Antibacterial,antioxidant and antiproliferation activities of essential oils and ethanolic extracts from Chinese mugwort(Artemisia vulgaris L.)leaf in Shanxi

Background:Artemisia vulgaris,a medicinal aromatic plant,is widely used as a food item,tonic pharmaceutical,and cosmetic industry additive owing to its antibacterial,antihypertensive,hepatoprotective,antioxidant,and antispasmodic properties.But the effect of different geographic locations on the chemical composition and bioactivities of its extracts is unclear.Methods:Biological activities of essential oils and ethanol extracts of three varieties of Artemisia vulgaris leaves,which are grown in Shanxi province China,were studied.Results:Gas chromatography-mass spectrometry analysis revealed that the main components of essential oils were terpenes and ketones.Essential oils and ethanol extract of Artemisia vulgaris leaves possessed good antioxidant activities,and their half maximal inhibitory concentrations determined using 1,1-diphenyl-2-picrylhydrazyl and 2,2’-azinobis-(3-ethylbenzthiazoline-6-sulphonate)assays were 57.0 and 22.9μg/mL,respectively.The essential oils also exhibited remarkable antibacterial activity against three foodborne pathogenic bacterial strains.The ethanol extract presented a high anticancer activity against the MGC-803 human gastric cancer cell line.Conclusion:These biological activities were well correlated with the composition of the extract and EOs,which in turn is affected by the genetic composition of Artemisia vulgaris and geographic location and diverse climatic condition under which it is grown.These findings demonstrate the remarkable potential of Artemisia vulgaris as a valuable source of antioxidant,antibacterial,and anticancer agents.

The contribution of different polyphenol compositions from chokeberry produced in China to cellular antioxidant and antiproliferative activities

Abundant polyphenols make chokeberry have beneficial antioxidant and antiproliferative activity. In order to explore the contribution of different polyphenols in chokeberry to these activities, this study was conducted to determine polyphenol composition from 7 chokeberry varieties produced in China. Totally, 11 kinds of main polyphenol monomers were identified and quantified by UPLC-Q-TOF-MS and UPLC-PDA. HepG2 cells were used to evaluate their cellular antioxidant and antiproliferative activities. Partial least squares method was utilized to analyze multivariate correlations between proportion of different composition and monomers in total polyphenols with these activities. The results showed that the highest proportion in chokeberry polyphenols was proanthocyanidins. In comparing the bioactivities of 7 varieties of chokeberry, ‘Viking' and purple chokeberry had the strongest antioxidant activity, while 'Fukangyuan 1#' had the strongest antiproliferative activity. In terms of the contribution sources of these bioactivities, the total antioxidant activity of chokeberry mainly depended on the contribution of free polyphenols. As the main source of cellular antioxidant activity, anthocyanins and neochlorogenic acid can provide more contribution. The antiproliferative activity mainly depended on the proportion of free polyphenols and proanthocyanidins in total polyphenols. The results may provide some new possibilities for the comprehensive utilization of polyphenols from chokeberry.

Influences of Melatonin on the Growth of HeLa Cells

Aim To investigate the influences of melatonin (MT) on the growth of HeLa cells in vitro. Methods Theantiprolfferation activities of MT were evaluated in HeLa cells by means of trypan blue dye exclusion and MTT vital staining.The morphological changes of HeLa cells induced by MT were observed under transmission electronic microscope. Cell divisioncycle influenced by MT was assessed by a flow cytometry. Results MT produced a certain inhibition of HeLa cells at the con-centration of 2 mmol@ L-1 and prolonged the TD. The fraction of cells inhibited was 61.0%. The IC. so of HeLa cells exposed toMT for 96 h was 2.039 mmol@ L- 1. The flow cytometric analyses showed that exposure to MT for 72 h reduced the number ofHeLa cells in phase S. Under electronic microscope, the HeLa cells exposed to MT for 72 h displayed morphological changesof necrosis, apoptosis, more hetero-chromosome and less somatic chromosome. Conclusion MT showed certain influences onthe growth of HeLa cells. Its mechanism may probably be attributable to reduction of the number of cells in phase S.

Apoptosis of human cholangiocarcinoma cells induced by ESC-3 from Crocodylus siamensis bile

AIM： To investigate the effects of ESC-3 isolated from crocodile bile on the growth and apoptosis induction of human cholangiocarcinoma cells.

