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Two new (1 and 2) compounds, together with five known (3–7) chromone derivatives, were isolated from the whole plants of Cassia pumila. Their structures were elucidated by spectroscopic methods, including extensive 1D and 2D NMR techniques. Compounds 1–7 were evaluated for their anti-methicillin-resistant Staphylococcus aureus (anti-MRSA) activity. The results revealed that compounds 1, 2, 5, and 6 showed good inhibition with IZD of 13.4 ± 2.5, 12.2 ± 2.0, 14.6 ± 2.2, and 14.2 ± 2.6 mm, and compounds 3, 4, and 7 showed weak inhibition with IZD of 10.7 ± 2.2, 11.3 ± 2.0, and 10.8 ± 2.1 mm, respectively. [ABSTRACT FROM AUTHOR]

Two new naphthalene derivatives, 1-(3-hydroxy-1-(hydroxymethyl)-2-methoxy-6-methylnaphthalen-7-yl) propan-2-one (1) and 1-(3-hydroxy-1-(hydroxymethyl)-6-methylnaphthalen-7-yl)propan-2-one (2), together three known naphthalene derivatives (3–5) were isolated from the fermentation products of the endophytic fungus Phomopsis fukushii. Their structures were elucidated by spectroscopic methods, including extensive 1D and 2D NMR techniques. Compounds 1 and 2 were evaluated for their anti-methicillin-resistant Staphylococcus aureus (anti-MRSA) activity. The results showed that compounds 1 and 2 showed weak inhibition with IZD of 10.2 ± 1.8 and 11.3 ± 2.0 mm, respectively. [ABSTRACT FROM AUTHOR]

Two new pentenyl coumarins (1 and 2), together with three known pentenyl coumarins (3–5), were isolated from the roots and stems of Nicotiana rustica. Their structures were elucidated by spectroscopic methods, including extensive 1D and 2D NMR techniques. Compounds 1–5 were tested for their anti-rotavirus activity. The results revealed that compounds 1–5 exhibited potent anti-rotavirus activity with therapeutic index (TI) value in the range of 11.1–15.7. [ABSTRACT FROM AUTHOR]

Two new (1 and 2) and two known arylbenzofuran lignans (3 and 4) were isolated from the seeds of Arctium lappa. Their structures were elucidated by spectroscopic methods, including extensive 1D and 2D NMR techniques. Compounds 1–4 were evaluated for their anti-methicillin-resistant Staphylococcus aureus (anti-MRSA) activity. The results revealed that compound 3 showed good inhibition with IZD of 13.5 ± 1.5 mm), and compounds 1, 2, and 4 showed weak inhibition with IZD of 9.6 ± 1.0, 11.6 ± 1.2, and 10.8 ± 1.2 mm, respectively. Compounds 1–4 were also tested for the antioxidant activity, and they show good antioxidant activity with an IC50 values of 4.38, 4.22, 3.96, and 4.15 μg/mL, respectively. [ABSTRACT FROM AUTHOR]

Two new isoflavones, 4′,6-dimethoxy-8-hydroxy-7-hydroxymethylisoflavone (1) and 4′,8-dihydroxy-7-hydroxymethyl-6-methoxyisoflavone (2), together with three known isoflavones (3-5), were isolated from Pueraria lobata. Their structures were elucidated by spectroscopic methods, including extensive 1D and 2D NMR techniques. Compounds 1-5 were evaluated for their anti-tobacco mosaic virus (anti-TMV) activities. The results showed that compound 2 exhibited high anti-TMV activity with inhibition rates of 32.6%. The other compounds also showed potential anti-TMV activities with inhibition rates in the range of 21.4-25.3%, respectively. The cytotoxic activity of compounds 1-5 against five human tumor cell lines (NB4, A549, SHSY5Y, PC3, and MCF7) was also tested. The results revealed that compounds 1-5 showed weak inhibitory activities against some human tumor cell lines, with IC50 values in the range of 6.9-9.8 μM. [ABSTRACT FROM AUTHOR]

