Search

The fruit and hulls of the water caltrop ( Trapa taiwanensis Nakai) are used as hepatoprotective herbal tea ingredients in Taiwan. The stability of hydrolysable tannins in herbal drinks has rarely been reported. In the present study, two hydrolysable tannins, tellimagrandin II (TGII) and 1,2,3,4,6-pentagalloylglucopyranose (PGG), were isolated from water caltrop hulls. The stability of the two compounds was evaluated by treatment with various pH buffer solutions, simulated gastric fluid and intestinal fluid, different temperatures, and photo-irradiation at 352 nm in different solvents. Results showed that TGII and PGG were more stable in a pH 2.0 buffer solution (with 91.88% remaining) and in a water solution with 352 nm irradiation (with 95% remaining). TGII and PGG were more stable in methanol or ethanol solutions (with >93.69% remaining) than in an aqueous solution (with <43.52% remaining) at 100 °C. In simulated gastric fluid, more than 96% of the hydrolysable tannins remained after incubation at 37 °C for 4 h. However, these hydrolysable tannins were unstable in simulated intestinal fluid, as after incubation at 37 °C for 9 h, the content of TGII had decreased to 31.40% and of PGG to 12.46%. The synthetic antioxidants, butyl hydroxy anisole (BHA), di-butyl hydroxy toluene (BHT), and propyl gallate, did not exhibit photoprotective effects on these hydrolysable tannins. However, catechin, a natural antioxidant, displayed a weak photoprotective effect. Ascorbic acid had a short-term thermal-protective effect but not a long-term protective effect. The different stability properties of hydrolysable tannins in solutions can be used in the development of related herbal teas in the future.

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 (SC 50 ) 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., (Copyright © 2017. Published by Elsevier B.V.)

Acne is a common skin condition with sebum overproduction, hyperkeratosis, Propionibacterium acnes ( P . acnes ) and Staphylococcus aureus , and inflammation. Punica granatum (pomegranate) is well-known for its anti-inflammatory effects; however, few studies have discussed the anti-acne effects of pomegranate. In this study, we found that pomegranate extract (PG-E) significantly reduced P . acnes -induced edema in Wistar rat ears. Therefore, an evaluation platform using multiple pathogenic mechanisms of acne was established to explore the anti-acne effects of pomegranate. Results showed that PG-E inhibited bacterial growth and lipase activity. Through a bioguided-fractionation-isolation system, four hydrolysable tannins, punicalagin ( 1 ), punicalin ( 2 ), strictinin A ( 3 ), and granatin B ( 4 ), were isolated. Compounds 1 and 2 had greater anti-bacterial activities and anti-testosterone-induced HaCaT proliferative effects than the others. Compounds 1 , 3 , and 4 displayed lipase inhibitory effects. Compound 4 decreased cyclooxygenase-2 expression and downregulated prostaglandin E₂ production in heat-killed P . acnes -treated RAW 246.7 cells. In conclusion, PG-E is abundant in hydrolysable tannins that display multiple anti-acne capacities, including anti-bacterial, anti-lipase, anti-keratinocyte proliferation, and anti-inflammatory actions. Hence, PG-E has great potential in the application of anti-acne and skin-care products, and punicalagin ( 1 ), the most effective component in PG-E, can be employed as a quality control marker., Competing Interests: The authors declare no conflict of interest.

Eight ethanolic extracts of indigenous Taiwanese plants of the genus Alpinia were tested for tumor cytotoxicity against AGS, Hep G2, HeLa, KB, and HL-60 cells. Among the 50 % and 95 % EtOH extracts of eight Alpinia species, the cytotoxic effects of Alpinia intermedia leaves were the strongest. When the leaf extract of A. intermedia was partitioned using n -hexane and aqueous solvents, the n -hexane layer showed a greater cytotoxic effect and could prolong the survival time of P-388D 1 tumor-bearing CDF1 mice. Two new labdane diterpene derivatives, intermedin A ( 1 ) and intermedin B ( 2 ), and coronarin E ( 3 ) were isolated from the n -hexane layer of A. intermedia . Intermedin A induced apoptosis in HL-60 cells at 30 µg/mL and significantly prolonged the survival time of P-388D 1 tumor-bearing CDF 1 mice by 48.7 % at 20 mg/kg of body weight. We suggest that intermedin A is a major compound of A. intermedia and has a cytotoxic effect on HL-60 and P-388D 1 cells., (Georg Thieme Verlag KG Stuttgart · New York.)

The rhizomes of many Atractylodes species, including Atractylodes chinensis Koidzumi, Atractylodes macrocephala Koidzumi, and Atractylodes japonica Koidzumi, are collectively termed Atractylodis Rhizoma. We prepared n-hexane extracts of the three species and evaluated their anti-inflammatory effects on lipopolysaccharide (LPS)-induced RAW 264.7 cells. Among all n-hexane extracts, those of A. japonica most strongly inhibited nitric oxide (NO) production in LPS-induced RAW 264.7 cells; five sesquiterpenes, atractylon, atractylenolide I, atractylenolide II, atractylenolide III, and 8-epiasterolid, were isolated from A. japonica. The phytochemical content of A. japonica was similar to those of A. chinensis and A. macrocephala. Moreover, the atractylon concentration was higher in A. japonica than in A. chinensis and A. macrocephala. Atractylon significantly inhibited NO and prostaglandin E2 production as well as inducible NO synthase and cyclooxygenase-2 expression in LPS-induced RAW 264.7 cells. Atractylon (40 mg/kg) also significantly reduced the acetic-acid-induced writhing response, carrageenan-induced paw edema, and hot-plate latent pain response in mice. According to the results, A. japonica has anti-inflammatory and antinociceptive effects and atractylon is the major active component of A. japonica. Therefore, atractylon can be used as a bioactivity marker in A. japonica.