Antiproliferative effect of silver nanoparticles synthesized using amla on Hep2 cell line

Objective:To synthesize silver nanoparticles by amla extract,screen the cytotoxic,oxidative stress and apoptotic effect of silver nanoparticles（AgNPs） on Hep2 cell line（laryngeal carcinoma cells） in vitro,and to compare the effect of Phyllanthm emblica（P.emblica）（amla） with AgNPs synthesized by amla and 5-FU.Methods:AgNPs was synthesized by P.emblica（aqueous extract） and nanoparticles were characterized UV-Vis spec,the presence of biomoloecules of amla capped in AgNPs was found by FT-IR analysis,shape and size were examined by SEM and DLS.Cytotoxicity of experimental drugs was tested to find IC50 value.ROS generation in cells have been measured by DCFH-DA staining.AO-EtBr,Rhodamine-123 staining and DNA fragmentation were performed to assess apoptotic cell death,mitochondrial membrane potential and apoptotic DNA damage,respectively.Oxidative stress was analyzed by measuring lipid peroxides and antioxidants level lo understand the cancer cell death by pro-oxidant mechanism. Results:PE-AgNPs was synthesized and confirmed through kinetic behavior of NPs.The shape of PE-AgNPs was spherical and cubic since it was agglomerated,and the nanoparticle surface was complicated.Average particle size distribution of PE-AgNPs was found to be 188 nm.Potent biomolecules of P.emblica such as polyphenols were capped with AgNPs and reduced its toxicity. In cytotoxicity assay the concentration in which the maximum number of cell death was 60μg/mL and 50μg/mL for P.emblica（alone） and AgNPs,respectively and IC50 values were fixed as 30μg/mL and 20μg/mL.ROS generation,apoptotic morphological changes,mitochondrial depolarization.DNA damage and oxidative stress was observed as more in AgNPs treated cells than in P.emblica（30μg/mL）（alone） treated cells and 5-FU treated cells gave similar result. Conclusions:The results suggest that the AgNPs are capped with biomolecules of amla enhanced cytotoxicity in laryngeal cancer cells through oxidative stress and apoptotic function on Hep2 cancer cells.

Cytotoxic effects of Thai noni juice product ethanolic extracts against cholangiocarcinoma cell lines

Objective:To investigate the cytotoxic activity and molecular mechanism(s)of two Thai noni juice(TNJ)products ethanolic extracts against cholangiocarcinoma(CCA)cell lines and non-cancerous cells,and to explore phenolic acid compositions of TNJ products.Methods:Phenolic acid profiles of TNJ Chiangrai(TNJ-Cr)and TNJ Buasri(TNJ-Bs)ethanolic extracts were determined by HPLC.The cytotoxicity of TNJ ethanolic extracts on cancer and non-cancerous cells was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide and trypan blue assays.Mechanism(s)underlying the anti-CCA activity of TNJ ethanolic extracts were determined by cell cycle,apoptosis,and reactive oxygen species(ROS)generation assays.The expression levels of proteins involved in apoptosis and ERK signaling were evaluated by Western blot analysis.Results:Phenolic acid profiles of both TNJ ethanolic extracts showed that the p-hydroxybenzoic,vanillic,and protocatechuic acids were the major phenolic acids in TNJ products.Cytotoxicity assays revealed that the TNJ-Cr and TNJ-Bs ethanolic extracts reduced viability of CCA cell lines through induction of apoptosis by up-regulation of p53 and Bax proapoptotic proteins.Both TNJ ethanolic extracts promoted ROS generation by activating the ERK1/2 signaling in well-differentiated CCA cells KKU-213B.Meanwhile,TNJ ethanolic extracts did not induce ROS production in poorly differentiated CCA cells KKU-100.Both TNJ ethanolic extracts showed no toxicity to human peripheral blood mononuclear cells.Conclusions:TNJ ethanolic extracts could inhibit CCA cell proliferation by inducing ROS generation and apoptosis and may be applicable for combination therapies in CCA treatment.

