Extracted compounds from Caesalpinia sappan L. were examined for the inhibitory activity against NO, PGE2 , and TNF-α productions and on associated transcription levels using RAW264.7 cells. They were also tested for their effects on wound healing using fibroblast L929 cells. Among the compounds tested, brazilin (8) was the most effective against lipopolysaccharide (LPS)-induced NO production in RAW264.7 cells with an IC50 value of 10.3 μM, followed by sappanchalcone (2, 31.0 μM). Brazilin (8) also inhibited PGE2 and TNF-α production with IC50 values of 12.6 and 87.2 μM, respectively. The antiinflammatory mechanism of brazilin involved down regulation of the mRNA expressions of the iNOS, COX-2, and TNF-α genes in a dose-dependent manner. An ethanol (EtOH) extract of C. sappan significantly increased fibroblast proliferation, fibroblast migration, and collagen production, whereas brazilin (8) only stimulated fibroblast migration. In addition, the EtOH extract showed no acute toxicity in mice, and it was therefore safe to make use of its potent antiinflammatory and wound healing activities. Brazilin was mainly responsible for its antiinflammatory effect through its ability to inhibit the production of NO, PGE2 , and TNF-α. This study supports the traditional use of C. sappan for treatment of inflammatory-related diseases.

The 2 h infusions of imipenem resulted in greater t > MICs than the 0.5 h infusion. For infections caused by pathogens with high MICs, a 2 h infusion of 1 g of imipenem every 6 h can provide plasma concentrations above the MIC of 4 mg/L for 60% of a 6 h interval.

Background Dioscorea bulbifera L. (Dioscoreaceae) has been traditionally used in Thai folk medicine as a diuretic and anthelmintic, for longevity preparations, and for wound and inflammation treatment. This plant is also commonly used in traditional Indian and Chinese medicines in the treatment of sore throat, gastric cancer, rectal carcinoma and goiters. However, the wound healing effects of the active compounds in this plant have not been investigated. Objective This study aimed to identify compounds responsible for the wound healing activity of D. bulbifera and determine their potential anti-inflammatory and antioxidant activities. Methods Crude extracts of D. bulbifera bulbils, their derived fractions and eleven purified compounds were tested for anti-inflammatory activity against LPS-induced NO production in RAW264.7 macrophages. The wound healing effects were evaluated via cell proliferation and migration assays using human dermal fibroblasts (HDFs), and the antioxidant effects were determined using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and hydroxyl radical (•OH) scavenging activity assays. Results 15,16-Epoxy-6α-O-acetyl-8β-hydroxy-19-nor-clero-13(16),14-diene-17,12;18,2-diolide (2), (+)-catechin (5), quercetin (6) and myricetin (11) exhibited significantly potent wound healing effects and promoted marked cell proliferation, resulting in % viabilities of 107.4–137.6, 121.1–151.9, 98.0–131.9, 90.9–115.9, respectively. Among them, (+)-catechin produced the highest % cell migration, resulting in 100.0% wound closure sooner (at day 2) than the other compounds. In addition, 1 μg/ml (+)-catechin significantly increased fibroblast migration by 2.4-fold compared to that in the control after 24 h. Regarding anti-inflammatory properties, kaempferol (7) and quercetin (6) decreased (p < 0.005) NO production, with IC50 values of 46.6 and 56.2 μM, respectively. In addition, the crude extracts, solvent fractions and flavonoid compounds were also found to possess marked antioxidant activity in both DPPH and •OH radical scavenging assays. Conclusions These findings provide more evidence to support the traditional use of D. bulbifera for the treatment of wounds and inflammation.

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Betula alnoides is a medicinal plant in Thai traditional longevity preparations. The crude extracts of this plant possess various biological activities. However, the isolated compounds from this plant have no reports of anti-HIV-1 integrase (IN) activity. Therefore, the present study aims to investigate the anti-HIV-1 integrase and anti-inflammatory effects of isolated compounds from this plant and predict the interaction of compounds with integrase active sites. From the bioassay-guided fractionation of the ethanol extract of B. alnoides stems using chromatographic techniques, five pentacyclic triterpenoid compounds were obtained. They are betulinic acid (1), betulin (2), lupeol (3), oleanolic acid (4), and ursolic acid (5). Compound 2 exhibited the most potent inhibitory activity against HIV-1 IN, with an IC50 value of 17.7 μM. Potential interactions of compounds with IN active sites were investigated using computational docking. The results indicated that active compounds interacted with Asp64, a residue participating in 3′-processing, and Thr66, His67, and Lys159, residues participating in strand-transfer reactions of the integration process. Regarding anti-inflammatory activity, all compounds exerted significant inhibitory effects on LPS-induced nitric oxide production (IC50 < 68.7 μM). Thus, this research provides additional scientific support for the use of B. alnoides in traditional medicine for the treatment of HIV patients.

The inhibitory activity of extract and compounds isolated from the roots of Cratoxylum formosum ssp. pruniflorum against nitric oxide (NO) was evaluated using RAW264.7 cells. Isolation of the CH2Cl2 extract of C. formosum ssp. pruniflorum roots afforded ten known xanthones including six tri-oxygenated xanthones (1-6) and four tetra-oxygenated xanthones (7-10), respectively. Compound 7 showed the highest inhibitory activity against NO release with an IC50 value of 3.9 μM, followed by compound 8 with an IC50 value of 4.3 μM, respectively. In order to understand the mechanism of this anti-inflammatory activity, the transcriptional level of 7 was found to down regulate mRNA expressions of iNOS and COX-2 in dose-dependent manners, whereas 8 inhibited only iNOS mRNA expression but did not affect on that of COX-2 gene. Xanthones might be the main anti-inflammatory components in C. formosum ssp. pruniflorum.