Wide Spectrum Of Biological Properties Research Articles

Exploring the Antimicrobial Properties of 99 Natural Flavour and Fragrance Raw Materials against Pathogenic Bacteria: A Comparative Study with Antibiotics

Currently, one of the most serious global problems is the increasing incidence of infectious diseases. This is closely related to the increase in antibiotic use, which has resulted in the development of multidrug resistance in microorganisms. Another problem is the numerous microbiological contaminations of cosmetic products, which can lead to dangerous bacterial infections in humans. Natural fragrance raw materials exhibit a wide spectrum of biological properties, including antimicrobial properties. Despite their prevalence and availability on the commercial market, there is little research into their effects on multidrug-resistant microorganisms. This study examines the inhibitory effect of natural substances on Gram-positive and Gram-negative bacteria. For this purpose, screening and appropriate assays were carried out to determine the minimum inhibitory concentration (MIC) value of individual substances, using the alamarBlueTM reagent. The lowest MIC values were observed for Staphylococcus aureus (black seed (Nigella sativa) expressed oil, MIC = 25 µg/mL), Kocuria rhizophila (fir balsam absolute, MIC = 12.5 µg/mL), and Pseudomonas putida (cubeb oil and fir balsam absolute, MIC = 12.5 µg/mL). The most resistant Gram-negative species was Enterobacter gergoviae, while Staphylococcus epidermidis was the most resistant Gram-positive species.

Microwave-assisted Synthesis of Pharmacologically Active 4-Phenoxyquinolines and their Benzazole-quinoline Hybrids Through SNAr Reaction of 4,7-dichloroquinoline and Phenols Using [bmim][PF6] as a Green Solvent.

Quinoline and its derivatives have been shown to display a wide spectrum of biological properties, especially anticancer activity. Particularly, diverse potent anticancer drugs are based on the 4-phenoxyquinoline skeleton, acting as small-molecules VEGR2 and/or c-Met kinase inhibitors. However, the design of new drugs based on these quinoline derivatives remains a challenge. Up till now, all approaches to 4-phenoxyquinoline skeleton construction do not obey any green chemistry principles. Developing a new, and efficient protocol for the synthesis of potentially bioactive 4-phenoxyquinoline derivatives and benzazole-quinoline-quinoline hybrids from commercially available 4,7-dichloroquinoline and phenol derivatives using microwave energy (MW) in the presence of 1-methyl 3-butylimidazolium hexafluorophosphate. Neweco-efficient protocol for valuable 7-chloro-4-phenoxyquinolines and their hybrids, which is based on SNAr reaction of 4,7-dichloroquinoline with respective simple phenols and hydroxyaryl- benzazoles under MWenergy in green reaction media, is studied for the first time. We found that among various solvents tested, the ionic liquid 1-methyl 3-butylimidazolium hexafluorophosphate ([bmim][PF6]) favored the SNAr reaction affording phenoxyquinolines in excellent yields (72-82%) in 10 min. The developed protocol allowed to obtain quickly in good yields (48-60%) new diverse benzazole-quinoline hybrids, which are expected to be pharmacologically active. According to the calculated bioactivity scores, new hybrids are potential kinase inhibitors that could be useful in anticancer drug research. We developed for the first time a new green, efficient method to prepare potentially bioactive functionalized 7-chloro-4-phenoxyquinolines and benzazole-quinoline molecules. Good to excellent yields of the quinoline products, use of MW irradiation in ([bmim] [PF6] as a green solvent, and short times of reactions are some of the main advantages of this new protocol.

