竹叶提取物的体外抑菌及抗氧化活性的研究

本文用水提取竹叶有效成分,将提取液浓缩至含生药量约1.0 g/mL,经醇沉后取清液浓缩,再经石油醚、三氯甲烷、乙酸乙酯、正丁醇分步萃取,得不同极性的各部分提取物。以金黄色葡萄球菌和大肠杆菌为供试菌,采用抑菌圈法(琼脂扩散法)和最低抑菌浓度(MIC)法测定其抑菌效果。结果显示,石油醚、三氯甲烷、乙酸乙酯部分均表现抑菌活性。各供试样对两种菌的抑菌圈直径达9.8～18.4 mm,最低抑菌浓度分别为1.25 mg/mL2,.50 mg/mL和5.00 mg/mL。最后采用亚硝基红盐-Co2+褪色法研究了竹叶提取物对.OH的清除作用,结果表明三氯甲烷和乙酸乙酯部分萃取物的抗氧化性明显优于水提物,其中乙酸乙酯部分萃取物的IC50值为1.06 mg/mL。     

Antibacterial activity of Punica granatum L. and Areca nut (P.A) combined extracts against some food born pathogenic bacteria

The antibacterial effects of combined extracts of Punica granatum L. and Areca nut (P.A) against resistant bacteria, a gram-positive bacterium, Staphylococcus aureus and three gram-negative bacteria, Escherichia coli, Salmonella, and Enterobacter aerogenes, in individual and biofilm forms was studied. Antibacterial activity was studied using disk diffusion method, microbroth dilution, and microtiter plate methods. Given the disc diffusion test (Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC)), the extracts had inhibitory effects on the individual forms of bacteria. However, the ethanolic extract had greater effectiveness than the methanolic extract. Generally, ethanol efficiently extracts flavonoids and their glycosides, catechol and tannins. This fact due to the ethanol polarity that is equal 0.654. The results indicated that the ability of extracts in inhibiting the formation of biofilms, destruction of biofilms, and prevention of metabolic activity of bacteria had a direct relationship with concentration and the highest inhibitory was seen on Staphylococcus aureus (98.98%), Staphylococcus aureus (94.98%), and Enterobacter aerogenes (88.55%). Based on the results, the P.A. combined extract can be used as an alternative combination with the ability to inhibit antibiotic-resistant bacteria in single and biofilm forms.     

The anti-biofilm potential of pomegranate (Punica granatum L.) extract against human bacterial and fungal pathogens

Infectious diseases caused by bacteria and fungi are the major cause of morbidity and mortality across the globe. Multi-drug resistance in these pathogens augments the complexity and severity of the diseases. Various studies have shown the role of biofilms in multi-drug resistance, where the pathogen resides inside a protective coat made of extracellular polymeric substances. Since biofilms directly influence the virulence and pathogenicity of a pathogen, it is optimal to employ a strategy that effectively inhibits the formation of biofilm. Pomegranate is a common food and is also used traditionally to treat various ailments. This study assessed the anti-biofilm activity of a methanolic extract of pomegranate against bacterial and fungal pathogens. Methanolic extract of pomegranate was shown to inhibit the formation of biofilms by Staphylococcus aureus, methicillin resistant S. aureus, Escherichia coli, and Candida albicans. Apart from inhibiting the formation of biofilm, pomegranate extract disrupted pre-formed biofilms and inhibited germ tube formation, a virulence trait, in C. albicans. Characterization of the methanolic extract of pomegranate revealed the presence of ellagic acid (2,3,7,8-tetrahydroxy-chromeno[5,4,3-cde]chromene-5,10-dione) as the major component. Ellagic acid is a bioactive tannin known for its antioxidant, anticancer, and anti-inflammatory properties. Further studies revealed the ability of ellagic acid to inhibit the growth of all species in suspension at higher concentrations (>75?μg?ml^?1) and biofilm formation at lower concentrations (<40?μg?ml^?1) which warrants further investigation of the potential of ellagic acid or peel powders of pomegranate for the treatment of human ailments.     

