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.

No abstract

Two new isopimarane diterpenes, 1α‐hydroxy‐14α‐methoxyisopimara‐8(9),15‐diene (7) and 1α,14α‐dihydroxyisopimara‐8(9),15‐diene (9) and eight known isopimarane diterpenes including (‐)‐sandaracopimaradiene (1), 6β‐acetoxysandaracopimaradiene‐9α‐ol (2), sandaracopimaradiene‐7β,9α‐diol (3), sandaracopimaradiene‐1α,9α‐diol (4), 6β‐acetoxysandaracopimaradiene‐9α‐ol‐1‐one (5), 6β‐acetoxysandaracopimaradiene‐1α,9α‐diol (6), 6β,14α‐dihydroxyisopimara‐8(9),15‐diene (8), and 6β,14β‐dihydroxyisopimara‐8(9),15‐diene (10) were isolated from hexane fraction of Kaempferia galanga ethanol extract. Compounds 5, 6, 8, and 9 exerted the good anti‐inflammatory effect on lipopolysaccharide‐stimulated nitric oxide production from RAW264.7 cells with IC50 of 11.2, 7.7, 14.3, and 12.1 μM, respectively. These four compounds inhibited nitric oxide synthase (iNOS) mRNA expression. Compounds 5 and 6 also suppressed cyclooxygenase 2 (COX‐2) mRNA expression; in addition, compound 6 had mild inhibitory effect on TNF‐α mRNA. Among these compounds, 5 dramatically inhibited iNOS and COX‐2 mRNA expression. The influential structures were proposed to be oxygen substitute at C‐1, C‐6, and α‐OH at C‐14.

Curcuma zedoaroides, a Zingiberaceae species, has been used for snake bite antidote and wound care in Thailand. Seven compounds were isolated from the bioactive chloroform extract consisted of one new guaiane sesquiterpene lactone, 5-epiphaeocaulisin A (4) and one new diarylheptanoid, 1,2,3,5-tetrahydroxy-1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl) heptane (7), together with five known guaiane-type sesquiterpene lactones including gweicurculactone (1), zedoalactone B (2), phaeocaulisin C (3), zedoalactone H (5), and zedoalactone E (6). The antiinflammation was investigated on NO and TNF-α production using RAW264.7 cells. In addition, the expressions of genes involved in inflammation including iNOS, COX-2, and TNF-α were assessed. The results found that Compounds 1-7 presented their antiinflammation against NO production. The most potential effects were demonstrated on Compounds 1 and 7 with IC of 27.3 and 32.6 μM, respectively. Although, Compounds 1 and 7 did not inhibit TNF-α production, their suppression on iNOS and COX-2 mRNA expression were revealed. These results support the ability of chloroform fraction, Compounds 1 and 7 on antiinflammation, whereas others exhibited moderate and mild effect.

Context: Acquired immunodeficiency syndrome (AIDS) is a serious health problem worldwide.