Delphinium uncinatum mediated biosynthesis of zinc oxide nanoparticles and in-vitro evaluation of their antioxidant,cytotoxic, antimicrobial,anti-diabetic,anti-inflammatory,and anti-aging activities

Nanotechnology is perhaps the most widely explored scientific domain in the current era. With the advent of NPs, revolutionary changes have been observed in various scientific disciplines. Among the NPs, ZnO-NPs are the center of contemplation owing to their biocompatible nature. These nanoparticles have been prepared using a number of techniques; however, biological methods are among the most popular synthesis approaches. The current research therefore reports the phyto-fabrication of ZnO-NPs mediated by Delphinium uncinatum root extract. The resulting NPs were subjected to standard characterization methods such fourier transformed infrared spectroscopy, X-ray diffraction and transmission electron microscopy. The resulting NPs are exploited to their possible antioxidant, antimicrobial, antidiabetic, cytotoxic, anti-inflammatory and anti-ageing potency. FTIR confirmed the capping of ZnO-NPs by a variety of phytochemicals. ZnO-NPs average size was approximately 30 nm. ZnO-NPs exhibited substantial bio-potency and proved to be highly biocompatible even at higher concentrations. ZnO-NPs revealed strong antimicrobial potency for Pseudomonas aeruginosa proving to be the most susceptible strain showing inhibition of 16 ± 0.98. ZnO-NPs also showed dose dependent antidiabetic and cytotoxic potential. COX-1, COX-2, 15-LOX and sPLA2 were efficiently inhibited upon exposure to ZnO-NPs confirming the anti-inflammatory potential of ZnO-NPs. Similarly, ZnO-NPs also revealed considerable anti-aging potential. With such diverse biological potentials, ZnO-NPs can prove to be a potent weapon against a plethora of diseases; however, further study is necessary in order to discover the precise mechanism that is responsible for the biological potency of these NPs.     

Variation on Composition and Bioactivity of Essential Oils of Four Common Curcuma Herbs

Chemical compositions, antioxidative, antimicrobial, anti‐inflammatory, and cytotoxic activities of essential oils extracted from four common Curcuma species (Curcuma longa, Curcuma phaeocaulis, Curcuma wenyujin, and Curcuma kwangsiensis) rhizomes in P. R. China are comparatively studied. In total, 47, 49, 35, and 30 compounds are identified in C. longa, C. phaeocaulis, C. wenyujin, and C. kwangsiensis essential oils by GC/MS, and their richest compounds are ar‐turmerone (21.67%), elemenone (19.41%), curdione (40.23%) and (36.47%), respectively. Moreover, C. kwangsiensis essential oils display the strongest DPPH (2,2‐diphenyl‐1‐picrylhydrazyl) radical‐scavenging activity (IC₅₀, 3.47 μg/ml), much higher than ascorbic acid (6.50 μg/ml). C. phaeocaulis oils show the best antibacterial activities against Escherichia coli (MIC, 235.54 μg/ml), Pseudomonas aeruginosa (391.31 μg/ml) and Staphylococcus aureus (378.36 μg/ml), while C. wenyujin and C. kwangsiensis oils show optimum activities against Candida albicans (208.61 μg/ml) and Saccharomyces cerevisiae (193.27 μg/ml), respectively. C. phaeocaulis (IC₅₀, 4.63 μg/ml) and C. longa essential oils (73.05 μg/ml) have the best cytotoxicity against LNCaP and HepG2, respectively. C. kwangsiensis oils also exhibit the strongest anti‐inflammatory activities by remarkably down‐regulating expression of COX‐2 and TNF‐α. Therefore, due to their different chemical compositions and bioactivities, traditional Chinese Curcuma herbs should be differentially served as natural additives for food, pharmaceutical, and cosmetic.     

The Gastrointestinal Tract Metabolism and Pharmacological Activities of Grosvenorine,a Major and Characteristic Flavonoid in the Fruits of Siraitia grosvenorii

Grosvenorine is the major flavonoid compound of the fruits of Siraitia grosvenorii (Swingle ) C. Jeffrey , a medical plant endemic to China. In the present study, for the first time, the grosvenorine metabolism in an in vitro simulated human gastrointestinal tract (including artificial gastric juice, artificial intestinal juice and intestinal flora), as well as its pharmacological activities (including anti‐complement, antibacterial and antioxidant activities), was investigated. The results showed that grosvenorine was metabolized by human intestinal flora; its four metabolites were isolated by semi‐preparative HPLC and identified by NMR as kaempferitrin, afzelin, α‐rhamnoisorobin, and kaempferol. Further pharmacological evaluation showed that grosvenorine exhibited good antibacterial and antioxidant activities, with its metabolites possessing more potent activities. Although grosvenorine did not present obvious anticomplement activity, its metabolites showed interesting activities. This study revealed that intestinal bacteria play an important role in the gastrointestinal metabolism of grosvenorine and significantly affect its pharmacological activities.     

