Citrus aurantium L. var. amara Engl. inhibited lipid accumulation in 3T3-L1 cells and Caenorhabditis elegans and prevented obesity in high-fat diet-fed mice.

Natural products with anti-obesity effects and few side effects have attracted great attention recently. Citrus aurantium L. var. amara Engl. (CAVA) is popularly consumed as an edible and medicinal resource in China. However, its anti-obesity effects were poorly understood. The anti-obesity effects of CAVA extracts were systematically evaluated using 3T3-L1 cells, Caenorhabditis elegans (C. elegans) and high fat diet (HFD)-fed mice. Flavonoid-rich (EA) extracts with neohesperidin, hesperidin and naringin comprising 32.15%, were isolated from CAVA. EA extracts treatment significantly inhibited differentiation of 3T3-L1 preadipocytes by modulating lipid metabolism-related mediators. EA extracts supplementation also inhibited antioxidant responses in C. elegans by decreasing reactive oxygen species generation and malonaldehyde value, and increasing superoxide dismutase content. EA extracts feeding markedly decreased triglyceride (TG) content, and affected expression of genes involved in lipid and glucose metabolism in wild type C. elegans. TG content in mdt-15 (XA7702) mutants was not decreased by EA extracts administration, suggesting that EA extracts treatment might inhibit lipid accumulation in C. elegans dependent on mdt-15. EA extracts intervention further reduced body weight gain and modulated plasma biochemical parameters in HFD-fed mice. EA extracts treatment prevented HFD-induced epididymal adipose hypertrophy, liver oxidative injuries and steatosis. EA extracts administration also strongly prevented HFD-induced reduction of gut microbial diversity, decreased the Firmicutes-to-Bacteroidetes ratio and the Erysipelotrichaceae abundance, and enhanced the Bifidobacteriace abundance in HFD-fed mice. EA extracts from blossoms of CAVA were excellent antiobesogenic candidates that acted through multiple mechanisms that acted simultaneously.

[Retrieval of spectral characteristics of hyperspectral sensor and retrieval of reflectance spectra].

On-orbit spectral calibration of hyperspectral imaging data is a key step for quantitatively analyzing them. Like the atmospheric correction, accurate spectral calibration is very necessary for improved studies of land or ocean surface properties. Based on the previous literatures, a new method which coupled an optimization algorithm was developed to simultaneously retrieve the central wavelength and the full width at half maximum (FWHM) of the hyperspectral sensor without needing the in situ reflectance spectra. Firstly, the Hyperion data set simulated using MODTRAN4 with the Hyperion spectral specification was used to test the new method, and the results indicated that the maximum error was less than 0.1 and 0.7 nm for central wavelength and FWHM respectively when the spectral shift is 5 nm. Then the algorithm was applied to the Hyperion data acquired on May 20, 2008 over Heihe River Basin and it was iteratively performed for each detector of the two spectrometers of Hyperion. The results showed that the VNIR of Hyperion had a pronounced smile effect, and the shift in on-orbit calibration with respect to the laboratory was from -2 to +2 nm, while the SWIR has essentially no smile effect, the wavelength correction was relatively flat over all sample with an approximately constant value of 3 nm. The FWHM in VNIR could range from -0.2 to 0.5 nm as a function of sample number of the spectrometer, and in SWIR it ranged from -2 to -3 nm. So for both the VNIR and SWIR, the original spectral calibration should be updated. These results showed good agreement with previous research findings, and which also proved the feasibility of the new method. Finally, with the updated spectral calibration characteristics, the sample reflectances of desert and vegetation target in our study site were reconstructed by applying a further atmospheric correction, and as expected, the strong spikes around the typical atmospheric absorption were almost disappeared.

Natural Products with Analgesic Effect from Herbs and Nutraceuticals Used in Traditional Chinese Medicines.

