Lanyue Zhang

Variation in Essential Oil and Bioactive Compounds of Curcuma kwangsiensis Collected from Natural Habitats

The chemical compositions of essential oils (EOs) extracted from Curcuma kwangsiensis rhizomes collected from six natural habitats in P. R. China were evaluated using gas chromatography/mass spectrometry (GC/MS). Fifty‐seven components were identified from the six EOs, and their main constituents were 8,9‐dehydro‐9‐formyl‐cycloisolongifolene (2.37 – 42.59%), germacrone (6.53 – 22.20%), and l‐camphor (0.19 – 6.12%). The six EOs exhibited different DPPH radical‐scavenging activities (IC50, 2.24 – 31.03 μg/ml), with the activity of most of EOs being much higher than that of Trolox C (IC50, 10.49 μg/ml) and BHT (IC50, 54.13 μg/ml). Most EOs had potent antimicrobial effects against the tested bacteria and fungus. They also exhibited cytotoxicity against B16 (IC50, 4.44 – 147.4 μg/ml) and LNCaP cells (IC50, 73.94 – 429.25 μg/ml). The EOs showed excellent anti‐inflammatory action by significantly downregulating expression of pro‐inflammatory cytokines, cyclooxygenase‐2, and tumor necrosis factor‐α. This study provides insight into the interrelation among growth location, phytoconstituents, and bioactivities, and the results indicate the potential of C. kwangsiensis as natural nutrients, medicines, and others additives.

Synthesis of carbazole derivatives containing chalcone analogs as non-intercalative topoisomerase II catalytic inhibitors and apoptosis inducers

Novel topoisomerase II (Topo II) inhibitors have gained considerable interest for the development of anticancer agents. In this study, a series of carbazole derivatives containing chalcone analogs (CDCAs) were synthesized and investigated for their Topo II inhibition and cytotoxic activities. The results from Topo II mediated DNA relaxation assay showed that CDCAs could significantly inhibit the activity of Topo II, and the structure-activity relationship indicated the halogen substituent in phenyl ring play an important role in the activity. Further mechanism studies revealed that CDCAs function as non-intercalative Topo II catalytic inhibitors. Moreover, some CDCAs showed micromolar cytotoxic activities. The most potent compound 3h exhibited notable growth inhibition against four human cancer cell lines. Flow cytometric analysis revealed that compounds 3d and 3h arrested the HL-60 cells in sub G1 phase by induction of apoptosis. It was further confirmed by Annexin-V-FITC binding assay. Western blot analysis revealed that compound 3h induces apoptosis likely through the activation of caspase proteins.

Variation on composition and bioactivity of essential oils of four common Curcuma herbs

Chemical compositions, antioxidative, antimicrobial, anti‐inflammatory, and cytotoxic activities of essential oils extracted from four common Curcuma species (Curcuma longa, Curcuma phaeocaulis, Curcuma wenyujin, and Curcuma kwangsiensis) rhizomes in P. R. China are comparatively studied. In total, 47, 49, 35, and 30 compounds are identified in C. longa, C. phaeocaulis, C. wenyujin, and C. kwangsiensis essential oils by GC/MS, and their richest compounds are ar‐turmerone (21.67%), elemenone (19.41%), curdione (40.23%) and (36.47%), respectively. Moreover, C. kwangsiensis essential oils display the strongest DPPH (2,2‐diphenyl‐1‐picrylhydrazyl) radical‐scavenging activity (IC50, 3.47 μg/ml), much higher than ascorbic acid (6.50 μg/ml). C. phaeocaulis oils show the best antibacterial activities against Escherichia coli (MIC, 235.54 μg/ml), Pseudomonas aeruginosa (391.31 μg/ml) and Staphylococcus aureus (378.36 μg/ml), while C. wenyujin and C. kwangsiensis oils show optimum activities against Candida albicans (208.61 μg/ml) and Saccharomyces cerevisiae (193.27 μg/ml), respectively. C. phaeocaulis (IC50, 4.63 μg/ml) and C. longa essential oils (73.05 μg/ml) have the best cytotoxicity against LNCaP and HepG2, respectively. C. kwangsiensis oils also exhibit the strongest anti‐inflammatory activities by remarkably down‐regulating expression of COX‐2 and TNF‐α. Therefore, due to their different chemical compositions and bioactivities, traditional Chinese Curcuma herbs should be differentially served as natural additives for food, pharmaceutical, and cosmetic.