Purification, antioxidant and moisture-preserving activities of polysaccharides from papaya

Polysaccharides extracted from papaya are a group of heteropolysaccharides, and their antioxidant activities and moisture-preserving activities were investigated employing various established in vitro systems. Available data obtained with in vitro models suggested that among the three samples, the second fraction (named after P2) showed significant inhibitory effects on superoxide, hydroxyl and DPPH radical; its reducing power was also the strongest. Data also reveal that P2 has strong in vitro moisture absorption and retention capacities as compared to hyaluronic acid and glycerol. These results clearly establish the possibility that polysaccharides extracted from papaya could be effectively employed as a type of natural moisturizer. However, comprehensive studies need to be conducted in experimental animal models.     

Laserpitium zernyi Hayek Flower and Herb Extracts: Phenolic Compounds,and Anti‐edematous,Antioxidant, and Antimicrobial Activities

Phenolic compounds and different biological activities of the dry MeOH extracts of the flowers and the herb (aerial parts without flowers) of Laserpitium zernyi Hayek (Apiaceae) were investigated. The total phenolic contents in the extracts were determined spectrophotometrically using Folin–Ciocalteu reagent. In both extracts, apigenin, luteolin, their 7‐O ‐glucosides, and chlorogenic acid were detected by HPLC . Identified phenolics were quantified in both extracts, except luteolin in L . zernyi herb extract. The extracts (p.o .) were tested for anti‐edematous activity in a model of carrageenan (i.pl .) induced rat paw edema. Antioxidant activity of the extracts was assessed by FRAP assay and DPPH and ^?OH radicals scavenging tests. Antimicrobial activity was investigated using broth microdilution test against five Gram ‐positive and three Gram ‐negative bacteria, as well as against two strains of Candida albicans . The polyphenol‐richer flower extract exerted higher anti‐edematous and antioxidant activities. The herb extract exhibited better antimicrobial effect against Micrococcus luteus , Enterococcus faecalis , Bacillus subtilis , and Pseudomonas aeruginosa , while against other tested microorganisms, the activity of both extracts was identical. Demonstrated biological activities of L . zernyi flower and herb extracts represent a good basis for their further investigation as potential new herbal medicinal raw materials.     

Activity of synthetic gibberellin A15 and (±)-gibberellin A15isolactone

The activities of (±)-gibberellin A₁₅ ((±)-GA₁₅) and (±)-gibberellin A₁₅-isolactone ((±)-iso-GA₁₅) which were obtained by stereocontrolled total synthesis and gibberellin A₁₅ (E-GA₁₅) synthesized by interconversion of enmein were assayed by the rice seedling test. As expected, (±)-GA₁₅ showed half the activity of natural gibberellin A₁₅ (GA₁₅). E-GA₁₅ which has a natural configuration showed the same activity as natural gibberellin A₁₅ while (±)-iso-GA₁₅ was almost inactive. These samples were also submitted to the cucumber hypocotyl assay. Contrary to what has already been reported, they were almost inactive.     

Synthesis And Biological Activity Of Substituted 4H-1,4-Benzothiazines,Their Sulfones,And Ribofuranosides

The present article describes the synthesis of new 4H-1,4-benzothiazines via condensation and oxidative cyclization of substituted 2-aminobenzenethiols with β-diketones/β-ketoesters in dimethyl sulfoxide. The oxidation of these synthesized 4H-1,4-benzothiazines with 30% hydrogen peroxide in glacial acetic acid yielded 4H-1,4-benzothiazine sulfones and the reaction of these synthesized benzothiazines with sugar (β-D-ribofuranose-1-acetate-2,3,5-tribenzoate) afforded the new ribofuranosides. These compounds were evaluated for their antioxidant and antimicrobial activities (using broth microdilution method). The structural assignments of the synthesized compounds were made on the basis of elemental analyses and spectroscopic data.     

