An efficient high-speed counter-current chromatography method for the preparative separation of sesquiterpenoids from the rhizomes of Cyperus rotundus L. combined with evaluation of the anti-inflammation activity in vitro and molecular docking.

Cyperus rotundus L. has been extensively used in ancient medication for the treatment of different disorders worldwide, in which sesquiterpenes are the most representative components. In this study, sesquiterpenes were effectively purified by two-dimensional counter-current chromatography in combination with continuous injection and inner-recycling mode with a solvent system of n-hexane/ethyl acetate/methanol/water (1:0.2:1:0.2, v/v/v/v). For one-dimension separation, continuous injection mode was used with three times injection and the inner-recycling mode was adopted for the separation of two mixtures for two-dimensional separation. Finally, four sesquiterpenoids, including scariodione (1), cyperenoic acid (2), scariodione (3), and α-cyperone (4), were obtained with purities over 98%. Mass spectrometry and nuclear magnetic resonance were applied to identify their structures. The results from the anti-inflammation effect with zebrafish demonstrated that cyperenoic acid exhibited stronger anti-inflammation activity. Molecular docking results suggested that cyperenoic acid possessed lower binding energies -9.4545 kcal/mol with 1CX2 to form formed hydrogen bond interaction with ARG120. In general, all the obtained findings proved that the strong anti-inflammation capacity of cyperenoic acid can have the potential of being adopted for treating diseases resulting from inflammation.

Ephedrae herba: A comprehensive review of its traditional uses, phytochemistry, pharmacology, and toxicology.

ETHNOPHARMACOLOGICAL RELEVANCE: Ephedrae herba (called Mahuang in China) is the dried herbaceous stem of Ephedra sinica Stapf, Ephedra intermedia Schrenk et C. A. Mey., and Ephedra equisetina Bge. Ephedrae herba has a long history of use as an herb, and it was originally recorded in Sheng Nong's herbal classic. Ephedrae herba has also been widely used as both medicine and food. In the clinic, Ephedrae herba is commonly used for treating colds, bronchial asthma, nasal congestion, and other diseases. AIM OF REVIEW: This review aims to provide a systematic summary on the traditional use, chemical constituents, pharmacological effects, clinical applications, quality control, toxicology, and pharmacokinetics of Ephedrae herba to provide a theoretical basis for further reasonable development of Ephedrae herba in clinical practice and creation of new drugs. MATERIALS AND METHODS: Information on Ephedrae herba was gathered from various sources, including the scientific databases including CNKI, PubMed, SciFinder and ScienceDirect, classical books on traditional Chinese herbal medicine, Ph.D. and M.Sc. dissertations; Baidu Scholar; and from different professional websites. RESULTS: Ephedrae herba is distributed in regions of China and other areas. Ephedra and its compound preparations can be used for colds, bronchial asthma, nasal congestion and other diseases. Approximately 281 chemical constituents have been isolated from Ephedrae herba, including alkaloids, flavonoids, tannins, polysaccharides, volatile oils, organic acids, and other compounds. Among these constituents, alkaloids and volatile oils are the most abundant and represent the major bioactive constituents. Ephedrae herba possesses multiple pharmacological activities, including diuretic effect, anti-allergic effect, blood pressure regulatory, anti-inflammatory effect, anti-oxidation effect and anti-viral effects. Ephedrine hydrochloride and pseudoephedrine hydrochloride are generally selected as indicators for the quantitative determination of Ephedrae herba. The maximum dosage of Ephedrae herba should not exceed 10 g. If overused, adverse reactions such as palpitations, sweating, irritability and insomnia will occur. CONCLUSIONS: Ephedrae herba is an ancient herbal medicine with a broad spectrum of pharmacological activities that has been used for thousands of years in China. It is one of the most commonly used herbal components of the TCM formulas. Hydrochloride and pseudoephedrine are the major bioactive constituents. However, there is a need to further understand the mechanisms of active components of Ephedrae herba. Future studies should perform an in-depth analyses of the pharmacokinetics and mechanisms of toxicity of Ephedrae herba. Quality standards should be developed to correspond to the various application methods to ensure the efficacy of drugs in actual treatment.

Evaluation of the antibacterial activity of Elsholtzia ciliate essential oil against halitosis-related Fusobacterium nucleatum and Porphyromonas gingivalis.

