Do chromium-resistant bacterial symbionts of hyperaccumulator Callitriche cophocarpa support their host in phytobial remediation of water?

Callitriche cophocarpa Sendtn. is a macrophyte widely distributed in aquatic systems of the temperate climate zone and a known hyperaccumulator of chromium. Ten pure symbiotic bacterial isolates of C. cophocarpa were obtained and identified. Three of the isolates showed the highest resistance to Cr(VI): Microbacterium sp. (Ct1), Aeromonas sp. (Ct3) and Acinetobacter sp. (Ct6). Acinetobacter sp. (Ct6) was able to survive up to a concentration of 104 mg/L (2 mM). The isolates were also able to effectively detoxify Cr(VI) by reducing it to Cr(III). We tested whether inoculation of plants with a consortium consisting of Ct1, Ct3 and Ct6 affects: (1) the phytoextraction of chromium from leachates, (2) the physiological state of plants after Cr(VI) treatment. The solutions were landfill leachates and contained 10.7 mg/L of Cr(VI) - an amount 530 times exceeding the legal limits. We influenced the plants with Cr in two steps, each lasting for 10 days, first using mature shoots and then apical ones. The highest Cr content concomitant with the highest bioconcentration factor (BCF) were found in the inoculated plants: 1274 and 119 mg/kg dry mass (d.m.), respectively. The physiological status of the plants was assessed by biometric tests and advanced chlorophyll fluorescence analyses. The photosynthetic activity of mature shoots was influenced by Cr(VI) more negatively than that of young apical shoots. The inoculation with the bacterial consortium significantly reduced the negative effect of Cr(VI) on mature organs. In some cases the inoculated mature plants exhibited photosynthetic activity that was even higher than in the control plants. The results unequivocally show a beneficial effect of C. cophocarpa inoculation with the tested isolates resulting in a significant improvement of the phytoremediation properties of this aquatic chromium hyperaccumulator.

Globunoids A-D, undescribed bichalconoid and biflavanoids with α-glucosidase and α-amylase inhibitory activities from Knema globularia stems.

A bichalconoid, globunoid A (1) and three biflavanones, globunoids B-D (2-4), previously undescribed, were isolated from the stems of Knema globularia, along with fourteen known analogues 5-18. The chemical structures of 1-4 were elucidated by the comprehensive spectroscopic analysis including UV, IR, HRESIMS, and NMR; the absolute configurations were determined based on their NOESY data, DP4+ statistical analysis, and ECD calculation. Up to now, compounds 2 and 3 represent the first 3,3″-linked biflavanone structures. Among the isolated compounds, 2, 3, and 2,3-dihydrocalodenin B (6) potently inhibited α-glucosidase and α-amylase activities, with IC50 values in the range 1.1-7.5 µM. Furthermore, the most active compound 6 was found to be a non-competitive inhibitor against these two enzymes.

Phytochemical evaluation and exploration of some biological activities of aqueous and ethanolic extracts of two species of the genus Plantago L.

Plantago major L. and Plantago lagopus L. are cosmopolitan species, belonging to the Plantaginaceae family, used in traditional and modern medicine. In this study, a phytochemical evaluation of different aqueous and ethanolic extracts of leaves and roots of both species from the region of Beja in Tunisia was performed. Some biological activities, including antioxidant, anticancer and antibacterial were also done. LC-MS qualitative analysis revealed that the aqueous extracts of the roots of P. lagopus were richer in polyphenols, mainly flavonoids (Luteoline 7-rutinoside, Luteoline 7-rhamnoside) and hydroxycinnamic acids including caffeic acid, than the hydro-ethanolic extracts. Additionally, we identified for the first time the presence of salicylic acid in the hot aqueous extracts of roots of P. lagopus and its absence in the roots of P. major. The antioxidant activity of the extracts was assessed using cyclic voltammetry (CV), revealing that the voltammograms of leaf and root extracts from P. lagopus exhibited a higher antioxidant capacity compared to those of P. major. Antiproliferative activity, was determined against two-colon cancer cell lines, demonstrated that only the 12 h treatments with P. lagopus leaf and root aqueous and hydro-ethanolic extracts at low concentration were able to significantly reduce the colon carcinoma coli-2 (CaCo-2) cells proliferation. The antibacterial /antibiofilm activity was performed on yeast, Gram- negative and +positive bacterial strains. We demonstrated for the first time that ethanolic extracts of leaves and roots of P. lagopus have an inhibitory activity against Escherichia coli and Klebsiella pneumonia at MIC = 2 µg/mL for leaves and 4 µg/mL for roots.

