GLUT1 Promotes NLRP3 Inflammasome Activation of Airway Epithelium in Lipopolysaccharide-Induced Acute Lung Injury.

Acute lung injury (ALI) is a devastating clinical syndrome caused by different factors, with high morbidity and mortality. Lung injury and inflammation caused by lipopolysaccharide (LPS) can be modulated by NLRP3 inflammasome activation, yet its exact function within the airway epithelium is still unknown. Meanwhile, glucose transporter protein 1 (GLUT1) contributes to a number of inflammatory illnesses, including ALI. The present study aimed to assess GLUT1's function in NLRP3 inflammasome activation of airway epithelium in LPS-induced acute lung injury. BALB/c mice and BEAS-2B cells were exposed to LPS (5 mg/kg and 200 µg/mL, respectively), with or without GLUT1 antagonists (WZB117 or BAY876). LPS up-regulated pulmonary expression of NLRP3 and GLUT1 in mice, which could be blocked by WZB117 or BAY876. Pharmacological inhibition of GLUT1 in vivo significantly attenuated lung tissue damage, neutrophil accumulation, and proinflammatory factors release (TNF-α, IL-6, and IL-1ß) in LPS-exposed mice. Meanwhile, the activation markers of NLRP3 inflammasome (ASC, caspase-1, IL-1ß, and IL-18) induced by LPS were also suppressed. In cultured BEAS-2B cells, LPS induced an increase in GLUT1 expression and triggered activation of the NLRP3 inflammasome, both of which were inhibited by GLUT1 antagonists. These results illustrate that GLUT1 participates in LPS-induced ALI and promotes the activation of the NLRP3 inflammasome in airway epithelial cells.

Adventitious roots support population expansion of the invasive plant Mikania micrantha Kunth.

Mikania micrantha Kunth is a serious invasive alien plant characterized by the formation of an adventitious root system in its prostrate growth form. Unlike the initial roots from seed germination, adventitious roots gradually appear above the stem and branch nodes. Little is known about adventitious roots play on plant growth and population expansion of M. micrantha. We hypothesized that adventitious roots provide an advantage for plant growth and nutrient availability. To test this hypothesis, plant growth, physiology, and nutrition characteristics of M. micrantha were measured under four soil surface conditions allowing various plant parts to touch the soil to stimulate variable adventitious root formation. The results showed that the biomass, stem length, branch number, and adventitious root biomass of M. micrantha were significantly increased (P < 0.05) with increasing nodes bearing adventitious roots. As the number of nodes with adventitious roots increased, the net photosynthetic rate, antioxidant enzyme activities like superoxide dismutase, catalase, peroxidase, and malondialdehyde, chlorophyll content, and plant nutrient contents (N, P, and K) of M. micrantha were increased (P < 0.05), with higher values in main stem leaves than in those of branch leaves. The concentrations of soil organic matter, total N, total P, total K, available N, available P, and available K were greater (P < 0.05) in initial soil (CK) than in treatment soil (with M. micrantha) and were significantly reduced by adventitious roots. Our study was the first to show that plant growth, physiology and nutrition status of M. micrantha were strongly promoted by adventitious roots in the prostrate growth form.

Potential use of Helianthus tuberosus to suppress the invasive alien plant Ageratina adenophora under different shade levels.

BACKGROUND: An ecological approach for managing biological invasions in agroecosystems is the selection of alternative crop species to manage the infestation of invasive alien plants through competition. In the current study, plant growth, photosynthesis, and competitive ability of the crop Helianthus tuberosus L. (Jerusalem artichoke) and the invasive alien plant Ageratina adenophora (Spreng.) R. M. King and H. Rob were compared under varying shade levels by utilizing a de Wit replacement series method. We hypothesized that H. tuberosus had higher competitive ability than A. adenophora even under shaded conditions. RESULTS: The results showed the main stem, leafstalk length, leaf area, underground biomass, and aboveground biomass of A. adenophora were significantly lower compared to H. tuberosus in monoculture although A. adenophora had a greater number of branches that were longer on average. Under full sunlight, the total shoot length (stem + branch length), main stem length and branch length of A. adenophora were significantly suppressed (P < 0.05) by increasing proportions of H. tuberosus, and the same morphological variables of H. tuberosus were significantly higher with decreasing proportions of H. tuberosus. With increasing shade rates and plant ratios, the plant height, branch, leaf, and biomass of both plants were significantly suppressed, but to a greater degree in the case of A. adenophora. The net photosynthetic rate (Pn) of H. tuberosus and A. adenophora increased gradually from July to September, then decreased in October. The Pn of H. tuberosus was consistently higher than that of A. adenophora. Although the Pn for both species was significantly reduced with increasing shade rates and plant ratios, A. adenophora experienced greater inhibition than H. tuberosus. The relative yield (RY) of A. adenophora was significantly less than 1.0 (P < 0.05) in mixed culture under all shade levels, indicating that the intraspecific competition was less than interspecific competition. The RY of H. tuberosus was significantly less than 1.0 under 40-60% shade and greater than 1.0 (P < 0.05) under 0-20% shade in mixed culture, respectively, showing that intraspecific competition was higher than interspecific competition under low shade, but the converse was true under high shade. The relative yield total (RYT) of A. adenophora and H. tuberosus was less than 1.0 in mixed culture, indicating that there was competition between the two plants. The fact that the competitive balance (CB) index of H. tuberosus was greater than zero demonstrated a higher competitive ability than A. adenophora even at the highest shade level (60%). CONCLUSIONS: Our results suggest that H. tuberosus is a promising replacement control candidate for managing infestations of A. adenophora, and could be widely used in various habitats where A. adenophora invades.

