Rhododendron album Blume (RA) has traditionally been used as an herbal medicine and is considered to have anti-inflammatory properties. In the present study, we screened RA extracts with anti-inflammatory properties. The biological effects of an RA methanol extract (RAME) on inflammation were investigated in lipopolysaccharide (LPS)-stimulated mouse RAW264.7 cells. We investigated the effects of RAME on the production of nitric oxide (NO) and prostaglandin E2 (PGE2) in LPS-stimulated RAW264.7 cells. To explore the anti-inflammatory mechanisms of RAME, we measured the mRNA and protein expression of pro-inflammatory mediators induced by RAME in the LPS-stimulated RAW264.7 cells by RT-PCR and western blot analysis, respectively. RAME significantly inhibited the production of NO, PGE2, interleukin (IL)-6, IL-1β and tumor necrosis factor (TNF)-α in the LPS-stimulated RAW264.7 cells. It also suppressed the mRNA and protein expression of inducible NO synthase (iNOS), cyclooxygenase-2 (COX-2) and mitogen-activated protein kinases (MAPKs) with a concomitant decrease in the nuclear translocation of nuclear factor-κB (NF-κB) in the LPS-stimulated RAW264.7 cells. These results indicate that RAME inhibits LPS-induced inflammatory responses. These effects were considered to be strongly associated with the suppression of NF-κB activation. We therefore suggest that RAME may be prove to be an effective therapeutic agent for the treatment of inflammatory diseases.

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.

Background: The quality of a medicinal plant is influenced by agronomic conditions and harvesting time. Objective: This study aimed to evaluate the effect of planting method (openair (OA) and shedding house (SH)) and harvesting time (2, 4, 6 months) of Lampeni (Ardisia humilis Vahl.) toward the inhibitory activity of alpha-glucosidase. Methods: The Lampeni seedling were placed under controlled light conditions (SH) and on direct sun exposure (OA). Harvesting of the leaves was carried out at the age of 2, 4, and 6 months after plantation (2m, 4m, and 6m). Each leaves dry powder was refluxed with methanol 70% and followed by liquid-liquid partition using n-hexane, ethyl acetate (EtOAc), and water. All samples were evaluated toward inhibition of the alpha-glucosidase enzyme in vitro. Total phenol levels were determined using Folin-Ciocalteu reagent. Results: The results showed that EtOAc fractions of both plantation techniques exhibited the highest inhibition of alpha-glucosidase. The highest activity was demonstrated by the 4m-OA-EtOAc fraction (IC 50 , 93.50 ppm) and followed by the 6m-OA-EtOAc fraction (IC 50 , 98.13 ppm). Based on the kinetic study, the inhibition type of the two most active samples were categorized as a non-competitive type. Total phenolic contents were decreased in the following order: 6m-SH-EtOAc > 4m-OA-EtOAc > 6m-OA-EtOAc > 4m-SH-EtOAc fraction. It was shown that there was no positive correlation between the strength of inhibition with total phenolic content. Conclusions: This study concluded that Lampeni at open-air plantation harvested on fourth months demonstrated the highest alpha-glucosidase inhibitory activity, although there was no positive correlation between the inhibition activity and phenolic content.

ABSTRAK Sambiloto (Andrographis paniculata) banyak digunakan untuk mengobati berbagai penyakit di Indonesia dan negara-negara Asia lainnya. Dalam studi ini, ekstrak metanol dan etanol sambiloto yang diperoleh dari B2PTO Tawangmangu telah diuji terhadap sel lini kanker payudara T47D dan MCF-7 dan sel lini normal fibroblast HFL-1 menggunakan reaksi enzimatik 3-(4,5-dimethylthiazoyl-2-yl) 2,5-diphenyltetrazoliumbromide (MTT ABSTRACTSambiloto (Andrographis paniculata) is widely used as medicine to treat various diseases in Indonesia and other Asian countries. In this study, methanolic and ethanolic extracts of sambiloto collected from B2PTO Tawangmangu have been tested againts breast cancer cell lines of T47D and MCF-7 and normal fibroblast cell line of HFL-1 using enzymatic reaction of 3-(4,5-dimethylthiazoyl-2-yl) 2,5-diphenyltetrazoliumbromide (MTT). In vitro assay performed on normal fibroblast of HFL-1 cell line showed that 50 ppm of methanolic extract of sambiloto did not inhibit cell growth. However, methanolic and ethanolic extracts of sambiloto gave relatively low of IC 50 on breast cancer cell lines which were 111 ppm and 122 ppm on the MCF-7 cell lines and 70 ppm and 197 ppm on the T47D cell lines, respectively. In addition, the mixture of sambiloto extract containing 25% of Thyponium divaricatum and Anredera cordifolia extracts confered greater growth inhibition on breast cancer cell line of MCF-7, where IC 50 values were 68 ppm and 34 ppm, respectively. In conclusion, the total methanolic or ethanolic extract of sambiloto collected from Tawangmangu has potency as a source of anti-cancer compounds and needs further study.