A chromosome-level reference genome of an aromatic medicinal plant Adenosma buchneroides.

Adenosma buchneroides Bonati, belonging to the genus Adenosum (Plantaginaceae), is an aromatic medicinal plant and utilized in traditional Chinese medicine. It has been widely used as plant-based repellents to prevent vector-borne diseases. However, the lack of a reference genome limits the study of conservation management and molecular biology of A. buchneroides. Here, we generated a chromosome-level de novo genome assembly of A. buchneroides which is a high-quality chromosome-scale assembly of aromatic medicinal plant in Plantaginaceae. The genome has a total length of 442.84 Mb with scaffold N50 of 27.98 Mb and 95.55% of the genome assigned to 14 chromosomes. BUSCO assessment yielded a completeness score of 97.2%. Furthermore, we predicted 24,367 protein-coding genes, and 95.79% of them was functionally annotated. The chromosome-scale genome of A. buchneroides will be a significant resource for understanding the genetic basis and evolution of active components biosynthesis, which will facilitate further study and exploit of A. buchneroides.

Metals in Callitriche cophocarpa from small rivers with various levels of pollution in SW Poland.

The anthropogenic impact of metals on aquatic environments is a risk for biota, and thus their levels must be controlled. Callitriche cophocarpa Sendtn. belongs to a genus with a potential for accumulation of elevated metal levels. Thus, it may provide consolidated evidence of contamination. Therefore, the aim of this investigation was to determine Cd, Co, Cr, Cu, Fe, Mn, Ni, Pb and Zn in this species collected together with water and bottom sediments from rivers with various levels of pollution. Of these rivers, one less polluted and one more polluted was selected for the collection of C. cophocarpa for an experiment to compare its Cu and Zn concentration potential. Both metals were supplemented at concentrations 0.01, 0.02, 0.03, 0.05, 0.08 and 0.14 mg L-1 of Cu as CuSO4 × 5H2O and 0.4, 0.6, 0,9, 1,35, 2.03 and 3.04 mg L-1 of Zn as ZnSO4 × 7H2O, and in the binary design containing (mg·L-1) 0.01Cu + 0.4Zn, 0.02Cu + 0.6Zn, 0.03Cu + 0.9Zn, 0.05Cu + 1.4Zn, 0.08Cu + 2.03 Zn and 0.14Cu + 3.04Zn. The upper concentrations of Cr, Cu, Mn and Zn in C. cophocarpa shoots from both types of rivers as well as of Ni and Pb in shoots from more polluted rivers were higher than the values typical for toxicity thresholds with no visible harmful effects, which may indicate accumulation abilities of C. cophocarpa for these metals. Both roots and shoots of C. cophocarpa may be included in the group of macroconcentrators for bottom sediments with respect to Cd, Co, Cr, Cu, Fe, Mn, Ni and Zn and deconcentrators of Pb. Greater accumulation of most metals in roots than in shoots indicates their restricted mobility and translocation by C. cophocarpa to shoots. C. cophocarpa from the less polluted river and exposed to all experimental solutions contained significantly higher levels of Cu and Zn than that from the more polluted river exposed to identical experimental solutions. The plants collected from the more polluted river influenced by surplus of metals and living under chemical stress could probably limit further accumulation by developing a resistance mechanism. Cu and Zn contents in C. cophocarpa were higher when treated with separate metals than for binary treatment both in the more and less polluted river. Such research presenting the impact of a combination of metals could be important for understanding and explaining the interactions of these elements which may influence their bioavailability in nature as well as importance in the evaluation of the risk of environmental toxicity.

Seasonal and Circadian Evaluation of the Essential Oil of Dizygostemon riparius (Plantaginaceae), a Wild Flavoring Herb from East Maranhão, Brazil.