Building a tissue: gingiva- and adipose-derived mesenchymal cell spheroids’ survivability and functionality after 3D extrusion bioprinting

While being the most extensively used cell type for spheroid-based 3D extrusion bioprinting, mesenchymal stromal cells (MSCs) provide a wide spectrum of biological properties depending on their origin. Understanding the specifics of each heterogeneous MSCs population subgroup would allow one to increase the survivability and functionality of the constructed tissue analogues. To answer this need, this study assessed the survivability, metabolic activity, proliferation, sprouting, migration, and differentiation capacity of MSCs spheroids depending on the cell source (adipose tissue, AT-MSCs/gingiva, G-MSCs) and on the tissue construct's geometry (bioprinted/manually mixed). This study has demonstrated that the cell origin defines the dynamics of spheroid reactivation, resulting in a varying construct's morphology after a 14-days-long cultivation period. AT-MSCs migrate in the hydrogel faster, forming clusters of wide and short sprouts. G-MSCs, oppositely, produce thin, long, and branched sprouts. Hence, AT-MSCs can quickly populate the hydrogel volume, achieving a high cell density, while G-MSCs can cover larger areas, but with a more sprout-like phenotype.

Ethnomedicinal Use, Phytochemistry, Pharmacology, and Toxicology of Euphorbia resinifera O. Berg. (B): A Review

Euphorbia resinifera (Zaggûm or Tikiut) is an endemic species of Morocco that grows in the Middle Atlas Mountain range. It is used in folk medicine to treat several diseases, especially various types of cancer. Aim of the review: In this review, we critically highlighted and discussed previous reports on E. resinifera, concerning its botanical description, taxonomy, geographical distribution, and medicinal use. In addition, bioactive compounds, toxicology, and pharmacological effects were reported. Materials and methods: We searched various scientific databases, such as Scopus, PubMed, Web of Science, SpringerLink, SciFinder, Wiley Online, and Google Scholar, to collect data on E. resinifera. Studies involving E. resinifera or its bioactive compounds with regards to antitumor, anti-inflammatory, antileishmanial, antiprotease, immunomodulatory, irritant, and lysosomal activities are discussed here. Results: E. resinifera has been widely used in folk medicine practice in Morocco to treat several diseases such as diabetes, cancer, and inflammatory skin conditions, as well as to heal wounds. In phytochemistry studies, biochemical compounds have been identified from E. resinifera belonging specially to terpenoids. Indeed, in vitro and in vivo pharmacological investigations showed that extracts and compounds from the latex of E. resinifera exhibited a wide spectrum of biological properties, particularly antioxidant, antimicrobial, antitumor, anti-inflammatory, antileishmanial, and immunomodulatory and neuroprotective activities. Conclusion: The use of E. resinifera in conventional medicine is supported by processes founded on biological evidence. However, in-depth research is necessary to prove the safety and efficacy of E. resinifera latex extracts and their compounds and to clarify their pharmacological mechanisms. In addition, pharmacokinetic and pharmacodynamics studies are required for extracts and bioactive compounds.

Screening of Chemical Composition, Antimicrobial and Antioxidant Activities of Essential Oil and Volatile Fraction from Olive Mill Wastewater

Oil mill wastewater is the main by-product of the olive oil industry resulting mainly from the treatment and pressing of olives in mills. It is a rich source of nutrients and phytochemicals with a wide spectrum of biological properties. The present study focuses on the chemical analysis and evaluation of the antimicrobial and antioxidant activity of the essential oil (EO) and the volatile fraction (VF) obtained, respectively, by hydrodistillation. Chemical analysis by gas chromatography coupled to mass spectrometry (GC/MS) and a flame ionisation detector (GC/FID) revealed the predominance of phenolic compounds (25.71%, 60.36%) and fatty acids (62.37%, 38.25%) for the VF and EO, respectively. It was also shown that the main compounds were oleic acid (24.9%) for the VF and 4-ethylphenol (28.5%) for the EO. The results of the antimicrobial activity in terms of MIC values against twelve microorganisms showed that, overall, the VF was more active than the EO. The antioxidant activity of the VF and EO was evaluated using the DPPH assay and expressed as half-maximal inhibitory concentration (IC50), where the EO (218 μg/mL) showed better antioxidant activity than the VF (244 μg/mL). The results also revealed that the antimicrobial activity and antioxidant activity values for both oils were significantly lower than the standards used.

Synthetic Mono-Carbonyl Curcumin Analogues Attenuate Oxidative Stress in Mouse Models.