Antitumor Effects and Acute Oral Toxicity Studies of a Plant Extract Mixture Containing <i>Rhus verniciflua</i>and Some Other Herbs

A novel antitumor agent was developed from six kinds of herbs containing Rhus verniciflua (Rv-PEM01). The components were traditionally established for each formula for traditional medicine. The formula was designed to affect antitumor effect as well as maintain host immune functions. First, we investigated the antiproliferative activities of Rv-PEM01 on human and canine tumor cell lines in vitro, and on antitumor effects using BALB/cAJcl-nu/nu mice in vivo. Acute oral toxicity of Rv-PEM01 was also investigated in vivo in ddY mice. Rv-PEM01 exhibited antiproliferative activities against PC-3 (IC50: 0.328 ± 0.081 mg/ml), A549 (IC50: 0.520 ± 0.070 mg/ml), D-17 (IC50: 0.124 ± 0.037 mg/ml) and MRC-5 (IC50: 0.505 ± 0.058 mg/ml) cells. Luteolin 7-β-D-glucopyranoside and apigenin 7-β-D-glucopyranoside were identified as the main active compounds in Rv-PEM01 by HPLC analysis. The single dose toxicity study of Rv-PEM01 did not result in any deaths or abnor-malities in daily behavior, body weight gain, or anatomical observations at necropsy. Thus, so we could not calculate the 50% lethal dose (LD50) in mice, but it would be higher than 5.0 g/kg. Treat- ment with Rv-PEM01 at a dose of 2.5 g/kg tended to show antitumor activities on mice bearing Colon26 tumors compared with the control group. It was concluded that the formula was a safe antitumor agent with no side effects on mouse physiological function as judged by survival and organ weight.

Anticancer Effect in HL-60 Human Leukemia Cells and Other Helath-Beneficial Functions of Cheese

With regard to the aim of cancer prevention and/or treatment, a considerable number of basic studies have indicated that dairy and other plant-originated natural food products may possess anticancer activity. On the growth of human leukemia cells, for example, enzymatically digested skim milk or fermented milk cultured with various bacteria can exhibit differential suppressive activities. Our research team has previously revealed that highly ripened cheese was capable of demonstrating strong growth inhibition and induction of apoptotic DNA damage on HL-60 human promyelocyticleukemia cells. In this short review, the available information concerning potent anticancer effects of cheese was summarized. From the stand point of Food Science, functional implications for cancer prevention as well as multifaceted function of cheese are discussed.

Screening of flavonoid "quercetin" from the rhizome of Smilax china Linn.for anti-psoriatic activity

Objective:To assess anti-psoriatic activity of the methanol extract and the isolated flavonoid quercetin from the rhizome of Smilax china(S.china) Linn.Methods:Mouse tail test was used for the evaluation of anti-psoriatic activity.Methanol extract(100 and 200 mg/kg b.w.) and isolated flavonoid quercetin(25 and 50 mg/kg b.w.) were tested in Swiss albino mice.Parameters studied in the mouse tail test were changes in epidermal thickness and percentage orthokeratotic values.The anti-inflammatory role of the methanol extract and isolated flavonoid quercetin was evaluated using carrageenan-induced pleurisy in rats.In vitro antiproliferant assay on HaCaT cell lines was also carried out.Results:The isolated flavonoid quercetin from the rhizome of S.china produced significant orthokeratosis(P<0.01) in the mouse tail test.In epidermal thickness,a significant reduction with respect to control was observed in groups treated with retinoic acid and isolated flavonoid quercetin.The methanol extract(200 mg/kg) and isolated flavonoid quercetin(50 mg/kg) showed anti-inflammatory effect in terms of significant inhibition(P<0.001) in leukocyte migration.Maximum antiproliferant activity was shown by isolated flavonoid quercetin(IC_(50),62.42± 10.20 μg/mL).Conclusions:From the above data,the flavonoid quercetin shows significant orthokeratosis,anti-inflammatory and maximum antiproliferant activities.To our knowledge,this is the first report on the anti-psoriatic effect of the flavonoid quercetin which is promising for further investigations to prove its anti-psoriatic activity.