Nicotiana tabacum (tobacco) has attracted interest as one of the most economically important industrial crops widely cultivated in China, whose dried leaves are popularly consumed medicinally and recreationally by human societies. In this study, five undescribed alkaloids derivatives, isoaspergillines A–E, together with eight known alkaloids, notoamide D, (1 R ,4 S)-4-benzyl-1-isopropyl-2,4-dihydro-1H-pyrazino-[2,1- b ]quinazoline-3,6-dione, protuboxepin K, notoamide C, notoamide M, deoxybrevianamide E, cyclo (D-Pro-L-Trp), and versicolamide B, were obtained from the culture of the Nicotiana tabacum -derived fungus Aspergillus versicolor. Their structures were mainly elucidated through comprehensive analyses of spectroscopic data. Bioactivity evaluation of all isolated compounds revealed that isoaspergilline A and notoamide M exhibited anti-TMV activities with IC 50 values of 20.0 and 22.8 μM, respectively. Molecular docking suggested that isoaspergilline A and notoamide M were well located into the active site of anti-TMV by interacting with SER138, SER143, and ASN73 residues. This study enlightens the therapeutic potential of the endophytic fungus A. versicolor and it is helpful to find undescribed anti-TMV activity inhibitors, as well as searching for new anti-TMV candidates from natural sources. [Display omitted] • Isoaspergilline A was an unusual tetrasubstituted indole core, and two isoprenyl groups. • Bioactivity evaluation of all compounds revealed that isoaspergilline A and notoamide M possess anti-TMV activities with IC 50 values 20.0, 22.8 μM, respectively, positive control (IC 50 = 36.1 μM). • Molecular docking suggested that isoaspergilline A and notoamide M were well located into the active site of anti-TMV by interacting with SER138, SER143, and ASN73 residues. [ABSTRACT FROM AUTHOR]

An Hg2+-selective fluorescent sensor ( 1) bearing pyrene as a fluorophore was synthesized. A sandwich-stacking binding mode was formed during the binding process, which increased the excimer fluorescence 22-fold at 490 nm. Compound 1 was successfully applied in in vivo imaging to trace the enrichment and distribution of mercury in the nervous system, digestive system, and reproductive system of Caenorhabditis elegans, as well as the organs of zebrafish. [ABSTRACT FROM AUTHOR]

Abstract: A 1,8-naphthalimide derivative (1) was intentionally designed and synthesized as a new turn-on fluorescent probe for the detection of zinc ion with high selectivity over other metal ions at pH 7.4 in aqueous media (CH3CN/HEPES, V/V=6:4). The reaction mechanism is attributed to the replacement of the protons of the O–H groups by zinc ion at the binding site and production of fluorescence which is blocked in the photo-induced electron transfer (PET) process. Remarkable enhancement of up to 13-fold in fluorescence intensity with a 38nm red-shift was achieved in the detection of zinc ion. Compound 1 was successfully applied to the fluorescence imaging of zinc ion, with a fluorescence emission color produced in the cell nucleus different from that produced in the cytoplasm, in A549, BEAS-2B, CHO, Hela, and HepG2 cells. Furthermore, cytokinesis-block micronucleus (CBMN) assay was carried out in CHO cells using 1 and zinc ion as the imaging agents, showing that the 1-Zn2+ agent is a nucleic acid selective stain, which could be applied in MN assays in different kinds of cell lines. [Copyright &y& Elsevier]

Two new benzo[c]azepin-1-ones, 2,3-dihydro-8-(3-hydroxypropyl)-4-methoxy-7-methylbenzo[c]azepin-1- one (1) and 2,3-dihydro-6-(hydroxymethyl)-8-(3-hydroxypropyl)-4-methoxybenzo[c]azepin-1-one (2), were isolated from the whole plants of Thalictrum glandulosissimum. Their structures were determined by means of HR-ESI-MS and extensive 1D and 2D NMR spectroscopic studies. Compounds 1 and 2 were tested for their antibacterial activity. The results showed that both compounds had high antibacterial activity against 12 microbial strains isolated from the saliva of smokers. [ABSTRACT FROM AUTHOR]