Alzheimer’s disease is the commonest form of dementia associated with short-term memory loss and impaired cognition and, worldwide, it is a growing health issue. A number of therapeutic strategies have been studied to design and develop an effective anti-Alzheimer drug. Curcumin has a wide spectrum of biological properties. In this regard, the antioxidant potentials of mono-carbonyl curcumin analogues (h1–h5) were investigated using in vitro antioxidant assays and hippocampal-based in vivo mouse models such as light–dark box, hole board, and Y-maze tests. In the in vitro assay, mono-carbonyl curcumin analogues h2 and h3 with methoxy and chloro-substituents, respectively, showed promising 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2, 2′-azinobis-3-ethylbenzothiazo-line-6-sulfonate (ABTS) free radical scavenging activities. In the in vivo studies, scopolamine administration significantly (p < 0.001) induced oxidative stress and memory impairment in mice, in comparison to the normal control group. The pretreatment with mono-carbonyl curcumin analogues, specifically h2 and h3, significantly decreased (123.71 ± 15.23 s (p < 0.001), n = 8; 156.53 ± 14.13 s (p < 0.001), n = 8) the duration of time spent in the light chamber and significantly enhanced (253.95 ± 19.05 s (p < 0.001), n = 8, and 239.57 ± 9.98 s (p < 0.001), n = 8) the time spent in the dark compartment in the light–dark box arena. The numbers of hole pokings were significantly (p < 0.001, n = 8) enhanced in the hole board test and substantially increased the percent spontaneous alternation performance (SAP %) in the Y-maze mouse models in comparison to the stress control group. In the biomarker analysis, the significant reduction in the lipid peroxidation (MDA) level and enhanced catalase (CAT), superoxide dismutase (SOD), and glutathione (GSH) activities in the brain hippocampus reveal their antioxidant and memory enhancing potentials. However, further research is needed to find out the appropriate mechanism of reducing oxidative stress in pathological models.

Thin-Layer Chromatography (TLC) in the Screening of Botanicals-Its Versatile Potential and Selected Applications.

The aim of this paper is to present a comprehensive overview of the main aims and scopes in screening of botanicals, a task of which thin-layer chromatography (TLC) is, on an everyday basis, confronted with and engaged in. Stunning omnipresence of this modest analytical technique (both in its standard format (TLC) and the high-performance one (HPTLC), either hyphenated or not) for many analysts might at a first glance appear chaotic and random, with an auxiliary rather than leading role in research, and not capable of issuing meaningful final statements. Based on these reflections, our purpose is not to present a general review paper on TLC in screening of botanicals, but a blueprint rather (illustrated with a selection of practical examples), which highlights a sovereign and important role of TLC in accomplishing the following analytical tasks: (i) solving puzzles related to chemotaxonomy of plants, (ii) screening a wide spectrum of biological properties of plants, (iii) providing quality control of herbal medicines and alimentary and cosmetic products of biological origin, and (iv) tracing psychoactive plants under forensic surveillance.

Chalcone Derivatives for Biological Potentials: A Strategy of Molecular Hybridization for Drug Design

Naturally and synthetically derived hybrid molecules are promising sources for new drug development due to their multiple modes of action and other advantages. Chalcone, two important classes of synthetic chemistry affording diverse pharmacological activities, make themselves ideal blocks for building a chalcone hybrid scaffold as a bioactive agent. Provoked by the promising medicinal applications of such hybrids, the scientific community has reported dozens of chalcone hybrids with a wide spectrum of biological properties including anticancer, antimicrobial, antimalarial, antioxidant, antianxiety and so on, through synthetic hybridization strategy. It is expected to assist medicinal chemists in the effective and successful development of chalcone hybrids. In view of these observations, we herein report the literature review of Chalcone hybrids which possessing antimicrobial antioxidant and antianxiety potential. Key words: Chalcone, Molecular hybridization, Biological potentials.