Characterization and simultaneous quantification of biological aporphine alkaloids in Litsea cubeba by HPLC with hybrid ion trap time-of-flight mass spectrometry and HPLC with diode array detection.

The root and rhizome of Litsea cubeba (Lour) Pers., named 'Dou-chi-jiang' in Chinese, has been traditionally used for treatment of cardiovascular and cerebrovascular diseases, rheumatic arthralgia, and other diseases in China. Aporphine alkaloids are its characteristic ingredients and responsible for its bioactivities, especially anti-inflammatory and analgesic effects. A sensitive and reliable high-performance liquid chromatography with diode array detection-tandem mass spectrometry method was developed for characterization and simultaneous determination of biological aporphine alkaloids in 'Dou-chi-jiang'. The optimized chromatographic conditions were performed on an Eclipse XDB C18 column with a gradient of acetonitrile/water containing 0.1% formic acid as the mass spectrometry mobile phase and acetonitrile/water containing 0.2% diethylamine (pH 3.10, adjusted by acetic acid) as the liquid chromatography mobile phase. The fragmentation pathways by loss of CO, ·CH3 , ·NH3 , and ·NH2 CH3 were detected as characteristic for aporphine alkaloids. Based on these characteristics, total 12 analogues were identified. The quantification method was validated in terms of linearity, precision, and accuracy for six major aporphine alkaloids, which was successfully applied for simultaneous determination in ten batches of samples. The established method is simple, rapid, and specific for characterization and quantitation of aporphine alkaloids in 'Dou-chi-jiang' and other traditional Chinese medicines rich in this kind of ingredient.

Chemical constituents with NO production inhibitory and cytotoxic activities from Litsea cubeba.

A bioassay-guided fractionation of the roots and stems of Litsea cubeba led to the isolation of 14 constituents, including three new compounds, cubebanone (1), N-cis-3,4-methylenedioxycinnamoyl-3-methoxytyramine (2), and 9,9'-O-di-(E)-feruloyl-(+)-secoisolariciresinol (3), together with 11 known ones (4-14). Compounds 1, 4, and 8-11 showed obvious in vitro anti-inflammatory activities against NO production in LPS-induced murine microglial (BV-2) cell line and RAW 264.7 macrophages. A cytotoxic evaluation showed that 2, 3, and 5-8 exhibited considerable inhibition against the growth of hepatocyte carcinoma (HepG2) cell line. These findings are evidence, to some extent, for the traditional medicinal application of L. cubeba, especially as folk medicine in the treatment of inflammation-related diseases.

[A phytochemical and pharmacological advance on medicinal plant Litsea cubeba (Lauraceae)].

Litsea cubeba is one of aromatic medicinal plant belonging to family Lauraceae. The roots, stems and fruits of L. cubeba have been widely applied as folk medicines in some districts in China for relieving rheumatism and cold, regulating Qi (meridian) to alleviate pain. Previous studies revealed that this species contains major alkaloids, in specific aporphines, and minor flavonoids, lignans as well. Related pharmacological investigations demonstrated its activities and clinical applications on cardiovascular diseases, anti-cancer, against rheumatoid arthritis, relieving asthma and anti-allergic effects, as anti-oxidants, and so on. As an effort for further exploration of this bioactive ingredients and potential drug development, this paper summarizes most phytochemical and pharmacological results. Further, future prospects are also included.

[Chemical constituents from a Tibetan medicine Meconopsis horridula].