Dizygostemon riparius (Plantaginaceae) is an aromatic herbal species known as "Melosa", endemic to the Municipality of São Benedito do Rio Preto, East Maranhão state, Brazil. It has a refreshing and pleasant aroma and is used for food flavoring and controlling domestic animal parasites. This work aimed to evaluate the seasonal and circadian influence on the composition and production of essential oils (EOs) from D. riparius. The plant aerial parts were hydrodistilled, and the oils were analyzed by GC and GC/MS. The seasonal study was conducted from August 2019 to July 2020, and the circadian study in dry (November) and rainy (May) periods, at 6 am, 12 am, and 6 pm. The results showed that the medium EOs yield was 2.8 %, and the primary constituents (>2 %) were endo-fenchyl acetate (30.5-42.1 %) and endo-fenchol (31.6-37.4 %), (E)-caryophyllene (2.8-7.6 %), α-fenchene (3.3-6.5 %), p-cymene (0.7-4.5 %), and caryophyllene oxide (1.4-2.7 %). Yield and composition of EOs did not significantly correlate with the climatic parameters, but their seasonal percentages influenced their two main components due to precipitation and solar radiation environmental factors. Quantitative variability in the EOs composition during the dry and rainy seasons was observed in the circadian period. These data may be significant for the plant's economic use.

Phytochemical Analysis and Evaluation of the Antioxidant, Antiproliferative, Antibacterial, and Antibiofilm Effects of Globularia alypum (L.) Leaves.

Globularia alypum L. (GA) is a Mediterranean plant of the Globulariaceae family which is widely used in traditional Tunisian medicine. The main goal of this study was to evaluate the phytochemical composition, antioxidant, antibacterial, and antibiofilm activities, and the antiproliferative potential of different extracts of this plant. The identification and the quantification of the different constituents of extracts were determined using gas chromatography-mass spectrometry (GC-MS). The antioxidant activities were evaluated using spectrophotometric methods and chemical tests. The antiproliferative study was based on the use of colorectal cancer SW620 cells, including an antibacterial assessment with the microdilution method and analysis of the antibiofilm effects via the crystal violet assay. All extracts presented several components, mainly sesquiterpenes, hydrocarbon, and oxygenated monoterpenes. The results revealed that the maceration extract had the most important antioxidant effect (IC50 = 0.04 and 0.15 mg/mL), followed by the sonication extract (IC50 = 0.18 and 0.28 mg/mL). However, the sonication extract demonstrated significant antiproliferative (IC50 = 20 µg/mL), antibacterial (MIC = 6.25 mg/mLand MBC > 25 mg/mL), and antibiofilm (35.78% at 25 mg/mL) properties against S. aureus. The results achieved confirm the important role of this plant as a source of therapeutic activities.

Genome assembly of the pioneer species Plantago major L. (Plantaginaceae) provides insight into its global distribution and adaptation to metal-contaminated soil.

Plantago is a major genus belonging to the Plantaginaceae family and is used in herbal medicine, functional food, and pastures. Several Plantago species are also characterized by their global distribution, but the mechanism underpinning this is not known. Here, we present a high-quality, chromosome-level genome assembly of Plantago major L., a species of Plantago, by incorporating Oxford Nanopore sequencing and Hi-C technologies. The genome assembly size was approximately 671.27 Mb with a contig N50 length of 31.30 Mb. 31,654 protein-coding genes were identified from the genome. Evolutionary analysis showed that P. major diverged from other Lamiales species at ~62.18 Mya and experienced two rounds of WGD events. Notably, many gene families related to plant acclimation and adaptation expanded. We also found that many polyphenol biosynthesis genes showed high expression patterns in roots. Some amino acid biosynthesis genes, such as those involved in histidine synthesis, were highly induced under metal (Ni) stress that led to the accumulation of corresponding metabolites. These results suggest persuasive arguments for the global distribution of P. major through multiscale analysis. Decoding the P. major genome provides a valuable genomic resource for research on dissecting biological function, molecular evolution, taxonomy, and breeding.

Comprehensive analysis of complete chloroplast genome sequence of Plantago asiatica L. (Plantaginaceae).