BACKGROUND: Pain is one of the most common clinical symptoms . This review aims to describe research on herbs and their active ingredients in treating pain and provide a valuable reference for the development and utilization of analgesic traditional Chinese medicine (TCM). MATERIAL AND METHODS: The literature search was performed from 1995 to October 2016, covering the relevant studies that concern the treatment of pain with TCM. Active ingredients extracted from TCM with analgesic activity are summarized and classified into six categories, including polysaccharides, saponins, alkaloids, flavonoids, terpenoids, and other constituents. RESULTS: There are two pathways constituting the analgesic mechanisms of TCM: through the central nervous system and the peripheral nervous system. The former pathway includes increasing the content of endogenous analgesic substances like opiate peptide, cutting down the second messenger of neurotransmitter like nitric oxide (NO), reducing the content of prostaglandin E2 (PGE2) in brain tissues, blocking the central calcium channel, reducing excitatory amino acids in brain tissues, inhibiting their receptors and raising the content of the central 5-hydroxytryptamine (5-HT). The latter one usually involves the decrease in the secretion of peripheral algogenic substances, the induction of pain-sensitive substances, the accumulation of a local algogenic substance, the increase in the release of peripheral endogenous analgesia materials and the regulation of c-Fos gene (immediate early gene).

Carriers Based on Zein-Dextran Sulfate Sodium Binary Complex for the Sustained Delivery of Quercetin.

Herein, a self-assembly formulation of Zein and dextran sulfate sodium (DSS) binary complex has been developed for the quercetin (Que) delivery. The prepared particles display a smooth sphere in the range of 180 ~ 250 nm. The addition of DSS shields the Trp residues of Zein that were located on the hydrophilic exterior and in-turn reduces the surface hydrophobicity of the nanoparticles. The presence of DSS, indeed, increases the encapsulation efficiency of Que from the initial 45.9 in the Zein to 72.6% in the Zein/DSS binary complex. A significant reduction of Que diffusion in the simulated intestinal conditions has been observed with the addition of DSS on the nanoparticles, which also improves Que bioavailability. The release mechanism of Que-loaded Zein/DSS composites is in accordance with the Higuchi model (Q = 0.0913t0.5+0.1652, R 2 = 0.953). Overall, nanoparticles based on Zein-DSS complexes stand out as an attractive carrier system of quercetin and the outcome could be extended to several bioactive compounds.

Bergaptol from blossoms of Citrus aurantium L. var. amara Engl inhibits LPS-induced inflammatory responses and ox-LDL-induced lipid deposition.

Aberrant activation of inflammation and excess accumulation of lipids play pivotal roles in atherosclerosis (AS) progression. Constituents from Citrus aurantium Linn variant amara Engl (CAVA) were effectively investigated for their various bioactivities, especially anti-inflammation. Bergaptol (BER) is particularly abundant in Citrus products. Accumulating studies have confirmed its predominant anti-cancer and antioxidant functions, whereas few studies focused on its antiatherogenic functions. In the current study, BER was isolated from CAVA for the first time. Macrophages were stimulated with lipopolysaccharides (LPSs) or oxidized low-density lipoproteins (ox-LDL) to mimic inflammatory responses and AS development. BER treatment significantly inhibited LPS-induced production of nitric oxide (NO), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α), and gene expression of inducible nitric oxide synthase (iNOS), IL-6, TNF-α, interleukin-1 beta (IL-1ß) and cyclooxygenase-2 (COX-2). BER also potently blocked LPS-induced mitogen-activated protein kinase (MAPK) phosphorylation and nuclear factor-kappa B (NF-κB) activation, as evidenced by the inhibitory effects on c-Jun N-terminal kinase (JNK), P38, P65, IκBα and IκKα/ß phosphorylation, and NF-κB nuclear translocation. Furthermore, BER treatment markedly mitigated ox-LDL-induced foam cell formation by inhibiting scavenger receptor class A type I (SRA1) and cluster of differentiation 36 (CD36)-dependent cholesterol uptake. In conclusion, BER might be a novel therapeutic agent for AS prevention through inhibiting inflammatory responses and cholesterol uptake.

Potential roles of dietary flavonoids from Citrus aurantium L. var. amara Engl. in atherosclerosis development.