一株红树林曲霉菌Aspergillus sp.WHUF0343的次级代谢产物研究

【目的】研究分离自三亚亚龙湾红树林根系土壤的真菌Aspergillus sp. WHUF0343的次级代谢产物及其生物活性。【方法】利用硅胶柱层析、Sephadex LH-20凝胶柱层析和半制备高效液相色谱等技术对该菌的发酵产物进行分离纯化;综合利用核磁共振波谱(NMR)和质谱(MS)等现代波谱技术以及与文献数据对照确定化合物的结构;分别采用肉汤微量稀释检测法和MTS法对化合物进行抗菌和肿瘤细胞毒活性测试。【结果】从真菌Aspergillus sp.WHUF0343的发酵产物共分离并鉴定了10个化合物,分别为isoechinulin A (1)、neoechinulin A (2)、neoechinulin E (3)、preechinulin (4)、neoechinulin D (5)、variecolorin J (6)、dehydroechinulin (7)、questinol (8)、emodin (9)和catenarin (10)。活性评价显示化合物2、9和10对幽门螺杆菌(Helicobacter pylori)和金黄色葡萄球菌(Staphylococcus aure...     

Seasonal determinations of extracellular hydrolytic activities in heterotrophic and mixed heterotrophic/autotrophic biofilms from two contrasting rivers

The temporal changes in extracellular enzyme activities in freshwater microbial biofilms were examined in two contrasting river sites in North Wales over a 12 month period. Sites were a first order, unshaded oligotrophic upland stream (Nant Waen) and a fourth order, mildly eutrophic river with riparian tree cover (River Clywedog). When algal populations were low, biofilms of the more eutrophic site supported greater enzyme activities and higher population densities than the oligotrophic site. Composition, concentration and origin of substrates available to the respective biofilm communities influenced extracellular processing patterns. Reduction in algal populations depressed total and extracellular activities in biofilms from the first order site, suggesting that biofilm communities here were maintained by in situ primary production. Biofilms from Nant Waen were often found to contain higher extracellular activities per cell than the more eutrophic River Clywedog biofilms, which might represent the enhanced ability of an oligotrophic biofilm to accumulate extracellular enzymes. In contrast, light and darkgrown River Clywedog biofilms were not enzymatically distinct, inferring a less important role for biofilm phototrophs. Some evidence was found for increased reliance on allochthonous substrates in the River Clywedog for biofilm maintenance.     

Anti-inflammatory and antiproliferative prenylated carbazole alkaloids from Clausena vestita

Twelve prenylated carbazole alkaloids, containing a novel prenylated carbazole alkaloid, named as clausevestine (1), and 11 known prenylated carbazole alkaloids (2–12), were isolated and identified from the stems and leaves of Clausena vestita, which is a Chinese endemic plant. The chemical structure of 1 was established by means of comprehensive spectroscopic data analyses and the known compounds were determined via comparing their NMR and MS data as well as optical rotation values with those reported in literature. Especially, clausevestine (1) is an unusual prenylated carbazole alkaloid possessing an unprecedented carbon skeleton holding 20 carbon atoms. The anti-inflammatory effects and antiproliferative activities of those isolated prenylated carbazole alkaloids were tested. Prenylated carbazole alkaloids 1–12 displayed remarkable inhibitory effects on NO (nitric oxide) production with IC₅₀ values equivalent to that of the positive control (hydrocortisone). Meanwhile, prenylated carbazole alkaloids 1–12 exhibited remarkable antiproliferative activities against diverse human cancer cell lines in vitro holding the IC₅₀ values ranging from 0.32 ± 0.04 to 18.76 ± 0.18 µM. These findings indicate that these prenylated carbazole alkaloids possessing remarkable anti-inflammatory effects and antiproliferative activities could be meaningful to the discovery of new anti-inflammatory and anti-tumor candidate drugs.     

New Resorcinol Derivatives from a Sponge‐Derived Fungus Hansfordia sinuosae

Ten new resorcinol derivatives named hansfordiols A – J ( 1  –  10 ) were isolated from the fermentation broth of the sponge‐derived fungus Hansfordia sinuosae. High resolution electron ionization mass spectrometry, FT‐IR spectroscopy, and NMR techniques were used to elucidate the structures of these compounds, and the absolute configurations were established by the modified Mosher's method and their specific optical rotation. The structures of compounds 8  –  10 were featured with various chlorination at aromatic rings. Their antioxidant activities on ABTS, cytotoxicity on the HCT‐8, Bel‐7402, BGC‐823, A549, and A2780 cell lines, and antibacterial activities were evaluated.     