Plantago asiatica L. is a representative individual species of Plantaginaceae, whose high reputation is owed to its edible and medicinal values. However, the phylogeny and genes of the P. asiatica chloroplast have not yet been well described. Here we report the findings of a comprehensive analysis of the P. asiatica chloroplast genome. The P. asiatica chloroplast genome is 164,992 bp, circular, and has a GC content of 37.98%. The circular genome contains 141 genes, including 8 rRNAs, 38 tRNAs, and 95 protein-coding genes. Seventy-two simple sequence repeats are detected. Comparative chloroplast genome analysis of six related species suggests that a higher similarity exists in the coding region than the non-coding region, and differences in the degree of preservation is smaller between P. asiatica and Plantago depressa than among others. Our phylogenetic analysis illustrates P. asiatica has a relatively close relationship with P. depressa, which was also divided into different clades with Plantago ovata and Plantago lagopus in the genus Plantago. This analysis of the P. asiatica chloroplast genome contributes to an improved deeply understanding of the evolutionary relationships among Plantaginaceae.

A review on the traditional uses, phytochemistry, and pharmacology of the genus Veronicastrum (Plantaginaceae).

ETHNOPHARMACOLOGICAL RELEVANCE: Veronicastrum Heist. ex Fabr. (Plantaginaceae) is a multifunctional plant in China and other parts of the continent. It has traditionally been used in the treatment of ascites, edema, blood stasis, pain relief, chronic nephritis injury, fever, cough, headache, arthritis, dysentery, rheumatism, pleural effusion, liver damage, and other disorders. Although research has confirmed that the genus Veronicastrum contain many active compounds, no review of its traditional uses, phytochemistry or pharmacology has been conducted to date. AIM: This review aims to systematically evaluate the traditional uses, phytochemistry, and pharmacology of the genus Veronicastrum, discuss its medicinal potential, modern scientific research, and the relationship between them, and put forward some suggestions to promote further development and utilization of Veronicastrum. MATERIALS AND METHODS: The traditional uses, phytochemical and pharmacological data related to the genus Veronicastrum from 1955 to date was compiled by surveying the ethnomedicinal books and published papers, and searching the online databases including Google Scholar, China National Knowledge Infrastructure (CNKI), Science Direct, Web of Science and World Flora Online. RESULTS: Species of the genus Veronicastrum are widely used in folkloric medicine and some of their uses have been confirmed in modern pharmacological activities. A total of 89 chemical constituents have been isolated from the genus Veronicastrum, including flavonoids, carbohydrates, iridoids, terpenoids, phytosterols, phenolic acids, and other constituents. Among the compounds isolated, iridoids, flavonoids, and terpenoids are responsible for the biological activities of this genus with significant pharmacological activities both in vitro and in vivo. The extracts and compounds isolated from this genus have been reported to contain a wide range of pharmacological activities such as immunosuppressive, antioxidant, anti-cancer, anti-inflammatory, gastro protective, and antimicrobial activity. CONCLUSION: The genus Veronicastrum is not only a great herbal remedy, but also has numerous bioactive chemicals with potential for new drug discovery. In the literature, phytochemical investigations have been undertaken on five species. Detailed scientific research is still needed to fully understand this genus. Furthermore, its bioactive chemicals' structure-activity connection, in vivo activity, and mechanism of action ought to be investigated further.

Globularia arabica Methanolic Leaf Extract Has Higher Efficacy on Burn Wound Healing in Diabetic Rats Compared to Malva slyvestries Methanolic Leaf Extract.

This study aimed to see how effective Globularia arabica and Malva slyvestries-based cream formulations were at healing scald burn wounds in rats. Depending on ointment, preparations of 1%, 5%, and 10% w/w were created. For comparison, an ointment base and a regular burn cream composed soframycine were utilized. Rats introduced a burn by solidifying equipment at 100°C on a 14-mm2 shaved dorsal region. A deep second-degree burn was created, and the percentage of wound contraction was measured over the next 15 days. The rats were euthanized on days 8 and 15, and histological slides were prepared using hematoxylin and eosin staining. Compared to the control group, there was a substantial increase in wound contraction and a significant decrease in the duration of epithelialization in the based ointment-treated groups. However, as paralleled to Globularia arabica, significant (P < .05) results were observed with 10% Globularia arabica cream, whereas Malva slyverstries indicate minimal healing. Soframycine causes a substantial increase in wound contraction (P < .05). Soframycine cream with 10% Globularia arabica therapy resulted in practically complete re-epithelialization and re-structuring of wound tissue on histological examination, whereas Malva slyversries treatment resulted in low epithelization during treatment days. The findings suggest that Globularia arabica-based cream has the wound-healing capability.