A Rhein-Based Rh(Ⅲ) Arene Complex with Anti-tumor Cell Proliferative Activity Inhibits RNA Demethylase FTO

Metallodrugs with fine-tuned coordination between metals and bioactive ligands can achieve cytotoxic effects in cancer therapy and have been considered as a new approach for drug design.However,it has yet to be elucidated whether these metallodrugs target epitranscriptomic proteins for gene expression regulation.This report describes a rhein-based Rh(l)-arene complex,Rh1,that exhibited promising antiproliferative ffects in several tumor cellines.Rh1 induced cell death through the autophagy,cell cycle arrest,and accumulation of intracllular reactive oxygen species(ROs),In addition,Rh1 upregulated the global N^(6)-methyladenosine(m^(6)A)levels in A549 cells in the fat mass-and obesity-associated protein(FTO)-dependent manner.Collectively,the metal-based FTO inhibitor Rh1 effectively suppressed tumor cell proliferation and modulated the abundance of cellular m^(6)A,highlighting the potential of metal-based agents to target and regulate epitranscriptomics for tumor suppression.

Antioxidant, antiangiogenic and antiproliferative activities of root methanol extract of Calliandra portoricensis in human prostate cancer cells

OBJECTIVE： Prostate cancer（PCa） is a major health concern. Calliandra portoricensis（CP） is traditionally known for its analgesic, anti-ulcerogenic and anticonvulsant properties. However, its antiproliferative properties for PCa still need to be investigated. METHODS： Antioxidant activities of CP were determined by 1,1-diphenyl-2-picryhydrazyl（DPPH） and hydroxyl（OH-） radicals-scavenging methods. PC-3 and LNCa P（androgen-refractory and androgendependent PCa-derived cell lines） were cultured and treated with CP（10, 50 and 100 μg/m L）. Effects of CP on cells were determined by cytotoxicity assay（lactate dehydrogenase, LDH） and viability assay（sodium 3′-[1-（phenylaminocarbonyl）-3,4-tetrazolium]-bis（4-methoxy-6-nitro） benzene sulfonic acid hydrate, XTT）. DNA fragmentation was detected by cell death detection enzyme-linked immunosorbent assay plus kit. CP was tested as an inhibitor of angiogenesis using chicken chorioallantoic membrane（CAM） assay. RESULTS： CP showed significant scavenging of DPPH and OH- radicals. CP significantly（P〈0.05） inhibited lipid peroxidation in a dose-dependent manner. Precisely, CP（10, 50 and 100 μg/m L） inhibited PC-3 and LNCa P growth by 7%, 74% and 92%, and 27%, 73%, and 85% respectively at 48 h. CP had low toxicity in vitro at its half inhibitory concentration dose. Detection of cell death induced by CP at 50 μg/m L showed higher enrichment factors in LNCa P（7.38±0.95） than PC-3（3.48±0.55）. Also, treatment with CP（50 μg/m L） significantly reduced network of vessels in CAM, suggesting its antiangiogenic potential. CONCLUSION： Calliandra portoricensis elicited antioxidant, antiangiogenic and antiproliferative effects in PCa cells.

Induction of sub-G0 arrest and apoptosis by seed extract of Moringa peregrina（Forssk.） Fiori in cervical and prostate cancer cell lines

Objective: This study investigated cytotoxicity and induction of apoptosis in human cervical cancer cells(HELA) and prostate cancer cells(PC-3) using the most active fraction of Moringa peregrina seed extract.Methods: Dried and powdered seeds were extracted using 95% ethanol. The total ethanolic extract was further dissolved in distilled water and separated into petroleum ether, chloroform, ethyl acetate and aqueous extracts. Based on the results of in vitro anticancer studies of all extracts, the most highly active extract was selected for evaluation of apoptosis induction and cell cycle analysis on HELA and PC-3 cells at its half maximal inhibitory concentration using flow cytometry;DNA fragmentation by agarose gel electrophoresis and the expression of protein were measured by Western blot.Results: The chloroform fraction from the ethanolic extract of M. peregrina(CFEE) was the most active antitumor fraction. The selectivity index, determined using the normal Vero cell line, indicated that CFEE had a high degree of selectivity against HELA and PC-3 cells. CFEE induced apoptosis, confirmed by cell cycle arrest at sub-G0 phase and DNA fragmentation. CFEE induced an increase in mRNA expression of caspase-3, a decrease in Bcl-2 mRNA expression, and decreased ATP levels. CFEE increased protein expression of caspase-3 and decreased protein expression of poly-ADP-ribose polymerase-1(PARP-1).Flow cytometric analysis showed an appreciable increase in the number of cells in the early apoptotic stage in CFEE-treated HELA and PC-3 cells. CFEE treatment significantly increased lipid peroxidation(malondialdehyde level) in HELA and PC-3 cells.Conclusion: Seed extract of M. peregrina displayed a significant antitumor effect through apoptosis induction in HELA and PC-3 cells.

