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.
One new betaenone, theissenoic acid (1), together with three new acetogenins, theissenolactones A-C (2-4, resp.), were isolated from the fermented broth of Theissenia cinerea 89091602 isolated in Taiwan. The structures of 1-4 were elucidated by spectroscopic methods. Biological tests revealed that 3 and 4 exhibited moderate growth-inhibitory activities against A549 lung cancer cell line with GI(50) values of 14.9 and 47.9 μM, respectively.
The rhizome of Atractylodes ovata De Candolle is rich in essential oils, which are usually removed by processing. In this study, anti-oxidative abilities of essential oils and aqueous extracts of A. ovata rhizome were explored, and the influence of processing on the anti-oxidative abilities was examined. Essential oils and aqueous extracts of A. ovata were extracted by boiling water and steam distillation, respectively. Quality of these two A. ovata samples was controlled by HPLC and GC-MS system, and anti-oxidative abilities were then evaluated. Results showed that surface color of A. ovata turned to brown and chemical components were changed by processing. Contents of both atractylon and atractylenolide II decreased in the essential oils, but only the contents of atractylon decreased by processing. Atractylenolide III increased in both A. ovata samples. However, A. ovata essential oils displayed stronger anti-oxidative abilities than aqueous extracts in DPPH-scavenging, TBH-induced lipid peroxidation and catalase activity assays. Moreover, the bioactivity of essential oils from raw A. ovata was stronger than oils from processed A. ovata. On the other hand, cytotoxicity of A. ovata essential oils was stronger than that of aqueous extracts, and was more sensitive on H9C2 cell than NIH-3T3 and WI-38 cells. In contrast, stir-frying processing method increased cytotoxicity of essential oils, but the cytotoxicity was ameliorated when processed with assistant substances. The results suggested that phytochemical components and bioactivity of A. ovata were changed after processing and the essential oils from raw A. ovata showed better anti-oxidative and fewer cytotoxicity effects.
A series of six isopimarane-type diterpene glycosides, along with an eremophilane-type sesquiterpene, i.e., elaeicolasides A-C (1-3, resp.), 16-(α-D-mannopyranosyloxy)isopimar-7-en-19-oic acid (4), hymatoxin K (5), hymatoxin L (6), and elaeicolalactone (7), were isolated from the AcOEt extract of the fermented broth of Stilbohypoxylon elaeicola YMJ173. Among these, 1-3 and 7 are new compounds based on their spectroscopic data and sugar composition analysis. The effects of 1-7 on the inhibition of nitric oxide (NO) production in lipopolysaccharide (LPS)-activated murine macrophage RAW264.7 cells were evaluated. All these compounds inhibited NO production, detected as nitrite in the culture medium, in activated macrophages without any cytotoxicity at a concentration of 100 μM. Among these compounds, 2 showed a significant activity with the average maximum inhibition (E(max)) and median inhibitory concentration (IC(50)) values of 93.3±0.5% and 79.3±0.4 μM, respectively.
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