Chemical profiling of Dizygostemon riparius (Plantaginaceae) plant extracts and its application against larvae of Aedes aegypti L. (diptera: culicidae).

Dengue fever is a reemerging disease of global concern among health authorities due to its high rate of proliferation. In 2019, Brazil registered its second-highest dengue mortality rate since 1998, with approximately 754 deaths and 1.5 million probable cases. Brazilian Ministry of Health prevention and control strategies for Aedes include insecticides, eradication of breeding sites, and awareness campaigns. However, as new mosquito variants resistant to conventional insecticides emerge, there is an increasing demand for effective environment-friendly plant extracts and natural substances against adult mosquitos and/or larvae of Aedes aegypti L. with no negative impacts on human health. This study aimed to investigate the larvicidal activity of Dizygostemon riparius extracts and analyze its chemical profile for the first time. Dizygostemon is a Plantaginaceae bytipic genus and D. riparius is an aromatic plant recently identified in Maranhão, Brazil. The essential oil from its lilac morphotype already exhibited larvicidal potential against Aedes albopictus, but the still limited data on this new plant species require further chemical and biological studies on other species, such as Aedes aegypti. Ethyl acetate and methanol crude leaf extracts yielded, respectively, 17.60 and 25.96%. High-performance liquid chromatography (HPLC) with UV detection coupled with electrospray ionization mass spectrometry (HPLC-UV-ESI-IT/MS) analyses confirmed the presence of polymethoxyflavones and coumarins, such as isorhamnetin 3-galactoside-7-rhamnoside, 5,7-dihydroxy-3-(3-hydroxy-4,5-dimethoxyphenyl)-6-methoxy-4-benzopyrone and 3',5-dihydroxy-4',6,7-trimethoxyflavone. Ethyl acetate extract presented the best performance in larvicide bioassays (LC50 = 542.2 ± 11.5 µg.mL-1). Our results highlight the chemical and biological potential of this new species found in the cerrado of eastern Maranhão and open perspectives for future studies focusing on isolating and identifying other active secondary metabolites of Dizygostemon riparius.

Characterization of Polyphenolic Compounds from Bacopa procumbens and Their Effects on Wound-Healing Process.

Wounds represent a medical problem that contributes importantly to patient morbidity and to healthcare costs in several pathologies. In Hidalgo, Mexico, the Bacopa procumbens plant has been traditionally used for wound-healing care for several generations; in vitro and in vivo experiments were designed to evaluate the effects of bioactive compounds obtained from a B. procumbens aqueous fraction and to determine the key pathways involved in wound regeneration. Bioactive compounds were characterized by HPLC/QTOF-MS, and proliferation, migration, adhesion, and differentiation studies were conducted on NIH/3T3 fibroblasts. Polyphenolic compounds from Bacopa procumbens (PB) regulated proliferation and cell adhesion; enhanced migration, reducing the artificial scratch area; and modulated cell differentiation. PB compounds were included in a hydrogel for topical administration in a rat excision wound model. Histological, histochemical, and mechanical analyses showed that PB treatment accelerates wound closure in at least 48 h and reduces inflammation, increasing cell proliferation and deposition and organization of collagen at earlier times. These changes resulted in the formation of a scar with better tensile properties. Immunohistochemistry and RT-PCR molecular analyses demonstrated that treatment induces (i) overexpression of transforming growth factor beta (TGF-ß) and (ii) the phosphorylation of Smad2/3 and ERK1/2, suggesting the central role of some PB compounds to enhance wound healing, modulating TGF-ß activation.

α-Glucosidase Inhibitors from the Stems of Knema globularia.