Synthesis of Hirtellanine B, an Isoflavonoid with Potent Antiproliferative Effects in Cancer Cells

We reported the first total synthesis of hirtellanine B, using oxidative coupling for the key reactions, which resulted in a high yield. The antiproliferative activities of hirtellanine B against Jurkat cells, Raji cells and K562 cells were also investigated. It was found that hirtellanine B could induce G2/M arrest and apoptosis in human lymphoid/leukemia tumor cells.

Linear polyketides produced by co-culture of Penicillium crustosum and Penicillium fellutanum

Two new polyketides, penifellutins A (1) and B (2), possessing a 22 carbon linear skeleton, were isolated from a co-culture of the deep-sea-derived fungi Penicillium crustosum PRB-2 and Penicillium fellutanum HDN14-323. Meanwhile, two esterification products of 1, penifellutins C (3) and D (4), were obtained because compound 1 could be esterified spontaneously when stored in methanol. Their configurations were difficult to determine because of chiral central crowdedness, structural flexibility and instability. As such, we solved this issue by comprehensively using Mo2(OAc)4-based CD experiments, density functional theory calculation of 13C NMR, DP4 + probability analysis and many chemical reactions, including making acetonide derivative, Mosher’s method, PGME method, etc. Compounds 1 and 2 show obvious inhibitory activity on the liver hyperplasia of zebrafish larvae at a concentration of 10 μmol/L, while 3 and 4 show no activity, indicating that two carboxyls in the structure are important active sites.

Chiral rhodium(Ⅱ)-catalyzed asymmetric aldol-type interception of an oxonium ylide to assemble chiral 2,3-dihydropyrans

A chiral dirhodium complex is an effective and robust catalyst for asymmetric carbene transformations.However,dirhodiumcatalyzed asymmetric ylide interception processes are rare,mainly because of the dissociation of the metal catalyst before the stereo-determining step.Herein,we report a chiral dirhodium(Ⅱ)-catalyzed asymmetric annulation of vinyl diazoesters withα-hydroxyl ketones,which provides an efficient way to form chiral 2,3-dihydropyrans in good yields with excellent diastereoselectivities and enantioselectivities.This article is the first example of the chiral dirhodium complex–controlled asymmetric aldol-type interception of an in situ–formed oxonium ylide.The origin of the high stereoselectivity is well expounded via experimental and computational studies.These generated chiral products exhibit potent antiproliferation activity in three tested cancer cell lines,namely HCT116(colon cancer),A549(lung adenocarcinoma),and SJSA-1(osteosarcoma cancer).

Comparative assessment of phenolics,antioxidant and antiproliferative activities between Hippophae rhamnoides ssp.sinensis and H.tibetana leaf in Qinghai-Tibet Plateau

Hippophae rhamnoides ssp.sinensis(Rha)and H.tibetana(Tib)are two species of sea buckthorn which distribute in Qinghai-Tibet Plateau.Our results showed that both sea buckthorn leaf exhibited high total phenolic and flavonoid content,and Rha leaf showed much higher level.In addition,66 phenolic compounds were detected,belonging to classes of benzoic acid derivatives,flavonols,flavanols,flavanones,and so on.Classes of benzoic acid derivatives and flavonols were most abundant,among them ellagic acid and rutin were the most and second abundant phenols.Besides,methyl gallate,2,6-dihydroxybenzoic acid,4-hydroxybenzoic acid,gentisic acid,narcissin,astragalin,nicotiflorin,prunin,procyanidin B3,cyanidin 3-O-rutinoside chloride,delphinidin 3-glucoside,gallocatechin,taxifolin,aromadendrin and trans-3,3′,4′,5,5′,7-Hexahydroxyflavanone were the first time to be identified in SBT leaf.Furthermore,significant free radical scavenging effects of ABTS and DPPH,ferric reducing antioxidant ability,cellular antioxidant properties and anti-proliferation activity against HepG2 cells were observed in the aqueous ethanol extracts of sea buckthorn leaf.While Rha showed stronger inhibitory effects,which might due to the higher content of total phenolic and flavonoid profiles.Our finding clearly supported that Rha leaf as a wild and non-pollution plant could be a better choice as a healthy food resource.