Preparation and Evaluation of Gallate Ester Derivatives Used as Promising Antioxidant and Antibacterial Inhibitors

Many gallate esters have been applied as food additives due to their good biological properties. Herein, nine novel gallate ester derivatives were synthesized by a Friedel-Crafts alkylation reaction and characterized by melting point (m.p.), infrared (IR) spectroscopy, nuclear magnetic resonance (¹H- and ¹³C-NMR) spectra, and high-resolution mass spectrometry (HR-ESI-MS). Their antioxidant and antibacterial activities were measured using a series of classical assays. Studies found that the products showed favorable antioxidant and antibacterial activities. Their 1,1-diphenyl-2-picrylhydrazyl free radical (DPPH ^⋅ ) scavenging effect IC₅₀ values were less than 5.00 μg mL⁻¹ and their reducing power was not less than that of vitamin C (Vc). Furthermore, the antibacterial results showed that the minimum inhibitory concentration (MIC) values of the products were not greater than 8.00 μg mL⁻¹, and their antibacterial rates were over 95 % at 300 μg mL⁻¹. The above data add valuable and novel information that gallate ester derivatives can be considered potential food additives to address food safety issues because of their high biological activity and health benefits.     

香茅精油的抑菌和抗氧化活性研究

选用产自福建厦门的香茅(Cymbopogon nardus),测定香茅精油对白色粘性沙雷氏菌、红色粘性沙雷氏菌、大肠杆菌、金黄葡萄球菌、铜绿假单胞菌和紫色杆菌等6种菌的抑菌活性,并利用ABTS^.+自由基清除法以及超氧阴离子清除法研究香茅精油的抗氧化活性。结果表明,新鲜香茅精油的平均提取率为0.29,对6种供试菌种都有较高的抑制作用,其中对紫色杆菌的抑制活性最强,且香茅精油有极高的清除ABTS^.+自由基以及超氧阴离子自由基的能力,证明香茅精油具有广谱抑菌活性及强抗氧化活性。     

白背三七大孔树脂富集物化学成分及抗氧化活性研究

本文采用HPLC-ESI-MS分析白背三七醇提液经HPD-100树脂富集分离后的黄酮类化合物,并采用化学和生物模型对富集物的抗氧化活性进行研究.实验结果表明该富集物主要黄酮成分为槲皮素和山奈酚的糖苷类化合物,且以山奈酚-3 -O-β-D-葡萄糖苷的含量最高;白背三七醇提液经富集后总黄酮含量提高了6倍.在试验模型中,除螯合能力外,富集后产物抗氧化能力较富集前均有显著提高,说明黄酮类化合物是白背三七抗氧化活性的主要物质基础.     

Phenolic Profiling,Antioxidant, and Antibacterial Activities of Selected Medicinal Plants from Tunisia