A phytochemical investigation on the aerial parts of a Tibetan medicine Meconopsis horridula, by solvent extraction, repeated chromatographies on silica gel, Sephadex LH-20, and preparative TLC techniques, led to the isolation of 9 compounds. By spectroscopic analysis and comparison of its 1H and 13C-NMR data with those in literatures, their structures were identified as oleracein E(1), N-( trans-p-coumaroyl) tyramine (2), chrysoeriol (3), apigenin (4), hydnocarpin (5), p-coumaric acid glucosyl ester (6), stigmast-5-ene-3beta-ylformate (7), 3beta-hydroxy-7alpha-ethoxy-24beta-ethylcholest-5-ene (8), and beta-sitosterol (9), respectively, among which compounds 6-8 were isolated from the genus for the first time,and 1,3 were isolated from the species for the first time. A MTT method was applied to evaluate the cytotoxic activity of compounds 14 against the human hepatocellular liver carcinoma cell line (HepG2), and compound 1 showed significant cytotoxicity against HepG2,with its inhibitory rate of 52.2% at 10 micromol x L(-1).

Chemical investigation of the roots of Polygala sibirica L.

AIM: To investigate the chemical constituents of the roots of Polygala sibirica L. (Polygalaceae) METHOD: The isolation was performed by solvent extraction and various chromatographic techniques, including silica gel, Sephadex LH-20, ODS, semi-preparative HPLC, and preparative TLC. The chemical structures were elucidated based on extensive spectroscopic analysis, including HR-ESI-MS and 1D- and 2D-NMR spectroscopic data. RESULTS: A total of sixteen compounds, including five xanthones (5, 7-10), five saccharide esters (1, 3, 4, 12, 13), two flavonoids (14, 16), two triterpenoids (11, 15), one phenylpropanoid (6), and one benzophenone glycoside (2) were isolated. Their structures were determined as sibiricose A7 (1), sibiriphenone A (2), polygalatenoside A (3), polygalatenoside C (4), lancerin (5), 3, 4, 5-trimethoxycinnamic acid (6), 6-hydroxy-1, 2, 3, 7-tetramethoxyxanthone (7), 1, 3, 7-trihydroxy-2-methoxyxanthone (8), onjixanthone II (9), 1, 2, 3, 6, 7-pentamethoxyxanthone (10), presenegenin (11), 3'-O-3, 4, 5-trimethoxycinnamoyl-6-O-4-methoxy benzoyl sucrose (12), tenuifoliside C (13), 5, 3'-dihydroxy-7, 4'-dimethoxyflavonol-3-O-ß-D-glucopyranoside (14), tenuifolin (15), and rhamnetin 3-O-ß-D-glucopyranoside (16). CONCLUSION: Compounds 1 and 2 are two new compounds from P. sibirica.

[Alkaloids from roots and stems of Litsea cubeba].

A phytochemical investigation on the roots and stems of Litsea cubeba led to the isolation of seven isoquinolone alkaloids. By spectroscopic analysis and comparison of their 1H and 13C-NMR data with those in literatures, these alkaloids were identified as (+)-norboldine (1), (+)-boldine (2), (+)-reticuline (3), (+)-laurotetanine (4), (+)-isoboldine (5), (+)-N-methyl-laurotetanine (6), and berberine (7), respectively. Among them, 7 was isolated from the genus for the first time. The evaluation of these compounds showed weak anti-inflammatory activity against NO production in RAW 267.4 and BV-2 cells.

[Research progress of Ypsilandra thibetica, a medicinal plant of Liliaceae].

Ypsilandra thibetica belongs to the family Liliaceae. Its whole plant has the medicinal functions of heat-clearing and detoxifying, relieving congestion and other effects, and is used as the folk medicine to cure scrofula, dysuria embolism and other symptoms. Previous chemical studies revealed that its major and active ingredient is steroidal saponin. Up to now, more than fifty steroidal saponins, mainly composed of spirostan and furostanol types, have been described. Pharmacological and clinical studies have demonstrated that Y. thibetica has anti-tumor, uterine contractions, hemostatic and antibacterial activities, in particular for the treatment of a variety of gynecological hemorrhagic diseases. In an effort to provide references for the advanced research and development of this species, this paper summarized the research progress on its pharmacognosy, including botany and authentication, its isolated secondary metabolites, biological activities and pharmacological applications. In addition, some advantages of this species which could be potentially used as a substitute for Paridis Rhizoma, one of ingredients of the well-known drug "Yunnan Baiyao", together with the future prospect are also briefly included.