Vitis thunbergii Sieb. et Zucc. var. taiwaniana Lu (VT) is an indigenous plant in Taiwan that is traditionally used for promoting joint health. In this study, we used in vitro primary human chondrocytes (PHCs) and two in vivo animal models to evaluate the anti-inflammatory effects of VT on arthritis. Results showed that the water extract of the stems and roots from VT (VT-SR) was rich in flavones and phenols with 1.1 mg/g of resveratrol, 6.7 mg/g of hopeaphenol, and 5.1 mg/g of (+)-ɛ-viniferin. VT-SR significantly scavenged DPPH radicals and inhibited prostaglandin E2 (PGE2) production in lipopolysaccharide (LPS)-induced PHCs without exhibiting significant cytotoxicity. In in vivo models, the VT-SR (500 mg/kg) significantly decreased serum PGE2 and knee 2-(18)F-fluoro-2-deoxy-D-glucose ((18)F-FDG) levels in LPS-induced acute inflammatory arthritis in rabbits. In addition, dietary supplementation with VT-SR for 28 days significantly alleviated type II collagenase-induced rat osteoarthritis with improvements in weight bearing and range of motion tests. In conclusion, our results suggest that the VT-SR is a good candidate for developing dietary supplements to prevent joint deterioration and inhibit inflammation.

Vitis thunbergii var. taiwaniana (VTT) is a wild grape native to Taiwan, where it has been used as a folk medicine. In this study, we found that the branch and leaf ethanol extracts of VTT significantly inhibited the inducible nitric oxide (NO) synthase protein expression and NO production in BV2 microglia. Using primary neuronal cells, kainic acid (KA) significantly increased hydrogen peroxide production in a dose-dependent manner. All four ethanol extracts of VTT significantly decreased hydrogen peroxide production. However, only root and branch ethanol extracts were able to prevent the neuronal cell death induced by KA in vitro. In the animal study, administration of all four plant part extracts of VTT delayed the onset of seizure and decreased the hippocampus neuronal cell loss, and the neuroprotective activity could be ranked as follows: branch approximately leaf > root > trunk. The results suggest that VTT extracts have a potential to prevent neurodegeneration through the antioxidative activity by their ability to inhibit NO and hydrogen peroxide production.

The fresh rhizome of Zingiber zerumbet (L.) Roscoe ex Smith (Zingiberaceae) is widely used as a folk medicine in Taiwan. In this study, the fresh rhizome was extracted with 95 % EtOH and partitioned with diethyl ether. The antitumor effects of the diethyl ether extract were measured in cultured P-388D (1) cells and in an animal model of P-388D (1)-bearing CDF (1) mice. The results indicated that the extract could induce DNA fragmentation in P-388D (1) cells in vitro, and significantly prolong the life of P-388D (1)-bearing CDF (1) mice (ILS% = 127.8) at a dosage of 5 mg/kg body weight. After column chromatography combined with an MTT cytotoxicity bioassay, zerumbone, a cyclic sesquiterpene was isolated from the diethyl ether extract. Zerumbone inhibited the growth of P-388D (1) cells, induced DNA fragmentation in culture, and significantly prolonged the life of P-388D (1)-bearing CDF (1) mice (ILS% = 120.5) at a dosage of 2 mg/kg. Furthermore, zerumbone inhibited the growth of a human leukemia cell line, HL-60 cells, in a time- and concentration-dependent manner, with IC (50) values of 22.29, 9.12, and 2.27 microg/mL for 6, 12, and 18 h, respectively. The cell cycle of HL-60 cells was observed after treatment with zerumbone, which induced G (2)/M cell cycle arrest in HL-60 cells in a time- and concentration-dependent manner, and decreased the cyclin B1/cdk 1 protein level. These results suggest that zerumbone is an active principal of Z. zerumbet and is potentially a lead compound for the development of anticancer drugs.

Cnidii monnieri Fructus [CmF; Cnidium monnieri (L.) Cusson] is used as a tonic agent in traditional Chinese medicine. In a previous Chinese herb-cytotoxicity screening test, the ethanol extract of CmF exhibited strong effects on human leukemia (HL-60), cervical carcinoma (HeLa) and colorectal carcinoma (CoLo 205) cells. Then, the CmF extract was subjected to silica gel column chromatography and recrystallization to give five coumarins: osthol, imperatorin, bergapten, isopimpinellin, and xanthotoxin. Among these compounds, osthol showed the strongest cytotoxic activity on tumor cell lines. The structure-activity relationship established from the results indicated that the prenyl group has an important role in the cytotoxic effects. However, imperatorin showed the highest sensitivity to HL-60 cells and the least cytotoxicity to normal PBMCs. Osthol and imperatorin both caused apoptotic bodies, DNA fragmentation, and enhanced PARP degradation in HL-60 cells by biochemical analysis. These results indicate that osthol and imperatorin can induce apoptosis in HL-60 cells. Therefore, osthol and imperatorin are cytotoxic marker substances in the fruits of Cnidium monnieri.