Two new isochromenes, 5-methoxy-3-methyl-7-prenyl-1H-isochromene (1) and 7-(3-hydroxypropyl)-5-methoxy-3-methyl-1H-isochromene (2), along with four known ones (3–6) were isolated from the fermentation products of the Nicotiana tabacum-derived endophytic fungus Aspergillus versicolor. Their structures were elucidated by spectroscopic methods, including extensive 1D and 2D NMR techniques. Compounds 1 and 2 were evaluated for their anti-tobacco mosaic virus (anti-TMV) and anti-methicillin-resistant Staphylococcus aureus (anti-MRSA) activities. The results showed that compounds 1 and 2 exhibited potential anti-TMV activities with inhibition rates of 36.5 and 42.2%, respectively, and also showed good anti-MRSA activities with IZD of 16.8 ± 2.2 and 20.6 ± 2.5 mm, respectively. [ABSTRACT FROM AUTHOR]

Two new indole alkaloids, 6-(4-methoxyphenoxy)-4-methoxy-2-methyl-1H-indole (1) and 6-(3,5-dimethoxyphenoxy)-4-methoxy-2-methyl-1H-indole (2), along with four known ones (3–6), were isolated from the fermentation products of the cigar tobacco-derived endophytic fungus Aspergillus oryzae. Their structures were elucidated by spectroscopic methods, including extensive 1D and 2D NMR techniques. Compounds 1 and 2 were evaluated for their antibacterial and antioxidant activities. The results showed that compounds 1 and 2 exhibited good anti-methicillin-resistant Staphylococcus aureus (anti-MRSA) activity with IZD of 22.4 ± 2.4 and 24.6 ± 2.2 mm, respectively. [ABSTRACT FROM AUTHOR]

Two new anthraquinones, 2′,6-dimethyl-7-methoxy-[2,3-b]furan-anthraquinone (1) and 1,7-dimethoxy-2′,6-dimethyl-[2,3-b]furan-anthraquinone (2), were isolated from the fermentation products of the cigar tobacco-derived endophytic fungus Aspergillus versicolor. Their structures were elucidated by spectroscopic methods, including extensive 1D and 2D NMR techniques. Compounds 1 and 2 were evaluated for their antibacterial and antioxidant activities. The results showed that compounds 1 and 2 demonstrated strong anti-methicillin-resistant Staphylococcus aureus (anti-MRSA) activities with an inhibition zone diameter of 16.4 ± 2.2 and 18.5 ± 2.5 mm, respectively. Compounds 1 and 2 also showed good antioxidant activities, with IC50 values of 4.05 and 3.94 μg/mL, respectively. [ABSTRACT FROM AUTHOR]

Two new (1 and 2), together with two known (3 and 4), quinoline alkaloids were isolated from the stems of Nicotiana tabacum. Their structures were elucidated using spectroscopic methods, including extensive 1H, 13C, and 2D NMR techniques. Compounds 1 and 2 were tested for their anti-tobacco mosaic virus (anti-TMV) activity. The results showed that compounds 1 and 2 exhibited potential anti-TMV activity with inhibition rates of 28.2 and 25.8% respectively. [ABSTRACT FROM AUTHOR]

Two new chromeno[3,2-c]pyridine alkaloids, 9-acetyl-7-methoxy-3-methyl-10H-chromeno[3,2-c]pyridin- 10-one (1) and 8-acetyl-7-methoxy-3-methyl-10H-chromeno[3,2-c]pyridin-10-one (2), were isolated from the whole plants of Thalictrum scabrifolium. Their structures were determined by means of HR-ESI-MS and extensive 1D and 2D NMR spectroscopic studies. Compounds 1 and 2 were tested for their antibacterial activity. The results showed that both compounds showed high antibacterial activity against 12 microbial strains isolated from the saliva of smokers. [ABSTRACT FROM AUTHOR]