Mechanistic Study of Inhibitory Effects of Metformin and Atorvastatin in Combination on Prostate Cancer Cells in Vitro and in Vivo

Metformin is a commonly used drug for the treatment of type II diabetes and atorvastatin is the most prescribed cholesterol-lowering statin. The present study investigated the effects and mechanisms of metformin and atorvastatin in combination on human prostate cancer cells cultured in vitro and grown as xenograft tumor in vivo. Metformin in combination with atorvastatin had stronger effects on growth inhibition and apoptosis in PC-3 cells than either drug alone. The combination also potently inhibited cell migration and the formation of tumorspheres. Metformin and atorvastatin in combination had a potent inhibitory effect on nuclear factor-kappaB (NF-κB) activity and caused strong decreases in the expression of its downstream anti-apoptotic gene Survivin. Moreover, strong decreases in the levels of phospho-Akt and phosphor-extracellular signal-regulated kinase (Erk)1/2 were found in the cells treated with the combination. The in vivo study showed that treatment of severe combined immunodeficient (SCID) mice with metformin or atorvastatin alone resulted in moderate inhibition of tumor growth while the combination strongly inhibited the growth of the tumors. Results of the present study indicate the combination of metformin and atorvastatin may be an effective strategy for inhibiting the growth of prostate cancer and should be evaluated clinically.

Distribution and diversity of twelve Curcuma species in China

Abstract Genus Curcuma a wild species presents an important source of valuable characters for improving the cultivated Curcuma varieties. Based on the collected germplasms, herbariums, field surveys and other literatures, the ecogeographical diversity of Genus Curcuma and its potential distributions under the present and future climate are analysed by DIVA-GIS. The results indicate Genus Curcuma is distributed over 17 provinces in China, and particularly abundant in Guangxi and Guangdong provinces. The simulated current distributions are close to the actual distribution regions. In the future climate, the suitable areas for four Curcuma species will be extended, while for other three species the regions will be significantly decreased, and thus these valuable resources need protecting.

Synergistic inhibitory effects of naproxen in combination with magnolol on TPA-induced skin inflammation in mice

The combination of naproxen with herbs having a range of pharmacological effects is a potential alternative to improve their bioactivity and limit their adverse effects. Inspired by magnolol, an active constituent found in the bark of Magnolia officinalis, we therefore evaluated the efficacy of naproxen (N) plus magnolol (M) in 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced skin inflammation. During application, treatment with N and M significantly reduced skin inflammation, and the combination of N and M resulted in a synergistic effect. Further mechanistic investigations clearly demonstrated that A3 (N : M = 1 : 3, mol mol−1) markedly suppressed TPA-induced pro-inflammatory cytokines and COX-2 expressions, inhibited NF-κB activity, downregulated IκBα and IκB kinase (IKK) activities, and inhibited PI3K/Akt and PI3K/PKC signaling pathways. These results indicated that a combination of N and M effectively inhibited TPA-induced skin inflammation via blocking PI3K/Akt/IKK and PI3K/PKC/IKK signaling pathways.

Aromatic-Turmerone Attenuates LPS-Induced Neuroinflammation and Consequent Memory Impairment by Targeting TLR4-Dependent Signaling Pathway

SCOPE Curcuma longa (turmeric) is a folk medicine in South and Southeast Asia, which has been widely used to alleviate chronic inflammation. Aromatic-turmerone is one of the main components abundant in turmeric essential oil. However, little information is available from controlled studies regarding its biological activities and underlying molecular mechanisms against chronic inflammation in the brain. In the current study, we employed a classical LPS model to study the effect and mechanism of aromatic-turmerone on neuroinflammation. METHODS AND RESULTS The effects of aromatic-turmerone were studied in LPS-treated mice and BV2 cells. The cognitive function assays, protein analyses, and histological examination were performed. Oral administration of aromatic-turmerone could reverse LPS-induced memory disturbance and normalize glucose intake and metabolism in the brains of mice. Moreover, aromatic-turmerone significantly limited brain damage, through inhibiting the activation of microglia and generation of inflammatory cytokines. Further study in vitro revealed that aromatic-turmerone targeted Toll-like receptor 4 mediated downstream signaling, and lowered the release of inflammatory mediators. CONCLUSION These observations indicate that aromatic-turmerone is effective in preventing brain damage caused by neuroinflammation and may be useful in the treatment of neuronal inflammatory diseases.

