts to approximately 0.02% of the EA extract whereas the content of LTC in the ET extract is even lower 23,24 . To explain the origin of extract's activities the values of IC 50 obtained for EA extract are compared with reported LTC cytotoxicity (last column in Table 1) and discussed as a function of LTC content.…”

“…Thus, a comparison of IC 50 values obtained for extracts with those reported for LTC (last column in Table 1) suggest that the activity of extracts is due to LTC and other secondary -secbutyl leptocarpin; rivularin; 8 -angeloyl-1 ,3 -dihydroxy-4,10-dimethyl-11 (13) methylen-4Z,9Z-dienheliangol-6,12-olide (4); and 8 -angeloyl-1 ,3dihydroxy-4-methyl-11 (13) 10 14-dimethylen-4Z-enheliangol-6,12-olide (5). All these lactones were isolated from the EA extract, except for 4 and 5 that have been not isolated due to the low percentage in which they are present 23,24,47 .…”

“…This plant has been used as folk medicine by the Mapuche ethnia for the treatment of gastric ulcers. Phytochemical studies have shown that L. rivularis contains a high percentage of SQL, highlighting leptocarpine (LTC) as the main component 23,24 . LTC has a similar structure to other active SQL (see Figure 1), and it is highly cytotoxic, induces apoptosis, and acts as an efficient inhibitor of NF-B 23,25 .…”