Two new anthraquinones, 2,6-dimethyl-3-hydroxy-5-methoxyanthraquinone (1) and 2,5-dimethyl-6-hydroxy-3-methoxyanthraquinone (2), were isolated from the twigs of Cassia alata. Their structures were determined by means of HR-ESI-MS and extensive 1D and 2D NMR spectroscopic studies. Compounds 1 and 2 were tested for their antibacterial activity. The results showed that both compounds exhibited high antibacterial activity against 11 microbial strains isolated from the saliva of smokers. [ABSTRACT FROM AUTHOR]

Indole alkaloids have attracted widespread attention of chemists and biologists. Therefore, the aim of this study is to screen more bioactivities indole alkaloids from the microorganisms. In this study, five undescribed CPA-type indole alkaloids, aspergillines F–J, and three known CPA-type indole alkaloids, aspergilline A, aspergilline C, and cyclopiamide E, were obtained from the Nicotiana tabacum - derived fungus Aspergillus versicolor. Notably, aspergillines F and G represent the first examples of indole alkaloids with a benzo[ cd ]indol-2(1 H)-one skeleton, and aspergilline J is also the firstly obtained indole alkaloids bearing a N -1-(2-(1 H -imidazole-5-yl)ethyl) moiety. Aspergillines F–J and cyclopiamide E were tested for their anti-TMV activities, and the results revealed that aspergillines G and J exhibited obvious anti-TMV activities with inhibition rates of 41.2 and 56.8% at the concentration of 20 μ M, respectively. These rates are high than that of positive control (with inhibition rate of 32.5%). In addition, the molecular docking studies for the isolated CPA-type indole alkaloids may also reveal that the benzo[ cd ]indol-2(1 H)-one substructure is the fundamental for anti-TMV activity and the oxygen-containing substituent groups at C-19 also increases the inhibitory activity. This study of structure-activity relationship is helpful to find new anti-TMV activity inhibitors. Five undescribed CPA-type indole alkaloids were obtained from N. tabacum -derived fungus A. versicolor. Aspergillines G and J exhibited obvious anti-TMV activities. [Display omitted] • Five undescribed CPA-type alkaloids were obtained from fungus A. versicolor. • Aspergillines F and G represent the examples of benzo[ cd ]indol-2(1 H)-one skeleton. • Aspergilline J is the CPA alkaloids bearing a N -1-(2-(1 H -imidazole-5-yl)ethyl) moiety. • Aspergillines G and J exhibited obvious anti-TMV activities. [ABSTRACT FROM AUTHOR]

Two new isobenzofuranone derivatives (1 and 2) together with six known compounds (3–8) were isolated from the roots of Phlomis betonicoides, a highly sweet plant in China. Their structures were determined by means of HR-ESI-MS and extensive 1D and 2D NMR spectroscopic studies. Compounds 1–8 were tested for their anti-rotavirus activity. The results showed that compounds 1–8 exhibited potent anti-rotavirus activity with therapeutic index value 7.5–16.4. [ABSTRACT FROM AUTHOR]

Eight phenolic compounds (1–8), including two new compounds (1 and 2), were isolated from the twigs of Gardenia jasminoides. Their structures were determined by means of extensive 1D and 2D NMR spectroscopic studies. Compounds 1–4 were tested for their antimethicillin-resistant Staphylococcus aureus (anti-MRSA) activity. The results revealed that compounds 1–4 showed good inhibition with IZD of 12.2 ± 2.2, 13.8 ± 2.4, 15.2 ± 2.8, and 12.9 ± 2.5 mm, respectively. [ABSTRACT FROM AUTHOR]

Two new anthraquinones, 3-hydroxy-6-hydroxymethyl-2,5-dimethylanthraquinone (1) and 6-hydroxymethyl-3-methoxy-2,5-dimethylanthraquinone (2), were isolated from the fermentation products of the endophytic fungus Phomopsis sp. Their structures were elucidated by spectroscopic methods, including extensive 1D and 2D NMR techniques. Compounds 1 and 2 were evaluated for their antimethicillin-resistant Staphylococcus aureus activity. The results showed that compounds 1 and 2 showed good inhibition with IZD of 14.2 ± 2.0 and 14.8 ± 2.2 mm, respectively. Compounds 1 and 2 were also tested for antioxidant activity; they show good activity with IC50 values of 4.18 and 4.36 μg/mL, respectively. [ABSTRACT FROM AUTHOR]