Six new compounds, globunones A-F (1-6), and two new flavonoids (7 and 8) together with nine known compounds (9-17) were isolated from the stems of Knema globularia. The chemical structures of 1-8 were elucidated by an analysis of their NMR and high-resolution electrospray ionization mass spectrometry data as well as by comparison with literature values. The absolute configurations were determined using time-dependent density functional theory electronic circular dichroism (TD-DFT-ECD). Globunones A-E (1-5) represent the initial combined structures of a flavan-3-ol core and a 1,4-benzoquinone core. Globunone F (6) is the first flavanone-type compound bearing a 2-(2,4-dihydroxyphenyl)-2-oxoethyl group found to date in Nature. Compounds 1-3 and 6-17 were tested for their yeast α-glucosidase inhibitory activity. All compounds tested (except for 13 and 14) showed potent inhibition toward α-glucosidase with IC50 values in the range 0.4-26.6 µM. Calodenin A (15) was the most active compound with an IC50 value of 0.4 µM (the positive control, acarbose, IC50 93.6 µM). A kinetic analysis of 15 revealed that it is a noncompetitive inhibitor with a Ki value of 3.4 µM.

In vitro and in vivo wound healing activities of Globularia arabica leaf methanolic extract in diabetic rats.

AIM: This study assessed the effects of topical application of the plant Globularia arabica extract on the diabetic rate of wound closure. METHODS: The effect of methanol extracts of G. arabica leaf extract on pro-inflammatory and anti-inflammatory cytokines, as well as the rate of wound contraction, hydroxyproline, and collagen content, was examined using an excision model of wound repair in male rats. RESULTS: The healing pattern was also highly related to using 10% plant extract and significantly, (p-values <0.025) increased wound contraction and increased hydroxyproline and collagen expression in both non-diabetic and diabetic rats, demonstrating that G. arabica extract possesses potent wound healing capacity. During the early wound healing phase, IL-6 levels were found to be upregulated by G. arabica treatment. Increased wound contraction augmented hydroxyproline and collagen content, supporting the early wound healing exhibited by G. arabica. One of the ways for speeding wound healing may be the induction of cytokine production. The result of our study shows that the fibroblast cell line treated with 20 µg/ml methanolic extract of G. arabica significantly (p-values <0.035) increases the cell migration that indicated the high wound healing activity. CONCLUSION: Results suggest that G. arabica may be useful in the topical management of wound healing.

The R2R3-MYB gene CgMYB4 is involved in the regulation of cell differentiation and fiber development in the stamens of Chelone glabra L.

A Plantaginaceae flowering plant, Chelone glabra, is different from Arabidopsis thaliana and cotton (Gossypium hirsutum), as it produces fibers on the anther surface. However, the evolutionary molecular mechanism of how fiber development is controlled in the stamen is unclear. MYB genes are essential transcription factors for trichome and fiber development in plants. In this study, we isolated 29 MYB domain-containing sequences using early-stage anthers and several sets of degenerated primers conserved in the R2R3 domain of the MYB transcription factor. Among them, CgMYB4 is an R2R3-MYB gene encoding 281 amino acids. Phylogenetic analysis showed that CgMYB4 is closely related to GhMYB25L/AmMIXTA, which controls fiber initiation and development in cotton and epidermal cell differentiation in the petals of Antirrhinum. Semiquantitative RT-PCR analysis showed that CgMYB4 is strongly expressed at the stamens and carpels. Overexpression of CgMYB4 significantly enhanced root hair formation in transformed hairy roots, contrary to the root hair numbers, which were reduced in silenced CgMYB4 hairy roots. Moreover, overexpression of CgMYB4 also evidently promoted fiber development at filaments and conical cell-like epidermal cell increases at the anther wall. Our results showed that CgMYB4 is an R2R3-MYB gene and is positively involved in regulating cell division and fiber differentiation in the early stages of stamen development in C. glabra.

Antibacterial and antibiofilm activity of Lagotis brachystachya extract against extended-spectrum ß-lactamases-producing Escherichia coli from broiler chickens.