Synergistic effects of carvacrol, \u03b1-terpinene, \u03b3-terpinene, \u03c1-cymene and linalool against Gardnerella species

Bacterial vaginosis (BV) is the most common vaginal infection affecting women worldwide. This infection is characterized by the loss of the dominant Lactobacillus community in the vaginal microbiota and an increase of anaerobic bacteria, that leads to the formation of a polymicrobial biofilm, mostly composed of Gardnerella spp. Treatment of BV is normally performed using broad-spectrum antibiotics, such as metronidazole and clindamycin. However, the high levels of recurrence of infection after treatment cessation have led to a demand for new therapeutic alternatives. Thymbra capitata essential oils (EOs) are known to have a wide spectrum of biological properties, including antibacterial activity. Thus, herein, we characterized two EOs of T. capitata and tested their antimicrobial activity as well as some of their main components, aiming to assess possible synergistic effects. Our findings showed that carvacrol and ρ-cymene established a strong synergistic antimicrobial effect against planktonic cultures of Gardnerella spp. On biofilm, carvacrol and linalool at sub-MIC concentrations proved more efficient in eliminating biofilm cells, while showing no cytotoxicity observed in a reconstituted human vaginal epithelium. The antibiofilm potential of the EOs and compounds was highlighted by the fact cells were not able to recover culturability after exposure to fresh medium.

Advances on Quinazoline Based Congeners for Anticancer Potential

The heterocyclic compounds have a great significance in medicinal chemistry because they have extensive biological activities. Cancer is globally the leading cause of death and it is a challenge to develop appropriate treatment for the management of cancer. Continuous efforts are being made to find a suitable medicinal agent for cancer therapy. Nitrogencontaining heterocycles have received noteworthy attention due to their wide and distinctive pharmacological activities. One of the most important nitrogen-containing heterocycles in medicinal chemistry is ‘quinazoline’ that possesses a wide spectrum of biological properties. This scaffold is an important pharmacophore and is considered a privileged structure. Various substituted quinazolines displayed anticancer activity against different types of cancer. This review highlights the recent advances in quinazoline based molecules as anticancer agents. Several in-vitro and in-vivo models used along with the results are also included. A subpart briefing natural quinazoline containing anticancer compounds is also incorporated in the review.

Green and Facile Synthesis and Antioxidant and Antibacterial Evaluation of Dietary Myricetin-Mediated Silver Nanoparticles.

Myricetin (MY) is a dietary flavonoid which exhibits a wide spectrum of biological properties, viz., antibacterial, antioxidant, anticancer, and so forth. The lower solubility in aqueous medium and hence lesser bioavailability of MY limits the use of such dietary flavonoids in further in vivo research. To overcome bioavailability limitations, a number of drug-delivery systems are being investigated. Herein, MY-mediated silver nanoparticles (MY-AgNPs) were synthesized by a green approach to improve the therapeutic efficacy of MY. MY-AgNPs were characterized by ultraviolet–visible spectroscopy (UV–Vis), scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier transform infrared (FTIR) spectroscopy, and X-ray powder diffraction (XRD). The results showed that the dispersion of AgNPs had the maximum UV–vis absorption at about 410 nm. The synthesized nanoparticles were almost spherical. MY-AgNPs were further investigated against human pathogenic bacteria, and their antioxidant potential was also determined. The free radical scavenging rate was about 60–87%. MY-AgNPs had good antibacterial activity against Escherichia coli and Salmonella at room temperature with minimum inhibitory concentrations of 10–4 and 10–5 g/L, respectively.

Current Trends on Repurposing and Pharmacological Enhancement of Andrographolide.

Andrographolide, the main bioactive component separated from Andrographis paniculata in 1951, has been scrutinized with a modern drug discovery approach for anti-inflammatory properties since 1984. Identification of new uses of existing drugs can be facilitated by searching for evidence linking them to known or yet undiscovered drug targets and human disease states to develop new therapeutic indications.Furthermore, a wide spectrum of biological properties of andrographolide such as anticancer, antibacterial, antiviral, hepatoprotective, antioxidant, anti-malarial, anti-atherosclerosis are also reported. However, poor water solubility and instability limit its clinical application. It becomes crucial to enhance its pharmacological function and find a new treatment option for more diseases. Therefore, this article reviews the major recent developments in andrographolide, including repurposing applications in different diseases and underlying mechanisms, particularly focusing on pharmacological enhancement of andrographolide such as derivatives, chemical modifications with potent biological activity and drug delivery. The repurposing and pharmacological enhancement of andrographolide would not only have exciting therapeutic potential to different diseases to facilitate drug marketing, but also decrease the economic burden on healthcare worldwide.