Phytochemical screening of aqueous extract from six medicinal wild plants grown in South-eastern of Tunisia: Atriplex halimus, Teucrium polium, Moricandia arvensis, Deverra tortuoa, Haplophyllum tuberculatum and Polygonum equisetiforme were evaluated. Both decoction and ultrasound assisted extraction were used. Antioxidant, antibacterial proprieties, and phenolic profiling, using LC-ESI-MS method, were assessed. Total polyphenols, flavonoids, and condensed tannins contents ranged from 7.47±0.19 to 22.25±0.49 mg GAE/g Dw, 5.47±0.06 to 7.55±0.07 mg RE/g Dw, and 0.33±0.02 to 19.43±0.64 mg TAE/g Dw, respectively. Moreover, the reducing power and DPPH tests showed that P. equisetiforme (EC₅₀: 12.50±0.50 μg/ml; DPPH⋅⁺: 213.49±4.24 mg TEAC/g DW), T. polium (EC₅₀: 25.00±1.00 μg/ml; DPPH⋅⁺: 181.39±9.47 mg TEAC/g DW) as well as H. tuberculatum (EC₅₀: 56.25±0.25 μg/ml; DPPH⋅⁺: 177.83±5.85 mg TEAC/g DW) extracts were the most effective natural antioxidants. For anti-bacterial activity, the ultrasonic extract of H. tuberculatum showed the highest activity against both P. aeruginosa (13.50±0.71 mm) and S. aureus (13.00±0.00 mm) at 10 mg/ml. Furthermore 24 phenolic compounds were identified, with predominance of quinic acid, gallic acid, protocatechuic acid, syringic acid, p-coumaric acid, trans-ferulic acid, catechin (+), trans-cinnamic and silymarin. These results were further consolidated by to heatmap clustering with P. equisetiforme, H. tuberculatum, T. polium as the main antioxidant and antibacterial sources which supports their domestication and industrial use.     

Investigations of Antibacterial,Antioxidant, and Antidiabetic Potential of Extract and Its Active Fractions from the Leaves of Horsfieldia spicata (Roxb.) J. Sinclair

This study was undertaken to analyse the potential bioactivities including antibacterial, antioxidant and antidiabetic derived from the methanolic extract and the column chromatography ethyl acetate fraction (AcOEt Fr) of Horsfieldia spicata leaves. Methanolic extract and 4 other fractions was calculated for total phenol and flavonoid contents along with tested for antibacterial, antioxidant and antidiabetic properties. Interestingly, the AcOEt Fr had the highest value for total flavonoid content and the best antioxidant, and antidiabetic activities. Therefore, the AcOEt Fr was further separated using column chromatography technique for obtaining 9 selected fractions namely fraction 1 (F1) - fraction 9 (F9) which were further tested. The results showed that the AcOEt column chromatography fractions namely F2, F3, F4 and F6 had the best clear inhibition antibacterial value against all bacterial tested. In addition, these fractions also exhibited better Minimum Inhibitory Concentrations (MIC) and Minimum Bactericidal Concentrations (MBC) values than others. Antioxidant, 2,2-diphenylpicrylhydrazyl (DPPH) assayed indicated that AcOEt Fr had the strongest IC₅₀ value of 47.30 μg/mL. Further, F4 column chromatography fraction showed the best inhibition against α-Glucosidase enzyme related to antidiabetic activity with an IC₅₀ value of 6.11 μg/mL. Liquid chromatography tandem-mass spectrometry (LC/MS/MS) analysis identified that F4 derived from AcOEt fraction had several compounds belonging to the flavonoid and phenolics such as 3′,5-dihydroxy-7,4′-dimethoxyflavone, 5,7-dihydroxy-3-(4′-hydroxybenzyl)chromone, and Kadsurenin I.     

侧柏叶精油的抗细菌和抗氧化活性(英文)

采用水蒸气蒸馏法提取侧柏叶精油,通过GC和GC-MS分析精油的组成。从侧柏叶精油中鉴定出29种成分,主要为单萜和倍半萜,含量较高的化合物有:8-丙氧基-柏木烷(15.41%)、松油烯-4-醇(12.98%)、α-蒎烯(9.85%)、桧烯(9.92%)和3-蒈烯(6.77%)。侧柏叶精油具有广谱的抗细菌活性,对供试细菌的最低杀菌浓度(MBC)在0.1 mg/mL和1.0 mg/mL之间,最低抑菌浓度(MIC)在0.063 mg/mL和0.90 mg/mL之间,半抑制浓度(IC50)在0.044 mg/mL和0.763 mg/mL之间。侧柏叶精油能有效抑制菲啰嗪与Fe2+的螯合(IC50值为0.409mg/mL)和β-胡萝卜素-亚油酸的氧化(IC50值为0.526 mg/mL)。     