The broad-spectrum antimicrobial activity of Elsholtzia ciliate essential oil (ECO) has been previously reported, but its effectiveness against halitosis-causing bacteria such as Fusobacterium nucleatum and Porphyromonas gingivalis is not well understood. In this study, we investigated the bacteriostatic activity of ECO against planktonic cells and biofilms of F. nucleatum and P. gingivalis, as well as its ability to inhibit bacterial metabolism and production of volatile sulfur compounds (VSCs) at sub-lethal concentrations. Our findings revealed that ECO exhibited comparable activities to chlorhexidine against these oral bacteria. Treatment with ECO significantly reduced the production of VSCs, including hydrogen sulfide, dimethyl disulfide, and methanethiol, which are major contributors to bad breath. As the major chemical components of ECO, carvacrol, p-cymene, and phellandrene, were demonstrated in vitro inhibitory effects on F. nucleatum and P. gingivalis, and their combined use showed synergistic and additive effects, suggesting that the overall activity of ECO is derived from the cumulative or synergistic effect of multiple active components. ECO was found to have a destructive effect on the bacterial cell membrane by examining the cell morphology and permeability. Furthermore, the application of ECO induced significant changes in the bacterial composition of saliva-derived biofilm, resulting in the elimination of bacterial species that contribute to halitosis, including Fusobacterium, Porphyromonas, and Prevotella. These results provide experimental evidence for the potential clinical applications of ECOs in the prevention and treatment of halitosis.

Mutualist- and antagonist-mediated selection contribute to trait diversification of flowers.

Flowers are generally short-lived, and they all face a multidimensional challenge because they have to attract mutualists, compel them to vector pollen with minimal investment in rewards, and repel floral enemies during this short time window. Their displays are under complex selection, either consistent or conflicting, to maximize reproductive fitness under heterogeneous environments. The phenological or morphological mismatches between flowers and visitors will influence interspecific competition, resource access, mating success and, ultimately, population and community dynamics. To better understand the effects of the plant visitors on floral traits, it is necessary to determine the functional significance of specific floral traits for the visitors; how plants respond to both mutualists and antagonists through adaptive changes; and to evaluate the net fitness effects of biological mutualisms and antagonism on plants. In this review, we bring together insights from fields as diverse as floral biology, insect behavioral responses, and evolutionary biology to explain the processes and patterns of floral diversity evolution. Then, we discuss the ecological significance of plant responses to mutualists and antagonists from a community perspective, and propose a set of research questions that can guide the research field to integrate studies of plant defense and reproduction.

Stimuli-responsive charge-reversal nano drug delivery system: The promising targeted carriers for tumor therapy.

The stimuli-responsive charge-reversal nano drug delivery system (CRNDDS) for the treatment of tumors has attracted much attention as an effective drug delivery system. The charge-reversal nanocarriers are either uncharged or negatively charged under normal physiological environment; however, they acquire positive charged in tumor tissue microenvironment. The process of charge reversal from negative-to-positive results in not only quick drug release in acidic environment but also enhance the cellular uptake of drug through electrostatic absorptive endocytosis resulting in improvement of cancer therapeutic outcome. In this review, we discuss the recent advances in the study of charge-reversal nanocarriers that could control the distribution of drugs in response to specific stimuli, such as pH, reduced glutathione (GSH) concentration, enzyme concentration, light and thermal stimulation. The applications of CRNDDS in the tumor treatment was also analyzed and summarized.

Ameliorating effects of exogenous calcium on the photosynthetic physiology of honeysuckle (Lonicera japonica) under salt stress.

Calcium (Ca2+) plays pivotal roles in modulating plant growth, development and stress responses. This work was conducted to study the effects of 20 mM calcium on the biomass, malondialdehyde content, chlorophyll content, ion ratio, chlorophyll a fluorescence and gas-exchange parameters, gene expression of annual honeysuckle under 50, 100 and 200 mM NaCl. At the end of treatment, Na+ concentration was increased with the mounting salinity, but a higher ratio of K+/Na2+, Ca2+/Na+, Mg2+/Na+ were obtained after calcium addition. Salinity exerted an adverse effect on the dry weights and chlorophyll content, whereas CaCl2 played a positive role. Consistent with biomass reduction, the photosynthetic rate and stomatal conductance declined in leaves of honeysuckle exposed to elevated salinity. However, the extent of reduction was much less under CaCl2 combination treatments than one caused by NaCl treatments. Exogenous calcium also protects the photochemical activity of PSII by protecting reaction centre from inactivation and maintaining electron transport from QA- to QB-. Further, exogenous calcium promoted the overexpression of LHCB coding gene Cab and Rubisco large subunit coding gene rbcL under short-term stress. In conclusion, exogenous calcium was effective in improving the salt tolerance of honeysuckle in the photosynthetic base, thereby improving the growth of plants.