Spectroscopic, Theoretical and Antioxidant Study of 3d-Transition Metals (Co (II), Ni(II), Cu(II), Zn(II) Complexes with Cichoric Acid.

Cichoric acid (CA) is a derivative of both caffeic acid and tartaric acid. It was isolated for the first time from Cichorium intybus L. (chicory) but it also occurs in significant amounts in Echinacea, particularly E. purpurea, dandelion leaves, basil, lemon balm and in aquatic plants, including algae and sea grasses. It has a wide spectrum of biological properties, including antioxidant, antiviral, anti-inflammatory and other. The work yielded cichoric acid complexes with selected transition metals, i.e., copper(II), nickel(II), zinc(II) and cobalt(II). In this work the dependency between the molecular structure and biological activity was discussed. The molecular structure was studied by means of infrared spectroscopy (Fourier transform infrared (FT-IR) Raman (FT-Raman)), electronic absorption spectroscopy (ultraviolet–visible (UV/VIS)) and theoretical calculations (density functional theory (DFT), Hartree–Fock (HF)). Understanding the mechanism of the effect of metals on the electronic system of ligands with biological importance will facilitate in the future the search for new, effective and natural antioxidants. The composition of the studied complexes in aqueous solutions was determined at a constant pH by the Job’s method. Antioxidative properties of the tested compounds were determined using the ferric-reducing antioxidant power (FRAP), DPPH (2,2-diphenyl-1-picryl-hydrazyl-hydrate free radical method), cupric-reducing antioxidant capacity (CUPRAC) and Superoxide Dismutase Activity Assay (SOD).

Synthetic Strategies and Biological Potential of Coumarin-Chalcone Hybrids: A New Dimension to Drug Design

Privileged scaffolds are ubiquitous as effective templates in drug discovery regime. Natural and synthetically derived hybrid molecules are one such attractive scaffold for therapeutic agent development due to their dual or multiple modes of action, minimum or no side effects, favourable pharmacokinetics and other advantages. Coumarins and chalcone are two important classes of natural products affording diverse pharmacological activities which make them ideal templates for building coumarin-chalcone hybrids as effective biological scaffold for drug discovery research. Provoked by the promising medicinal application of hybrid molecules as well as those of coumarins and chalcones, the medicinal chemists have used molecular hybridisation strategy to report dozens of coumarin- chalcone hybrids with a wide spectrum of biological properties including anticancer, antimicrobial, antimalarial, antioxidant, anti-tubercular and so on. The present review provides a systematic summary on synthetic strategies, biological or chemical potential, SAR studies, some mechanisms of action and some plausible molecular targets of synthetic coumarin-chalcone hybrids published from 2001 till date. The review is expected to assist medicinal chemists in the effective and successful development of coumarin- chalcone hybrid based drug discovery regime.

Aryl Quinazolinone Derivatives as Novel Therapeutic Agents against Brain-Eating Amoebae.

Naegleria fowleri and Balamuthia mandrillaris are protist pathogens that infect the central nervous system, causing primary amoebic meningoencephalitis and granulomatous amoebic encephalitis with mortality rates of over 95%. Quinazolinones and their derivatives possess a wide spectrum of biological properties, but their antiamoebic effects against brain-eating amoebae have never been tested before. In this study, we synthesized a variety of 34 novel arylquinazolinones derivatives (Q1-Q34) by altering both quinazolinone core and aryl substituents. To study the antiamoebic activity of these synthetic arylquinazolinones, amoebicidal and amoebistatic assays were performed against N. fowleri and B. mandrillaris. Moreover, amoebae-mediated host cells cytotopathogenicity and cytotoxicity assays were performed against human keratinocytes cells in vitro. The results revealed that selected arylquinazolinones derivatives decreased the viability of B. mandrillaris and N. fowleri significantly (P < 0.05) and reduced cytopathogenicity of both parasites. Furthermore, these compounds were also found to be least cytotoxic against HaCat cells. Considering that nanoparticle-based materials possess potent in vitro activity against brain-eating amoebae, we conjugated quinazolinones derivatives with silver nanoparticles and showed that activities of the drugs were enhanced successfully after conjugation. The current study suggests that quinazolinones alone as well as conjugated with silver nanoparticles may serve as potent therapeutics against brain-eating amoebae.