Evaluation of Pomelo Seed Extracts as Natural Antioxidant,Antibacterial, Herbicidal Agents,and Their Functional Components

Pomelo seeds (PS) are important by-product of pomelo fruits (Citrus grandis Osbeck). The value-added utilization of PS remains highly challenged. This study aimed to investigate the utilization potential of PS as natural antioxidant, antibacterial, herbicidal agents, and their functional components. The ethanolic extract (EE) of PS and its four fractions as PEE (petroleum ether extract), AcOEtE (ethyl acetate extract), BTE (butanol extract), and WE (water extract), were prepared and biologically evaluated. BTE exhibited the best antioxidant activity among all these extracts, in both ABTS (2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt) and FRAP (ferric reducing antioxidant power) assays. AcOEtE was superior to other extracts in herbicidal assay against both Festuca elata Keng (IC₅₀ of 0.48 mg mL⁻¹) and Amaranthus retroflexus L. (IC₅₀ of 0.94 mg mL⁻¹). Meanwhile, both AcOEtE and BTE demonstrated inhibitory effects against Bacillus subtilis, Escherichia coli, and Xanthomonas citri subsp. citri, with MIC ranging 2.5–5.0 mg mL⁻¹. Furthermore, the primary chemical components involving naringin, deacetylnomilin, limonin, nomilin, and obacunone, were quantified in all these extracts. PCA (principal component analysis) suggested that naringin might highly contribute to the antioxidant activity of PS, and the herbicidal activity should be ascribed to limonoids. This study successfully identified AcOEtE and BTE as naturally occurring antioxidant, antibacterial, and herbicidal agents, showing application potential in food and cosmetics industries, and organic farming agriculture.     

Preparation of New Spiropyrazole,Pyrazole and Hydantoin Derivatives and Investigation of Their Antioxidant and Antibacterial Activities.

In this study, the synthesis of new spiropyrazoles, pyrazole and hydantoin heterocycles is reported by three component reactions of parabanic acids, hydrazine derivatives, and phenacyl bromides in the presence of triphenylphosphine as a nucleophile and triethylamine as a base in good to high yields (69–91 %). Evaluation of the synthesized compounds revealed a good to excellent antioxidant activities (37.6–96.2 %) using DPPH inhibitory potency. Among these compounds, hydantoin derivatives displayed higher antioxidant activities (93.7–96.2 %) comparing with spiropyrazoles and pyrazoles. The obtained results showed that Cl and Br substituents on the phenyl ring increased antioxidant activities of the related heterocycles. The antibacterial activities of the synthesized compounds were examined against two Gram-negative (Escherichia coli and Pseudomonas aeruginosa) and two Gram-positive (Staphylococcus aureus and Bacillus subtilis) bacteria. Among the synthesized heterocycles, 2-[1,3-dimethyl-2,5-dioxo-4-(2-oxo-2-phenylethyl)imidazolidin-4-yl]hydrazine-1-carbothioamide exhibited the excellent antibacterial activity against both Gram-positive and Gram-negative bacteria.     

Synthesis and Antibacterial Activity Evaluation of Biphenyl and Dibenzofuran Derivatives as Potential Antimicrobial Agents against Antibiotic-Resistant Bacteria

