ORTHOSIPHON ARISTATUS (Orthosiphonis folium DAB 9) was studied with regard to its phenolic constituents. Twenty compounds were isolated and identified on the basis of their spectral characteristics. The compounds included nine lipophilic flavones, two flavonol glycosides, and nine caffeic acid derivatives. The presence of the recently reported methylripariochromene A could not be confirmed. All compounds identified were quantified by HPLC. The caffeic acid derivatives including the major compounds rosmarinic acid and 2,3-dicaffeoyltartaric acid (67% of total identified phenolics) predominated over the flavones (33%) in an aqueous MeOH extract. The predominance of the caffeic acid derivatives was even more pronounced in a hot water extract (94.5% of total identified phenolics) that was comparable to a herbal tea.
Analysis of the tropical marine sponge Axinella carteri afforded six unusual alkaloids, including the new brominated guanidine derivative 3-bromo-hymenialdisine. The structure elucidation of the new alkaloid is described. The alkaloid patterns of sponges collected in Indonesia or in the Philippines were shown to be qualitatively identical suggesting de novo synthesis by the sponge or by endosymbiontic microorganisms rather than uptake by filterfeeding. All alkaloids were screened for insecticidal activity as well as for cytotoxicity. The guanidine alkaloids hymenialdisine and debromohymenialdisine exhibited insecticidal activity towards neonate larvae of the polyphagous pest insect Spodoptera littoralis (LD50s of 88 and 125 ppm, respectively), when incorporated into artificial diet and offered to the larvae in a chronic feeding bioassay. The remaining alkaloids, including the new compound, were inactive in this bioassay. Cytotoxicity was studied in vitro using L5178y mouse lymphoma cells. Debromohymenialdisine was again the most active compound (ED50 1.8 μg/ml) followed by hymenialdisine and 3-bromohymenialdisine, which were essentially equitoxic and exhibited ED50s of 3.9 μg/ml in both cases. The remaining alkaloids were inactive against this cell line
A phytochemical analysis of the leaves of Aglaia dasyclada collected in Yunnan Province (People's Republic of China) yielded five cyclopentabenzofurans (1-5) of the rocaglamide family that are common secondary metabolites of Aglaia species as well as four biogenetically related compounds of the aglain (7), aglaforbesin (8) and forbaglin (9, 10) types. In addition, the cinnamic acid amide dasyclamide (6), which is a putative biogenetic precursor of these compounds (7-10), was isolated. The structures of the new compounds (6-10) were assigned unambiguously from the combined use of 1D and 2D NMR spectroscopy and mass spectrometry.
Polo-like kinase 1 (Plk1) is over expressed in many types of human cancers, and has been implicated as an adverse prognostic marker for cancer patients. Plk1 is localized to its intracellular anchoring sites via its polo-box domain (PBD). The PBD of Plk1 has a crucial role in proper subcellular localization and mitotic functions of Plk1. Plk1 is the preferential target for inhibition of the mitotic processing therefore it can be chosen as drug target for the treatment of cancer. The aim of the study is to find plk1 inhibitor potential from naphthoquinone derivatives through binding free energy analysis into plk1 using molecular docking. We conducted docking simulation to naphthoquinone derivatives as ligands into plk1 as receptor. The 3D structure of plk1 was downloaded from PDB (Code ID:3THB). The structure of ligands and protein were prepared using ChemBioDrawUltra 12.0. Docking process, the interaction and binding of ligands-protein were done and visualized using software Molegro Virtual Docking.(MVD). The results showed no hydrogen bonding and electrostatic interaction between compound NO11(modified naphthoquinone) with Plk1, but this compound have more steric interaction with Phe 133, Asp 194, Glu 101, Lys 82, Cys 133 and Glu 140 of Plk1. Moldock scores of compound NO11, is-134.73 kcal/mol. It is predicted that compound NO11 has potency as lead compound to find a new anticancer candidates for possible therapeutic agents.
Cantigi is an endemic plant of sub-alpine area of Mount Tangkuban Parahu in Bandung, Indonesia. Previous study showed ethanol extract of young red leaves had antioxidant activity, however no information on this activity if changed into nanoparticles. The purpose of this study was to determine the effects of gelatin and glutaraldehyde concentrations on the characteristics of Cantigi extract loaded gelatin nanoparticles and to evaluate the antioxidant activity of nanoparticles. Cantigi leaves were extracted by maceration using n-hexane, ethyl acetate, and ethanol 96%. The ethanol extract was dried, made into nanoparticles by varying gelatin (0.1; 0.2; and 0.3 g) and glutaraldehyde (0.1; 0.2; and 0.3 mL) amounts, and conducted at 500 rpm and 40 °C for 3 hours. Nanoparticles were evaluated for particle size, zeta potential, morphology, and antioxidant activity. Nanoparticles with glutaraldehyde amount variation had particle sizes (PS) of 105.9±26.2; 37.1±8.7; and 32.5±7.4 nm; polydispersity indeces (PI) of 0.508; 0.717; and 0.563; zeta potential values (ZPV) of 0.55; 0.89; and 0.78 mV; and antioxidant activities (IC50) of 56.15±0.16; 53.67±0.10; and 51.57±0.39 ppm, respectively. Then, nanoparticles with gelatin amounts variation had PS of 22.5±5.1; 37.1±8.7; and 83.3±21 nm; PI of 0.604; 0.717; 0.326; ZPV of 1.27; 0.89; 0.18 mV; and antioxidant activities of 51.58±0.19; 53.67±0.12; and 55.46±0.04 ppm, respectively. Nanoparticle morphology was spherical. Cantigi leaf extract can be made into gelatin nanoparticles; the smaller the concentration of the polymer used and higher the concentration of the glutaraldehyde, the smaller the resulted particle size and increased antioxidant activity. Antioxidant activities of nanoparticles was lower than those of the extract (IC50 16.84±0.30 ppm).
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