Atorvastatin and Caffeine in Combination Regulates Apoptosis, Migration, Invasion and Tumorspheres of Prostate Cancer Cells

Atorvastatin is the most prescribed cholesterol-lowering statin, while caffeine enhances chemo-sensitivity and induces apoptosis of tumor cells through its DNA repair-inhibiting effect. The present study investigated the effects and mechanisms of atorvastatin and caffeine in combination on human prostate cancer cells cultured in vitro . Cell growth were determined by the trypan blue exclusion assay. The cell apoptosis and colony formation were determined by morphological assessment. The ability of cell migration and invasion were performed using a scratch wound-healing and Transwell assay. Tumorspheres were formed in suspension under the condition of non-adherence and serum-free medium. Finally, the western blot assay was used to determine the levels of proteins. The combination synergistically suppressed proliferation and induced apoptotic death. Meanwhile, the migration, invasion, and the formation of tumorspheres were significantly inhibited by the combination. We found that atorvastatin and caffeine in combination downregulated phospho-Akt, phospho-Erk1/2, anti-apoptotic Bcl-2 and Survivin protein levels. Results of the present study indicate treatment with the combination of caffeine and atorvastatin may be an effective strategy for inhibiting the growth of prostate cancer and should be evaluated clinically.

The Chemical Compositions of Angelica pubescens Oil and Its Prevention of UV-B Radiation-Induced Cutaneous Photoaging

Angelica pubescens, a plant of the family Umbelliferae, has been widely used as traditional Chinese medicine for the treatment of many diseases. However, there has been minimal modern research focused on the pharmacological activity of oils extracted from Angelica pubescens, in particular, the potential anti‐photoaging effects. Therefore, in the present study, we analyzed the chemical composition of Angelica pubescens oil (AO) and evaluated its bioactivity against photoaging in ultraviolet (UV) ‐B radiation‐induced hairless mice. Overall, we identified and analyzed 93 compounds from the AO by gas chromatography‐mass spectrometry (GC/MS). The top ten compounds were as follows: osthole (44.608%), glutaric acid hexadecyl pent‐4‐en‐1‐yl ester (5.758%), α‐bisabolol (3.795%), eugenol (3.637%), (Z)‐docos‐13‐enamide (3.286%), (3S,3aR)‐3‐butyl‐3a,4,5,6‐tetrahydro‐3H‐2‐benzofuran‐1‐one (3.043%), m‐cresol (2.841%), trans‐sesquisabinene hydrate (2.128%), 4‐hydroxy‐2‐methylacetophenone (1.735%), and (Z)‐9‐pentadecenol (1.509%). Application of AO improved the condition of UV‐B radiation‐induced damaged skin, and the mechanism of action was found to be related to inhibition of the production of inflammatory cytokines. These results highlight the potential application of AO for the development of skin care products.

Antioxidative Activities of Essential Oils and Ethanol Extrations from Ornamental Zingiberaceae Species

Abstract The essential oils from five different Zingiberaceae species [Costus speciosus (J. Konig.) Smith, Hedychium coronarium J. Koenig, Hedychium gardnerianum Griff., Zingiber zerumbet (Linn.) Roscoe ex Smith, Hedychium chrysoleucum Hook.] were extracted through hydro-distillation process and their chemical compounds were analyzed by GC-MS. In addition, the antioxidant activities of essential oils and ethanol extractions were described. The yields of essential oils ranged from 0.20 % in C. speciosus to 1.52 % in Z. zerumbet. A total of 48 components were identified, of which majority were ⟨-santalo (0.22-41.83 %), aromadendrene oxide I (39.63-55.40 %) and zerumbone (1.67-84.07 %). The essential oils showed an effective DPPH• scavenging activities with IC50 values ranging between 5.28 and 13.26 μg/mL. The result showed that the ethanol extractions had different DPPH• scavenging (IC50, 0.94-9.92 μg/mL) and most of them were lower than ascorbic acid (IC50, 8.37 μg/mL) and trolox (IC50, 10.19 μg/mL). The results indicate that the essential oils and ethanol extractions from the five ornamental Zingiberaceae species could serve as an important bio-resource of antioxidant for using in the functional food, cosmetic, and pharmaceutical industries.