Lagotis brachystachya Maxim (L. brachystachya) is an herb widely used in traditional Tibetan medicine. In the present study, the antibacterial activity of L. brachystachya extract to extended-spectrum-lactamases (ESBLs)-producing E. coli was determined by Kirby-Bauer disc diffusion, minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs) methods as well as time-kill curve assay. Meanwhile, the biofilm inhibition and eradication effects of L. brachystachya extract on the ESBLs-producing E. coli were evaluated by crystal violet staining, and further confirmed by confocal laser scanning microscope (CLSM) and scanning electron microscopy (SEM). The results indicated that L. brachystachya extract exhibited moderate antibacterial activity, with diameter of inhibition zones varying from 15.4 to 20.3 mm, and the MIC and MBC values were 6.25 to 25 mg/mL and 12.5 to 100 mg/mL, respectively. Time-kill curve showed that 4 × MIC level of L. brachystachya extract concentration of was able to kill 99.9% of ESBLs-producing E. coli after 16 h treatment. The biofilm inhibition rate and eradication rate for the ESBLs-producing E. coli were 35.66 to 79.91% and 22.18 to 56.21% at MIC level of extract concentration, respectively. CLSM images showed that the biofilm became thinner as the ESBLs-producing E. coli isolate exposed to L. brachystachya extract with a concentration-dependent manner from 1/4 × MIC to MIC compared with the control isolate. SEM images indicated that L. brachystachya extract at 1/2 × MIC and MIC levels could evidently inhibit the biofilm formation or eradicate the mature biofilms. The effect of L. brachystachya highlights its potential of antibacterial and antibiofilm activities against the ESBLs-producing E. coli.

A new diarylhexane and two new diarylpropanols from the roots of Knema globularia.

A new diarylhexane, kneglobularone B (1) and two new diarylpropanols, kneglobularols A - B (2 - 3) along with seven known compounds (4 - 10) were isolated and characterized from the roots of Knema globularia. It is the first time to find arylpropyl quinone (4) and isoflavone (8) in Myristicaceae family. In addition, 5 was found for the first time in Knema genus. Their structures were elucidated by UV, IR, MS, 1 D and 2 D NMR techniques. Compound 4 exhibited strong cytotoxicity against the NCI - H187 and MCF - 7 cell lines with IC50 values of 3.08 and 6.68 µg/mL, respectively.

Chemical constituents from the Knema globularia fruits and their in vitro cytotoxicity.

Two new compounds, designated as knecorticosanones A-B (1-2), along with three known compounds (3-5) were isolated from the fruits of Knema globularia. Their structures were elucidated by extensive spectroscopy analysis, including 1D- and 2D-NMR, UV, IR, and HRESIMS and by comparison with the reported data in the literature. Compounds 1-5 were evaluated for their cytotoxicity. Knecorticosanone B (2) and malabaricone D (5) exhibited moderate cytotoxic effect against Hep-G2, MCF-7 and SK-LU-1 cell lines with IC50 values ranging from 8.76 ± 1.02 to 18.74 ± 1.75 µM while knecorticosanone A (1), virolane (3) and 7-hydroxy-3',4'-methylenedioxyflavan (4) exhibited weak inhibitory effect against these cell lines with IC50 values ranging from 25.85 ± 2.75 to 66.75 ± 2.08 µM.

Anti-obesity, anti-hyperglycaemic, anti-antipyretic and analgesic activities of Globularia alypum extracts.

OBJECTIVES: The aim of this study is to evaluate the anti-obesity, anti-hyperglycaemic, analgesic and antipyretic activities of Globularia alypum (GA). MATERIALS AND METHODS: GA methanol and water extracts (GAME, GAWE) were administered to high-fat-high-glucose diet (HFFD) rats. RESULTS: This study showed that GAME exhibited the highest antioxidant, anti-α-amylase and anti-lipase activities, with half inhibitory concentration (IC50) values 0.067, 1.05 and 2.97 mg/ml respectively. In HFFD rats, the administration of GAME inhibited lipase activity by 36, 37 and 30% in the intestine, pancreas and serum, respectively, reduced body weight by 17.7% and modulated lipid profile. In addition, administration of GAME to HFFD-rats decreased α-amylase activity, improved glucose level and protected liver function. Furthermore, the administration of GA extracts to rats revealed antipyretic (reduction in writhing by 64%) and analgesic (decrease of temperature by 1.11 °C) activities. CONCLUSION: This study showed that GA extracts exhibited an anti-obesity, anti-hyperglycaemia, anti-pyretic and analgesic activities.