Biologically Active Heterocyclic Hybrids Based on Quinazolinone,Benzofuran and Imidazolium Moieties: Synthesis,Characterization, Cytotoxic and Antibacterial Evaluation

Cytotoxic and antimicrobial agents structurally based on quinazolinone, benzofuran and imidazole pharmacophores, have been designed and synthesized. Spectral (IR, ¹H‐NMR) and elemental analysis data established the structures of these novel 3‐[1‐(1‐benzofuran‐2‐yl)‐2‐(4‐oxoquinazolin‐3(4H)‐yl)ethyl]‐1‐methyl‐1H‐imidazol‐3‐ium chloride hybrid derivatives. All the synthesized compounds were evaluated for in vitro cytotoxicity and antimicrobial activities. Cytotoxic evaluation using MTT assay revealed that compounds 12c , 12g and 12i exhibited significant cytotoxicity with IC₅₀ values 1, 1, and 0.57 μm on this cell line, respectively. Biological activity of the synthesized compounds as antibacterial agent were also evaluated against three Gram‐negative (Escherichia coli, Pseudomonas aeruginosa and Salmonella typhi), three Gram‐positive (Staphylococcus aureus, Bacillus subtilis and Listeria monocitogenes) and one yeast‐like fungi (Candida albicans) strains. All compounds 12a  –  12i showed slightly higher activity against Gram‐positive bacteria than the Gram‐negative one. Among the nine new compounds screened, 3‐[1‐(5‐bromo‐1‐benzofuran‐2‐yl)‐2‐(6‐chloro‐4‐oxoquinazolin‐3(4H)‐yl)ethyl]‐1‐methyl‐1H‐imidazol‐3‐ium chloride ( 12e ) has pronounced higher antimicrobial activity against all tested strains. These results demonstrated potential importance of molecular hybridization in the development of new lead molecules with major cytotoxicity and antimicrobial activity.     

Biological evaluation of glycosyl-isoindigo derivatives against the pathogenic agents of tropical diseases (malaria, Chagas disease, leishmaniasis and human African trypanosomiasis)

The biological activities of diversely substituted glycosyl-isoindigo derivatives against the causative agents of tropical diseases (malaria, Chagas disease, leishmaniasis and human African trypanosomiasis) are reported. Some of the compounds tested showed interesting activities with good selectivity indices, particularly against Trypanosoma brucei rhodesiense. These results suggested, for the first time, that glycosyl-isoindigo derivatives could be of interest for the discovery of new lead compounds to treat tropical diseases.     

Chemodiversity Associated with Cytotoxicity and Antimicrobial Activity of Piper aduncum var. ossanum

Chemical analysis, antimicrobial activity and cytotoxic effects of essential oils (EOs) from leaves of Piper aduncum var. ossanum from two localities Bauta (EO‐B) and Ceiba (EO‐C), Artemisa Province, Cuba, were determined. EOs were obtained by hydrodistillation and analyzed by gas chromatography/mass spectrometry. EO‐B demonstrated higher activity against S. aureus and L. amazonensis; while a lower cytotoxicity on mammalian cells was observed. Both EOs displayed the same activity against Plasmodium falciparum, Trypanosoma cruzi, Trypanosoma brucei, and Leishmania infantum. Both EOs were inactive against Escherichia coli and Candida albicans.     

Study and Synthesis of Biologically Active Phenothiazines,their Sulfones,and Ribofuranosides

The present article describes the synthesis of new 10H-phenothiazines using the Smiles rearrangement. These synthesized phenothiazines on oxidation with 30% hydrogen peroxide in glacial acetic acid yield sulfones, and when treated with sugar give ribofuranosides. These compounds are evaluated for their anthelmintic and antimicrobial activities. The structural assignment of the synthesized compounds is made on the basis of elemental analysis and spectroscopic data.     

Unusual transformation of substituted-3-formylchromones to pyrimidine analogues: Synthesis and antimicrobial activities of 5-(o-hydroxyaroyl)pyrimidines

Substituted-3-formylchromones (4a–e) on reaction with 1,3-bis-dimethylaminomethylene-thiourea (5) in refluxing toluene solution give novel substituted 5-(o-hydroxyaroyl)pyrimidines (6a–e) in high yields. A mechanistic rationalization of the formation of products (6a–e) is proffered. Antimicrobial activities of all the synthesized compounds (6a–e) were evaluated against various fungal and bacterial strains. Compound 6d display significant antifungal activity (MIC 15) against Geotrichum candidum in comparison fluconazole used as positive control. Some of the compounds also display good antibacterial activity. Cytotoxic profile of compound 6d against HeLa cells indicates that at concentration (20 μM) no significant cell death (～2%) was observed.     