The escalating prevalence of antibiotic-resistant bacteria has led to a serious global public health problem; therefore, there is an urgent need for the development of structurally innovative antibacterial agents. In our study, a series of biphenyl and dibenzofuran derivatives were designed and synthesized by Suzuki-coupling and demethylation reactions in moderate to excellent yields (51–94% yield). Eleven compounds exhibited potent antibacterial activities against the prevalent antibiotic-resistant Gram-positive and Gram-negative pathogens, among which compounds 4′-(trifluoromethyl)-[1,1′-biphenyl]-3,4,5-triol (6i) and 5-(9H-carbazol-2-yl) benzene-1,2,3-triol (6m) showed the most potent inhibitory activities against methicillin-resistant Staphylococcus aureus and multidrug-resistant Enterococcus faecalis with MIC (minimum inhibitory concentration) values as low as 3.13 and 6.25 μg/mL, respectively. Compounds 3′,5′-dimethyl-[1,1′-biphenyl]-3,4,4′,5-tetraol (6e), 4′-fluoro-[1,1′-biphenyl]-3,4,5-triol (6g), and 4′-(trifluoromethyl)-[1,1′-biphenyl]-3,4,5-triol (6i) showed comparable inhibitory activities with ciprofloxacin to Gram-negative bacterium carbapenems-resistant Acinetobacter baumannii. Study of the structure–activity relationship indicated that a strong electron-withdrawing group on the A ring and hydroxyl groups on the B ring of biphenyls were beneficial to their antibacterial activities, and for benzo-heterocycles, N-heterocycle exhibited optimal antibacterial activity. These results can provide novel structures of antibacterial drugs chemically different from currently known antibiotics and broaden prospects for the development of effective antibiotics against antibiotic-resistant bacteria.     

Evaluation of the Antioxidant and Antifungal Actions of the Optimized Crude Extract and Fractions from the Aerial Parts of Acanthospermum hispidum

This study investigated the phytochemical characteristics of the aerial parts of Acanthospermum hispidum, by chromatographic and spectrophotometric methods, and evaluated the antioxidant and antifungal activities of the crude extract and polyphenol-enriched fractions of the species. The phytochemical prospection showed the presence of polyphenols from the groups of hydroxycinnamic derivatives and flavonoids in the crude extract (CE) and fractions of the aerial parts of A. hispidum. In the chromatographic analysis, it was possible to observe that the fractionation process of the CE with hexane and ethyl acetate was efficient in enriching the fractions in phenolic compounds. This enrichment provided an increase in antioxidant activity by the DPPH and ABTS methods, in which it was observed a higher antioxidant activity for EAF in the DPPH test and higher activity against the ABTS radical by the fractions AqF and RAqF. The extract and fractions were effective against Candida non-Candida albicans strains, mainly against C. glabrata, C. parapsilosis and C. krusei, acting predominantly fungicidal. The results indicate that the aerial parts of A. hispidum can serve as a basis for the development of new antioxidant and antifungal products. Moreover, the fractionation process can contribute to increasing the biological potential of the species.     

Comparative Analysis of Antioxidant,Anticholinesterase, and Antibacterial Activity of Microbial Chondroitin Sulfate and Commercial Chondroitin Sulfate

Chondroitin synthesis was performed using the recombinant Escherichia coli(C2987) strain created by transforming the plasmid pETM6-PACF-vgb, which carries the genes responsible for chondroitin synthesis, kfoA, kfoC, kfoF, and the Vitreoscilla hemoglobin gene (vgb). Then, Microbial chondroitin sulfate (MCS)’s antioxidant, anticholinesterase, and antibacterial activity were compared with commercial chondroitin sulfate (CCS). The antioxidant studies revealed that the MCS and CCS samples could be potential targets for scavenging radicals and cupric ion reduction. MCS demonstrated better antioxidant properties in the ABTS assay with the IC50 value of 0.66 mg than CCS. MCS showed 2.5-fold for DPPH and almost 5-fold for ABTS⋅+ (with a value of 3.85 mg/mL) better activity than the CCS. However, the compounds were not active for cholinesterase enzyme inhibitions. In the antibacterial assay, the Minimum inhibitory concentration (MIC) values of MCS against S. aureus, E. aerogenes, E. coli, P. aeruginosa, and K. pneumoniae (0.12, 0.18, 0.12, 0.18, and 0.18 g/mL, respectively) were found to be greater than that of CCS (0.42, 0.48, 0.36, 0.36, and 0.36 g/mL, respectively). This study demonstrates that MCS is a potent pharmacological agent due to its physicochemical properties, and its usability as a therapeutic-preventive agent will shed light on future studies.     