Two new chromone derivatives (1 and 2), together with four known (3–6) ones, were isolated from the stems of a local sun cured tobacco (Fenghuang tobacco, widely cultivated in Shifang prefecture, Sichuan Province). Their structures were elucidated by spectroscopic methods, including extensive 1D and 2D NMR techniques. Compounds 1 and 2 were tested for their anti-tobacco mosaic virus (anti-TMV) activity. The results showed that compounds 1 and 2 exhibited high anti-TMV activities with inhibition rates of 35.8 and 28.6% at the concentration of 20 μM. These rates are close to that of the positive control. [ABSTRACT FROM AUTHOR]

Two new isobenzofurans, 5-(methoxymethyl)-2,2-dimethyl-2H-furo[3,4-h]chromen-7(9H)-one (1) and 5-(2-methoxyethyl)-2,2-dimethyl-2H-furo[3,4-h]chromen-7(9H)-one (2), together with two known isobenzofurans (3 and 4), were isolated from the roots of Yunnan local sun cured tobacco. Their structures were determined by means of HR-ESI-MS and extensive 1D and 2D NMR spectroscopic studies. Compounds 1–4 were tested for their anti-methicillin-resistant Staphylococcus aureus (anti-MRSA) activity. The results revealed that compound 4 showed strong inhibition with IZD of 16.5 ± 2.2. Compounds 1–3 also showed good inhibition with IZD of 13.6 ± 2.0, 14.0 ± 2.3, and 11.8 ± 1.6 mm, respectively. Compounds 1–4 were also tested for their antioxidant activity, and they showed good antioxidant activity with IC50 value of 4.38, 4.57, 4.46, and 4.28 μg/mL, respectively. [ABSTRACT FROM AUTHOR]

Two new furan-2-carboxylic derivatives (1 and 2), together with three known compounds (3–5), were isolated from the leaves of Nicotiana tabacum. Their structures were determined by means of HR-ESI-MS and extensive 1D and 2D NMR spectroscopic studies. Compounds 1 and 2 were tested for their anti-TMV activities. The results showed that compounds 1 and 2 exhibited high anti-TMV activity with inhibition rates of 33.2 and 30.8%. These rates are close to that of positive control. [ABSTRACT FROM AUTHOR]

Two new coumarins, 6-hydroxymethyl-3-prenyl-7-methoxycoumarin (1) and 6-hydroxyethyl-3-prenyl-7- methoxycoumarin (2), together with three known coumarins (3–5), were isolated from the roots and stems of Yunyan-300, a variety of Nicotiana tabacum L. Their structures were elucidated by spectroscopic methods, including extensive 1D and 2D NMR techniques. Compounds 1 and 2 were tested for their anti-methicillinresistant Staphylococcus aureus (anti-MRSA) activity and their antioxidant activity. The results revealed that compounds 1 and 2 showed good anti-MRSA inhibitions with IZD of 12.2 ± 1.8 and 11.8 ± 1.5 mm, respectively, and antioxidant activity with an IC50 value of 4.65 and 4.85 μg/mL, respectively. [ABSTRACT FROM AUTHOR]

Two new tricyclic alkaloids (1 and 2), together with three known (3–5) alkaloids, were isolated from the whole plants of Thalictrum cultratum. Their structures were determined by means of HR-ESI-MS and extensive 1D and 2D NMR spectroscopic studies. Compounds 1–5 were tested for their anti-rotavirus activity. The results revealed that compounds 1–5 exhibited potent anti-rotavirus activity with therapeutic index (TI) values in the range 10.7–17.7. [ABSTRACT FROM AUTHOR]

Two new isoquinoline alkaloids, 3-hydroxy-1-(7-hydroxy-6-methylisoquinolin-1-yl)propan-1-one (1) and 3-hydroxy-1-(7-methoxy-6-methylisoquinolin-1-yl)propan-1-one (2) were isolated from the whole plants of Thalictrum glandulosissimum. Their structures were determined by means of HR-ESI-MS and extensive 1D and 2D NMR spectroscopic studies. Compounds 1 and 2 were tested for their anti-tobacco mosaic virus (anti-TMV) activity. The two compounds showed weak anti-TMV activity with inhibition rates of 28.9 and 32.6%. These rates are close to that of positive control. [ABSTRACT FROM AUTHOR]

