ABSTRACT
Cisplatin remains the most widely used chemotherapeutic agent in cancer treatment; however, its inherent drawbacks have fueled the development of novel metalloanticancer drugs. In this study, two novel Cu(II) complexes (Cu1 and Cu2) were designed and synthesized. Notably, these Cu(II) complexes showed higher cytotoxicity against HL-7402 cells than cisplatin. Moreover, Cu(II) complexes significantly inhibited liver cancer growth in a xenograft model. A mechanism study revealed that the Cu(II) complexes reduced the mitochondrial membrane potential of cancer cells, produced excessive reactive oxygen species (ROS), induced mitochondrial DNA (mtDNA) damage, and ultimately facilitated cancer cell apoptosis.
Subject(s)
Antineoplastic Agents , Apoptosis , Coordination Complexes , Copper , DNA Damage , DNA, Mitochondrial , Liver Neoplasms , Mitochondria , Reactive Oxygen Species , Humans , Copper/chemistry , Copper/pharmacology , Apoptosis/drug effects , Liver Neoplasms/drug therapy , Liver Neoplasms/pathology , Liver Neoplasms/metabolism , Animals , DNA Damage/drug effects , Coordination Complexes/pharmacology , Coordination Complexes/chemistry , Coordination Complexes/chemical synthesis , Antineoplastic Agents/pharmacology , Antineoplastic Agents/chemistry , Antineoplastic Agents/chemical synthesis , Mice , Mitochondria/drug effects , Mitochondria/metabolism , DNA, Mitochondrial/metabolism , DNA, Mitochondrial/genetics , Reactive Oxygen Species/metabolism , Membrane Potential, Mitochondrial/drug effects , Cell Line, Tumor , Hydrazones/pharmacology , Hydrazones/chemistry , Hydrazones/chemical synthesis , Xenograft Model Antitumor Assays , Mice, Nude , Mice, Inbred BALB CABSTRACT
Phytochemical investigation on the aerial parts of Gnetum parvifolium led to the isolation of 15 new and eight known structurally diverse stilbenes. The isolated compounds comprised (E)- or (Z)-stilbene (1-6, 15-20), dihydrostilbene (21), phenylbenzofuran (7, 8, 22), benzylated stilbene (9-11), benzylated stilbene dimer (12), and nitrogen-containing stilbene (13a, 13b, 14) types. The structures of the new compounds (1-12, 13a, 13b, 14) were established through spectroscopic analyses and experimental and calculated ECD data. Compound 12 is the first stilbene dimer connected through a benzyl group. In the anti-neuroinflammatory activity assay, compounds 4, 5, 9-11, 13b, and 16-21 displayed significant inhibitory effects against LPS-induced NO release in BV-2 microglial cells, with IC50 values of 0.35-16.1 µM. Compound 10 had the most potent activity (IC50 = 0.35 µM), and the further research indicated that it could decrease the mRNA levels of iNOS, IL-1ß, IL-6, and TNF-α in a dose-dependent manner.
Subject(s)
Gnetum , Stilbenes , Molecular Structure , Gnetum/chemistry , Stilbenes/pharmacology , Stilbenes/chemistryABSTRACT
Ventilago leiocarpa Benth. is an important medicinal and edible plant. The complete chloroplast genome of V. leiocarpa Benth. was assembled and annotated. In this study, the chloroplast genome of V. leiocarpa Benth. was a circular form of 161,880 bp in length. The genome presented a typical quadripartite structure consisting of a pair of inverted repeats (IRa and IRb) of 26,357 bp separated by a large single copy (LSC) region of 90,056 bp and a small single copy (SSC) region of 19,129 bp. The genome contained a set of 127 genes, including 82 protein-coding genes, 37 tRNA genes, and 8 rRNA genes. Phylogenetic analysis showed that V. leiocarpa Benth. closely related to Rhamnus taquetii, which beyond to Rhamnaceae.
ABSTRACT
The vibrational dynamics of water around serine was investigated by using Raman spectroscopy and inelastic incoherent neutron scattering. Experiments with serine in deuterium oxide were performed to assist the assignment. The study shows that for the serine, the exchange of protons-deuterons on the active -NH3+ and -OH groups were relatively easy, whereas there were hardly any exchanged on the -CH or -CH2- groups. The main features of the spectra for hydrated samples (versus the dry samples) were altered considerably; new sharp peaks in the measured spectra appeared, indicating that the hydrogen bonding between water and serine had disturbed the structure of the serine molecule.