Optimizing the Production of Antioxidant and Antibacterial Alkaloids from Macleaya cordata by Subcritical Water Extraction Technology

In this work, the subcritical water extraction technology was used to extract alkaloids from Macleaya cordata, and the effects of extraction temperature and time on its yield were investigated to find the best extraction conditions. Moreover, the antioxidant capacity and antibacterial activity of Macleaya cordata extract were studied. Furthermore, through the single-factor method, it was found that properly increasing the extraction temperature and prolonging the extraction time was conducive to increasing alkaloid yield. Still, a considerable amount of alkaloids might be decomposed by heat, resulting in a decrease in their yield. The results showed that the optimal extraction temperature of alkaloids from Macleaya cordata with subcritical water is 190 °C, the time is 45 min, and the corresponding maximum yield is 35.19±0.12 mg/g (sanguinarine equivalent in raw materials). In addition, the antioxidation and bacteriostasis abilities of subcritical water extract are better than those of traditional hot water extract, indicating that it is a feasible method to extract alkaloids from Macleaya cordata with subcritical water.     

蔓茎堇菜和柔毛堇菜多糖的抑菌抗氧化活性

利用乙醇沉淀法提取蔓茎堇菜Viola diffusa和柔毛堇菜V.principis多糖并分别进行抑菌及抗氧化试验。结果表明,蔓茎堇菜和柔毛堇菜多糖提取率分别为7.0%和8.3%。不同倍数体积无水乙醇沉淀提取的多糖抑菌和抗氧化能力不同。抑菌效果显示,蔓茎堇菜多糖对大肠杆菌和枯草芽孢杆菌的抑菌圈分别可达8.46mm和8.59mm,柔毛堇菜对大肠杆菌和枯草芽孢杆菌的抑菌圈均可达9.13mm,但两种堇菜多糖对黑曲霉和啤酒酵母未呈现抑制活性;抗氧化研究发现,蔓茎堇菜多糖抗氧化活性为243.64U·mL^-1,柔毛堇菜多糖抗氧化活性为411.78U·mL^-1。由此可见,无论是抑菌还是抗氧化活性方面,柔毛堇菜极显著优于蔓茎堇菜(P<0.01)。蔓茎堇菜和柔毛堇菜多糖都具有一定的抑菌抗氧化活性,均可作为食药两用植物资源进行开发利用。     

Analysis of Chemical Composition and Assessment of Antioxidant,Cytotoxic and Synergistic Antibacterial Activities of Essential Oils from Different Plant Parts of Piper boehmeriifolium

The essential oils (EOs) from leaves, stems, and whole plant of Piper boehmeriifolium were analyzed using GC/FID and GC/MS. The main constituents of P. boehmeriifolium EOs were β‐caryophyllene, caryophyllene oxide, β‐elemene, spathulenol, germacrene D, β‐selinene, and neointermedeol. The antioxidant potential of the EOs were determined using DPPH^?, ABTS^?+ and FRAP assays. In ABTS^?+ assay, the leaf oil exhibited a remarkable activity with an IC₅₀ value of 7.36 μg/mL almost similar to BHT (4.06 μg/mL). Furthermore, the antibacterial activity of the oils as well as their synergistic potential with conventional antibiotics were evaluated using microdilution and Checkerboard assays. The results revealed that the oils from different parts of P. boehmeriifolium inhibited the growth of all tested bacteria and the minimum inhibitory concentrations were determined to be 0.078 – 1.250 mg/mL. In combination with chloramphenicol or streptomycin, the oils showed significant synergistic antibacterial effects in most cases. Besides, the results of MTT assay indicated that the oil of the whole plant exhibited significant cytotoxic activities on human hepatocellular carcinoma cells (HepG2) and human breast cancer cells (MCF‐7). In summary, the P. boehmeriifolium oils could be regarded as a prospective source for pharmacologically active compounds.     