Autophagy inhibition enhances Matrine derivative MASM induced apoptosis in cancer cells via a mechanism involving reactive oxygen species-mediated PI3K/Akt/mTOR and Erk/p38 signaling

BackgroundIn the quest for new anti-cancer drugs, the drug discovery process has shifted to screening of active ingredients in traditional eastern medicine. Matrine is an active alkaloid isolated from plants of the Sophora genus used in traditional Chinese herbal medicine that exhibits a wide spectrum of biological properties and has a potential as an anti-proliferative agent. In this study, we investigated the anticancer property of MASM, ([(6aS, 10S, 11aR, 11bR, 11cS)210-Methylamino-dodecahydro-3a, 7a-diaza-benzo (de)anthracene-8-thione]), a potent derivative of matrine.MethodsFour epithelial cancer cell lines representing the dominant cancers, namely: A549 (non-small-cell lung cancer cell line), MCF-7 and MDA-MB-231 (breast cancer cell lines), and Hela (cervical cancer cell line) were employed, and the mechanistic underpinning of MASM-induced apoptosis was investigated using flow cytometry, western blot and immunofluorescence.ResultsMASM, induced apoptosis via caspase 3 dependent and independent pathways, and autophagy in all the four cancer cell lines, but post-EMT (epithelial mesenchymal transition) cells showed greater sensitivity to MASM. Scavenging reactive oxygen species using N-acetylcysteine rescued all cancer cell lines from apoptosis and autophagy. Mechanistic analysis revealed that MASM induced autophagy involves inhibition of Akt signaling and the activation of Erk and p38 signaling, and inhibition of autophagy further enhanced the apoptosis induced by MASM.ConclusionsThese results indicate that MASM possesses potency against cancer cells and modulating autophagy during MASM administration could be used to further enhance its therapeutic effects.

Agastache rugosa Kuntze Attenuates UVB-Induced Photoaging in Hairless Mice through the Regulation of MAPK/AP-1 and TGF-β/ Smad Pathways.

Chronic exposure to ultraviolet (UV) radiation, regarded as a major cause of extrinsic aging or photoaging characterized by wrinkle formation and skin dehydration, exerts adverse effects on skin by causing the overproduction of reactive oxygen species. Agastache rugosa Kuntze, known as Korean mint, possesses a wide spectrum of biological properties including antioxidation, anti-inflammation, and anti-atherosclerosis. Previous studies have reported that A. rugosa protected human keratinocytes against UVB irradiation by restoring the anti-oxidant defense system. However, the anti-photoaging effect of A. rugosa extract (ARE) in animal models has not yet been evaluated. ARE was orally administered to hairless mice at doses of 100 or 250 mg/kg/day along with UVB exposure for 12 weeks. ARE histologically improved UVB-induced wrinkle formation, epidermal thickening, erythema, and hyperpigmentation. In addition, ARE recovered skin moisture by improving skin hydration and transepidermal water loss (TEWL). Along with this, ARE increased hyaluronic acid levels by upregulating HA synthase genes. ARE markedly increased the density of collagen and the amounts of hydroxypoline via two pathways. First, ARE significantly downregulated the mRNA expression of matrix metalloproteinases responsible for collagen degradation by inactivating the mitogen-activated protein kinase/activator protein 1 pathway. Second, ARE stimulated the transforming growth factor beta/Smad signaling, consequently raising the mRNA levels of collagen-related genes. In addition, ARE not only increased the mRNA expression of antioxidant enzymes but also decreased inflammatory cytokines by blocking the protein expression of nuclear factor kappa B. Collectively, our findings suggest that A. rugosa may be a potential preventive and therapeutic agent for photoaging.