橙盖鹅膏多糖(AC-1)体外免疫调节活性、细胞毒性和抗肿瘤活性的研究

为研究橙盖鹅膏多糖的体外免疫调节活性、细胞毒性和抗肿瘤活性,本研究运用细胞学技术探究AC-1对T细胞、B细胞和RAW264.7三种免疫细胞的体外免疫调节活性;研究AC-1对小鼠成纤维细胞(L929)的细胞毒性以及对小鼠胃癌细胞(MFC)、小鼠肉瘤细胞(S180)的体外抗肿瘤活性。结果表明,AC-1能在体外显著刺激三种免疫细胞的增殖及RAW264.7细胞的吞噬,表明AC-1在增强机体免疫方面具有重要作用,进一步研究发现AC-1主要通过显著促进IgE和IgG的分泌来增强体液免疫。在浓度为5~20μg/mL时AC-1对L929细胞无显著的促进及抑制作用,说明AC-1对正常细胞无毒性;在浓度为10~20μg/mL时AC-1能显著抑制小鼠胃癌细胞(MFC)的生长,但对小鼠肉瘤细胞(S180)的抑制效果较弱,说明AC-1在体外能够直接抑制肿瘤细胞的生长,但对不同的肿瘤细胞具有不同的抑制效果。综上所述,橙盖鹅膏多糖(AC-1)在体外具有良好的免疫调节活性、抗肿瘤活性,但对不同的肿瘤细胞具有不同的抑制效果并且对正常细胞无毒性。     

α-Pyrones,secondary metabolites from fungus Cephalotrichum microsporum and their bioactivities

Cephalotrichum microsporum (SYP-F 7763) was a fungus isolated from the rhizosphere soil of traditional Chinese medicine Panax notoginseng. The EtOAc extract of Cephalotrichum microsporum cultivated on sterilized moistened-rice medium was separated by various chromatographic techniques, which yielded 11 metabolites (1–11) of this fungus. On the basis of the widely spectroscopic data, the chemical structures of isolated metabolites were determined, most of which were α-pyrones, including 5 compounds (4–7, and 10) unreported. In the anti-bacterial bioassay, compound 1 displayed significant inhibitory effects on three pathogenic bacteria, MR S. aureus, S. aureus, and B. cereus. α-Pyrones 2, 3, and 5–7 also displayed moderate inhibitory effects on MR S. aureus, S. aureus, and B. subtilis, which could be the major anti-bacterial constituents of Cephalotrichum microsporum. Additionally, compounds 1, 4, and 5 displayed significant cytotoxicity on five human cancer cell lines, with the IC₅₀ values < 20 μM, which are more effective than positive control 5-fluorouracil. Therefore, α-pyrones were important secondary metabolites of Cephalotrichum microsporum, which displayed anti-bacterial and anti-tumor activities.     

Bioactive cucurbitane triterpenoids from the tubers of Hemsleya penxianensis

Four new cucurbitacins, jinfushanencins C-F (1–4) and three known analogues (5–7) were isolated from the tubers of Hemsleya penxianensis by Silica gel column, ODS column, pre-HPLC techniques. The structures of 1–7 were establishhed on the basis of extensive spectroscopic. The isolated compounds were tested for their cytotoxic activity against Hela human cancer cell line and compounds 1, 5, and 7 showed significant cytotoxicity with IC₅₀ values at 5.1, 8.7, and 1.2 μM, respectively. None of the compounds had active anti-HIV activity.     

Degenerative joint disease in hunter-gatherers and agriculturalists from the Southeastern United States

This study examines degenerative joint disease of the major appendicular joints in hunter-gatherers and agriculturalists from northwestern Alabama. Arthritis is highest at the shoulder, elbow, and knee and lower at the hip and ankle. There are virtually no sex differences in the hunter-gatherer group, but in the agriculturalists, males have more severe osteoarthritis than females. The hunters-gatherers have a somewhat greater prevalence of arthritis than the agriculturalists, but the differences are rarely significant. The similarity in osteoarthritis levels over time conflicts with biomechanical evidence, which indicates an increase in usual activities in the agricultural period. Several possible reasons for this are explored, including the suggestion that arthritis is a response to intensive or infrequent activities. Whatever the cause, it is clear that biomechanical data and osteoarthritis are responding to different factors and do not equally represent the level of usual activities.