New ent-kaurene and germacrene derivatives from Mesona procumbens Hemseley and their biological activity.

Mesona procumbens Hemseley is a well-known traditional herbal medicine used for heat-related ailments. In Taiwan, boiled extracts of M. procumbens are also used as desserts called grass jelly. In this study, the hexane extract from 75% EtOH of M. procumbens showed potent activities on inhibition of E. coli ß-glucuronidase (eßG) and NO production and cytotoxicity against MCF-7 and HepG2 cancer cell lines. Furthermore, using various flash columns and HPLC chromatography on the bioactive layer led to the isolation of twelve compounds (1-12), including a new ent-kaurene, mesokaurol A (1), and a new germacrene derivative, mesogermapene A (2). Their structures were elucidated by extensive spectroscopic analyses, especially 2 D NMR and mass data. Biological assays showed that compound 9 (linolenic acid) had specific activity on inhibition of eßG (68.27%) at 100 µg/mL but was non-inhibitory to human ß-glucuronidase. Compound 1 possessed significant cytotoxicity against MCF-7 (EC50 = 9.76 µM) and HepG2 (EC50 = 8.64 µM) cancer cell lines.

4-O-Caffeoylquinic acid as an antioxidant marker for mulberry leaves rich in phenolic compounds.

Mulberry (Morus alba L.) leaves are widely used as herbal tea to prevent heat stroke. Potential chemical markers of the antioxidant properties and its correlation with harvesting times and leaf location were explored in this study. A 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical-scavenging assay guided isolation of mulberry leaves extract provided five phenolic compounds: 5-O-caffeoylquinic acid (1), 4-O-caffeoylquinic acid (2), gastrodin (3), isoquercetin (4) and rutin (5). The 50% radical-scavenging concentrations (SC50) of these compounds were 32.76 ± 0.27, 11.41 ± 0.48, 404.30 ± 4.92, 10.63 ± 0.96, and 10.57 ± 0.61 µg/mL, respectively. Chromatographic fingerprinting allowed content analysis of 1-5 in samples over a 12-month period. Compounds 1-5 were abundance in apical leaves (0-10 cm) in January and February at temperatures < 20 °C. Contents of 2 and 5 were highest in these months and were strongly correlated to the antioxidant property. Therefore, we suggested that the mulberry leaves harvested during January and February have high yield of 4-O-caffeoylquinic acid and this compound can be used as antioxidative marker in mulberry leaves.

Effects of Dang-Gui-Bu-Xue-Tang, an herbal decoction, on iron uptake in iron-deficient anemia.

Dang-Gui-Bu-Xue-Tang (DBT), a combination of Angelicae Sinensis Radix and Astragali Radix, is a widely used herbal decoction in traditional Chinese medicine primarily to promote or invigorate the "blood". In this study, we explored this ancient formulation and provide evidence of its blood-toning properties. We used the improvement iron uptake as promote or invigorate the "blood" indicator. Ferritin formation of Caco-2 cells in vitro assay and diet-induced anemia (DIA) in rat model were used to prove its improvement iron uptake and ameliorating effects. Finally, the iron-DBT interactions were measured by iron-binding assay. We first demonstrated DBT increased uptake of ferrous iron through the biosynthesis of ferritin by Caco-2 cells and determined which complementary treatment would provide optimum results. Thereafter, effects of the treatment on improving the bioavailability of absorbed iron in the form of hemoglobin (Hb) were established using a DIA-animal model. The results showed that DBT slightly improved Hb levels compared with the baseline Hb and pretreatment with DBT for 2 hours prior to supplementation with ferrous sulfate provided the greatest gain in Hb levels in DIA rats. However, DBT and ferrous sulfate were co-treated with Caco-2 cell or DIA rats, the ferritin formation and Hb levels both were decreased. In iron-binding assay, the DBT extract influenced the free Fe(II) type in the FeSO4 solution. Therefore, we suggest that complementary treatment with DBT and iron supplementation can have a strong ameliorating effect on iron-deficiency anemia in clinical settings, but needs a 2-hour interval of DBT administration prior to ferrous sulfate treatment.