New insight on the structural diversity of holothurian fucosylated chondroitin sulfates

Abstract Fucosylated chondroitin sulfates (FCS) are unique glycosaminoglycans isolated from body walls of sea cucumbers (holothuria). These biopolymers are composed of a chondroitin core [→4)-β-D-GlcA-(1→3)-β-D-GalNAc-(1→]n bearing fucosyl branches and sulfate groups. Structural variations of FCS are species specific and depend on type, amount and position of branches, as well as on degree and pattern of sulfation of a backbone and branches. A wide spectrum of biological properties was determined for these polysaccharides including anticoagulant, antithrombotic, antitumor, anti-inflammatory activities. Structural features of FCS influence significantly on their biological effect. In this review recent data about structural variations within holothurian FCS are summarized. The NMR data of the key building blocks are presented, which may be used for the analysis of new FCS.

Antibacterial activity of newer Quinazolin-4(3H)-one derivatives

Event Abstract Back to Event Antibacterial activity of newer Quinazolin-4(3H)-one derivatives Gopal Natesan1*, Appalaraju Velaga1, Nelycia Su Yean Tze1 and Soon An Nie1 1 Faculty of Pharmacy, Mahsa University, Malaysia Background Heterocyclic chemistry has gained remarkable attention recently due to its pharmacological diversity in medicinal chemistry research. Quinazolin-4(3H)-one pharmacophore is one of the most important heterocycles, which possess wide spectrum of biological properties like antimicrobial, anticonvulsant, anti-inflammatory and anticancer activities. Hence, this pharmacophore has been considered as a privileged structure to introduce many bioactive moieties to its nucleus for creating new prospective medicinal agents. Methods Quinazolinone derivatives were synthesized by reacting anthranilic acid with benzoyl chloride/4-methoxy benzoyl chloride followed by condensation with hydrazine hydrate, which was further subjected to Schiff base reaction with the different aromatic/heterocyclic aldehydes. The structures of all newly synthesized compounds were characterized by using FT-IR, H1 NMR Spectra. Ten (10) final compounds and two (2) intermediates were evaluated for their antibacterial property against gram-positive (Staphylococcus aureus ATCC 29213 and Bacillus cereus ATCC11778) and gram-negative bacteria (Escherichia coli ATCC 25922 and Pseudomonas aeruginosa ATCC 27853) using agar well diffusion method at a concentration of 50 µg/ml and 100 µg/ml using Norfloxacin as reference drug. Results The parent 2-phenyl-3-amino quinazoline-4(3H)-one (IIa) showed moderate activity against both gram-positive bacteria and gram-negative bacteria whereas substitution of –OCH3 in the phenyl position at the 2nd position of quinazolinone reduces the activity against both strains. The same pattern of the results has been observed among the final Schiff bases. Among the Schiff bases, increase in substitution of –OCH3 group at benzylidene nucleus alters the antibacterial activity. Lower number of methoxy groups exhibited moderate activity against all microorganism whereas increase in number of methoxy group substitution at benzyl-inde nucleus decreases the antibacterial activity against B. cereus and P. aeruginosa and diminishes the activity against S. aureus and E. coli. On the other hand, substitution of a heteryl group at the aldimine in 3-amino quinazolinone pharmacophore significantly increases the antibacterial activity against all the tested bacterial pathogens. Conclusion From the present study, it has been concluded that 2-Phenyl-3-[1-(furfurylidene amino)]-quinazolin-4-(3H)-one (IIIe) showed superior activity among the synthesized compounds. Replacement of benzene ring with heteryl group or substitution of electron donating group in the benzylidene nucleus displayed good antibacterial effects. Keywords: Quinazolin-4(3H)-one, Schiff base, Antibacterial, benzoxazinone, Benzylidene Conference: International Conference on Drug Discovery and Translational Medicine 2018 (ICDDTM '18) “Seizing Opportunities and Addressing Challenges of Precision Medicine”, Putrajaya, Malaysia, 3 Dec - 5 Feb, 2019. Presentation Type: Poster Presentation Topic: Infectious diseases Citation: Natesan G, Velaga A, Yean Tze N and An Nie S (2019). Antibacterial activity of newer Quinazolin-4(3H)-one derivatives. Front. Pharmacol. Conference Abstract: International Conference on Drug Discovery and Translational Medicine 2018 (ICDDTM '18) “Seizing Opportunities and Addressing Challenges of Precision Medicine”. doi: 10.3389/conf.fphar.2018.63.00101 Copyright: The abstracts in this collection have not been subject to any Frontiers peer review or checks, and are not endorsed by Frontiers. They are made available through the Frontiers publishing platform as a service to conference organizers and presenters. The copyright in the individual abstracts is owned by the author of each abstract or his/her employer unless otherwise stated. Each abstract, as well as the collection of abstracts, are published under a Creative Commons CC-BY 4.0 (attribution) licence (https://creativecommons.org/licenses/by/4.0/) and may thus be reproduced, translated, adapted and be the subject of derivative works provided the authors and Frontiers are attributed. For Frontiers’ terms and conditions please see https://www.frontiersin.org/legal/terms-and-conditions. Received: 16 Oct 2018; Published Online: 17 Jan 2019. * Correspondence: Dr. Gopal Natesan, Faculty of Pharmacy, Mahsa University, Bandar Saujana Putra, Malaysia, gopal@mahsa.edu.my Login Required This action requires you to be registered with Frontiers and logged in. To register or login click here. Abstract Info Abstract The Authors in Frontiers Gopal Natesan Appalaraju Velaga Nelycia Su Yean Tze Soon An Nie Google Gopal Natesan Appalaraju Velaga Nelycia Su Yean Tze Soon An Nie Google Scholar Gopal Natesan Appalaraju Velaga Nelycia Su Yean Tze Soon An Nie PubMed Gopal Natesan Appalaraju Velaga Nelycia Su Yean Tze Soon An Nie Related Article in Frontiers Google Scholar PubMed Abstract Close Back to top Javascript is disabled. Please enable Javascript in your browser settings in order to see all the content on this page.