Two new chromone derivatives, 5-(isobutyryl)-2-(2-oxopropyl)-7-methoxy-4H-chromen-4-one (1) and 5-(isobutyryl)-2-(2-oxopropyl)-6-methoxy-4H-chromen-4-one (2), were isolated from Cassia nomame. Their structures were elucidated by spectroscopic methods, including extensive 1D and 2D NMR techniques. Compounds 1 and 2 were evaluated for their anti-tobacco mosaic virus (anti-TMV) activity. The results showed that compounds 1 and 2 showed potential anti-TMV activities with inhibition rates of 28.7% and 31.2%, at the concentration of 20 μM, respectively. These rates are close to that of positive control. [ABSTRACT FROM AUTHOR]

Two new flavones, 8,4′-dimethoxy-6-(2-oxopropyl)-flavone (1) and 8,4′-dimethoxy-6-(3-hydroxypropyl)- flavone (2), were isolated from the seeds of Arctium lappa. Their structures were elucidated by spectroscopic methods, including extensive 1D and 2D NMR techniques. Compounds 1 and 2 were evaluated for their anti-methicillin-resistant Staphylococcus aureus (anti-MRSA) activity. The results showed that compounds 1 and 2 exhibited weak active with diameter of inhibition zone (IZD) 10.8 ± 1.0 and 9.3 ± 0.8 mm, respectively. Compounds 1 and 2 were also tested for antioxidant activity, and they show good antioxidant activity with IC50 values of 3.85 and 3.47 μg/mL, respectively. [ABSTRACT FROM AUTHOR]

Three new diphenyl ethers (1-3), together with four known isopentylated diphenyl ethers derivatives (4-7), were isolated from the fermentation products of an endophytic fungus Phomopsis fukushii. Their structures were elucidated by spectroscopic methods, including extensive 1D and 2D NMR techniques. Compounds 1-3 were evaluated for their anti-methicillin-resistant Staphylococcus aureus (anti-MRSA) activity. The results revealed that compounds 1 and 2 showed strong inhibitions with inhibition zone diameters (IZD) of 20.2 ± 2.5 mm and 17.9 ± 2.2 mm, respectively. Compound 3 also showed good inhibition with IZD 15.2 ± 1.8 mm. The IZD data of compound 1 is close to that of positive control with IZD 21.9 ± 2.1 mm. [ABSTRACT FROM AUTHOR]

A 'turn-on' pattern Fe3+-selective fluorescent sensor was synthesized and characterized that showed high fluorescence discrimination of Fe3+ over Fe2+ and other tested ions. With a 62-fold fluorescence enhancement towards Fe3+, the probe was employed to detect Fe3+ in vivo in HeLa cells and Caenorhabditis elegans, and it was also successfully used to elucidate Fe3+ enrichment and exchange infected by innexin3 (Inx3) in hemichannel-closed Sf9 cells. [ABSTRACT FROM AUTHOR]

Abstract: A 1,8-naphthalimide–Cu(II) ensemble was rationally designed and synthesized as a new turn-on fluorescent probe utilizing the ‘chemosensing ensemble’ method for detections of thiols (Cys, Hcy and GSH) with high selectivity over other α-amino acids at pH 7.4 in organic aqueous media (EtOH/HEPES, v/v=9:1). The recognition mechanism was attributed to the remove Cu(II) from the 1,8-naphthalimide–Cu(II) ensemble by thiols and the release of flurescence of ligand 1. Remarkable fluorescence enhancements were therefore observed in the sensing process of thiols by the 1,8-naphthalimide–Cu(II) ensemble. Furthermore, the 1,8-naphthalimide–Cu(II) ensemble was successfully applied to the fluorescence imaging of thiols in CHO cells with high sensitivity and selectivity. [Copyright &y& Elsevier]