Dietary consumption of flavonoids correlated positively with lower risk of cardiovascular disease. However, the precise roles of flavonoids from the blossoms of Citrus aurantium Linn variant amara Engl (CAVA) in atherosclerosis (AS) are still poorly understood. This study aimed to find novel flavonoid-type skeletons with protection against AS. Total flavonoids (CAVAF), homoeriodictyol (HE) and hesperetin-7-O-ß-d-glucopyranoside (HG) were isolated from the blossoms of Citrus aurantium Linn variant amara Engl. by chromatography. Their suppressive effects on lipopolysaccharide (LPS)-induced inflammatory responses and ox-LDL-induced foam cell formation were systematically and comparatively investigated using macrophage RAW264.7 cells. HE was more powerful than HG in inhibiting LPS-induced production of nitric oxide (NO), interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), interleukin-1 beta (IL-1ß) and gene expression in RAW264.7 cells. HE and HG showed different responses to extracellular signal-regulated kinases (ERK), c-Jun N-terminal kinases (JNK), P38, P65, IκBα, IκKα/ß phosphorylation, and nuclear factor-kappa B (NF-κB) nuclear translocation. HE and HG also differentially decreased oxidized low-density lipoprotein (ox-LDL)-induced foam cell formation by regulating peroxisome proliferator-activated receptor-gamma (PPARγ), phospholipid ATP-binding cassette transporter A1 (ABCA1), phospholipid ATP-binding cassette transporter G1 (ABCG1), scavenger receptor class B type I (SRB1), scavenger receptor class A type I (SRA1) and cluster of differentiation 36 (CD36) expression at gene and protein levels in RAW264.7 cells. HG showed weaker potential than HE in preventing AS development. Their chemical differences might partially explain the discrepancy in their bioactivity. In conclusion, HE and HG might be developed into novel therapeutic agents against inflammation and AS-associated diseases.

Bioassay-guided isolation and identification of anticancer and antioxidant compounds from Gynostemma pentaphyllum (Thunb.) Makino.

Gynostemma pentaphyllum (Thunb.) Makino is a medicinal and edible plant in China whose buds and leaves are used for making a popular kind of tea drink. The anticancer and antioxidant properties of the ethyl acetate (EA) and n-butanol (n-Bu) fractions provide a basis for conducting experiments for isolation and identification of key compounds that may be responsible for the aforementioned properties of G. pentaphyllum. Four compounds were isolated from the two fractions using ODS packing column, silica gel column, polyamide column, Sephadex LH-20 gel column and HPLC. With the aid of 1H, 13C NMR and mass spectrometry, they were identified as 3,4-dihydroxy phenyl-O-ß-d-glucoside, gypenoside XLVI, gypenoside L and ginsenoside Rd. 3,4-Dihydroxy phenyl-O-ß-d-glucoside showed the strongest DPPH (97.23%) and ABTS (101.37%) scavenging effect and ferric ion reducing power (FRAP value 0.8846), which may be closely related to the hydrogen atoms of phenolic hydroxyls. Gypenoside L and ginsenoside Rd displayed the highest inhibition of tumor cell proliferation of A549 and MCF-7 cell lines, which had to do with the chemical structure of the compounds bearing glycosylated parts and free hydroxyls at the 20th or 21st carbon atom of dammarane-type saponin.

Various Antioxidant Effects Were Attributed to Different Components in the Dried Blossoms of Citrus aurantium L. var. amara Engl.

Citrus aurantium L. var. amara Engl. (CAVA) was traditionally used as an edible and medicinal material in China. Total flavonoids (CAVAF), alkaloids (CAVAA), polysaccharides (CAVAP), coumarins (CAVAC), and neroli (CAVAO) were extracted from CAVA. Hesperidin, naringin, and neohesperidin composed 83.94% of CAVAF, and synephrine represented 50.56% of CAVAA. On the basis of 1,1-diphenyl-2-picrylhydrazyl radical (DPPH•), 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt radical cation (ABTS• +), hydroxyl radical (•OH), ferric-reducing antioxidant power (FRAP), and reducing power assays, the antioxidant activities of five components were comprehensively and comparatively investigated. CAVAF had a stronger DPPH• scavenging effect and FRAP and reducing power. CAVAP and CAVAA exhibited comparable •OH scavenging effects to vitamin C. CAVAA showed the highest ABTS• + scavenging activity. In conclusion, different constituents varied significantly toward different sources of free radicals and other oxidants. It is obvious that CAVA has various antioxidant effects, which are attributed to different components.