Five fractions separated from Nannochloropsis oculata using solvent-solvent partition chromatography of 80% methanolic extract of N. oculata (NOM) followed by the open silica column chromatography of its hexane fraction (NOMH) for the anti-inflammatory on RAW 264.7 cells and anti-cancer activities on HL-60, A-549, HEP-3B, HCT-116, and SW-480 cancer cells. All the five fractions showed potential anti-inflammatory activities against lipo polysaccharide-stimulated RAW 264.7 macrophages cells with IC 50 values less than 6.25 µg mL-1. Moreover, 90% n-hexane column elution of NOMH (NOMH90) down-regulated lipopolysaccharide-stimulated protein levels of inducible nitric oxide synthase and cyclooxygenase-2. Furthermore, NOMH90 showed marked cytotoxic effect on the HL-60 cells with IC 50 value of 23.58 ± 0.09 µg mL-1. In addition, Hoechst 33342 cell permeable dye used to visualize the apoptosis nucleus and cell cycle analysis measured Sub-G1 DNA contents to confirm reduction of the cell viability in NOMH90 treated cells due to induction of apoptosis in HL60. These results are quite related to the phytosterol contents of the NOMH fractions and the results suggest N. oculata extracts might be useful as potential sources of natural anti-inflammatory and anti-cancer compounds. In conclusion, the sterol content in N. oculata might provide a promising role in future medicines in anti-inflammatory and anti-cancer.
Ru(II)-catalyzed enantioselective C−H activation/hydroarylation has been developed for the first time, allowing for highly enantioselective synthesis of indoline derivatives via catalytic C−H activation. Commercially available Ru(II) arene complexes and chiral α-methylamines were employed as highly enantioselective catalysts. Based on a sterically rigidified chiral transient directing group, multisubstituted indolines were produced in up to 92% yield with 96% ee. Further transformation of the resulting 4-formylindoline enables access to an optically active tricyclic compound that is of potential biological and pharmaceutical interest.
Catalytic [2 + 2 + 2] cycloaddition with three double bond systems has been developed for construction of hexahydropyrimidine and 1,3-diamine derivatives.
Developing
tandem multiple C–H substitution reactions of
simple alkenes provides rapid access to structurally complex unsaturated
building blocks. Amidomethylative reactions that reserve CC
double bonds have been composed sequentially for tandem catalytic
substitutions around the CC bonds of alkenes. As a proof-of-concept
demonstration, tandem catalytic amidomethylative processes, which
effectively form multiple C–C bonds, have been developed to
directly and selectively transform α-substituted styrenes into
unsaturated N-heterocycles. Using Fe(OTf)3 as the sole catalyst, the operationally simple protocols employ
bench-stable bisamidomethane as the sole reagent to produce hexahydropyrimidines
and 1,2,3,6-tetrahydropyridine derivatives. Moreover, the practical
catalytic processes constituted facile two-step pathways, from simple
α-substituted styrenes, to access unsaturated 1,3-diamine and
bispidine derivatives.
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