Synthesis of Schiff Bases and Secondary Amines with Indane Skeleton; Evaluation of Their Antioxidant,Antibiotic, and Antifungal Activities

In this study, Schiff bases were synthesized by utilizing the reaction of 4- and 5-aminoindane with substituted benzaldehydes. After the reduction of isolated Schiff bases with NaBH₄, the corresponding secondary amine derivatives were obtained. The structures of all synthesized molecules were confirmed by ¹H-NMR, ¹³C-NMR, FT-IR, and ESI-MS. Antioxidant activities of all synthesized molecules were investigated by DPPH method, and IC₅₀ values were calculated. In addition, antibacterial activities of targets were investigated by the well diffusion method, and then MIC99 values were calculated. While only four of the sixteen synthesized molecules showed a high level of antioxidant activity, all of the molecules exhibited biological activity against Gram-positive and Gram-negative bacteria to varying degrees. In addition, all the synthesized molecules showed high antifungal activity. In antioxidant capacity studies, the IC₅₀ values of 2-(((2,3-dihydro-1H-inden-5-yl)amino)methyl)-6-methoxyphenol ( 4 d ) and 2-(((2,3-dihydro-1H-inden-4-yl)amino)methyl)-6-methoxyphenol ( 7 d ) were determined to be 18.1 μg and 35.1 μg, respectively, and these values are much stronger than BHT (butylated hydroxytoluene) and BHA (butylated hydroxyanisole) used as positive controls. The fact that targets have the same core structure with different substituents has revealed a good structure-activity relationship.     

Chemical Composition,Antibacterial, Antioxidant and in Vitro Antidiabetic Activities of Essential Oils from Eruca vesicaria

This work describes the study of the chemical composition and bioactivity of the essential oils (EOs) of the different organs (leaves, flowers, stems and roots) from Eruca vesicaria. According to the GC and GC/MS analysis, all the EOs were dominated by erucin (4‐methylthiobutyl isothiocyanate) with a percentage ranging from 17.9 % (leaves) to 98.5 % (roots). The isolated EOs were evaluated for their antioxidant (DPPH, ABTS and β‐carotene/linoleic acid), antibacterial and inhibitory property against α‐amylase and α‐glucosidase. Most EOs exhibited an interesting α‐glucosidase and α‐amylase inhibitory potential. The roots essential oil was found to be the most active with IC₅₀ values of 0.80±0.06 and 0.11±0.01 μg mL^?1, respectively. The essential oil of roots exhibited the highest antioxidant activity (DPPH, PI=92.76±0.01 %; ABTS, PI=78.87±0.19; and β‐carotene, PI=56.1±0.01 %). The isolated oils were also tested for their antibacterial activity against two Gram‐positive and three Gram‐negative bacteria. Moderate results have been noted by comparison with Gentamicin used as positive control.     

Synthesis,Cytotoxic, and Antibacterial Evaluation of Quinazolinone Derivatives with Substituted Amino Moiety

A series of novel quinazolinone derivatives containing a substituted amino moiety were synthesized, evaluated for their cytotoxic and antibacterial activities. The results of MTT assay showed that all synthesized target compounds 5A  –  5O showed potent cytotoxicity against SGC‐7901 (IC₅₀, 0.72 – 1.41 μm ). Moreover, the compounds 5D , 5I , and 5K showed better selectivity as compared with positive controls pemetrexed and MTX due to weak cytotoxicity against normal tissue cell line HUVSMC. Among synthesized compounds, the compounds 5E , 5J , 5L , and 5N showed broad‐spectrum cytotoxic activities against at least four cancer cell lines at a micromolar level. The results of antibacteria evaluation revealed that all synthesized compounds showed good to moderate antibacterial activities against Gram‐negative bacteria Escherichia coli. Among them, the MIC values of the compounds 5C , 5F , and 5M were 0.31 μg/mL.