Chinese materia medica used in medicinal diets

Ethnopharmacological relevanceMedicinal diets have a history of more than 2000 years. Locally referred to as yaoshan (Chinese: 药膳), a medicinal diet is understood in China as a dietary product that combines herbs and food with the purpose of preventing and treating diseases or improving health under the guidance of traditional Chinese medicine theory. Medicinal diets are used in Chinese people's daily life and in specialized restaurants. Hundreds of Chinese materia medica (CMM) are used in medicinal diets; however, a comprehensive evaluation of medicinal diets is lacking. Aims of the studyThis is an exploratory study that aims to identify the CMM that are most frequently used in medicinal diets and to provide an updated view of the current situation of medicinal diets in China. Materials and methodsA field study of 1221 people in 32 Chinese provinces was conducted over a period of approximately 6 months and included various types of interviews as well as a written questionnaire. Two approaches were used to analyse the data collected in the survey: (1) estimating the frequency of CMM consumed in daily diets; and (2) collecting CMM used in medicinal diet restaurants. Complementary information on the selected CMM was obtained from relevant databases, including PubMed, Google Scholar, Baidu Scholar, CNKI, and Web of Science. ResultsTen CMM were reported as commonly used by more than 50% of the participants. Among these 10 species, most medicinally used parts were seeds and fruits. Pharmacological data from the literature revealed that these species are associated with a wide spectrum of biological properties, including antitumour (80%), antioxidant (50%), anti-diabetic (40%), antilipemic (40%), anti-aging (40%), antimicrobial (40%) and cardioprotective (40%) activities. Our survey shows that most medicinal diet restaurants are located in the eastern part of China, with the greatest numbers being found in Beijing and Guangzhou. Only Dioscoreae Rhizoma, Lycii Fructus, Chrysanthemi Flos and Longan Arillus were frequently consumed both in daily diets and at medicinal diet restaurants. Some of the similarities shared by these 4 species include an extensive history of use (>2000 years); a sweet flavour; and antioxidant, antidiabetic, antilipemic and cardioprotective effects. ConclusionsThe 10 most commonly consumed CMM possess various biological effects that are currently target the most frequent health problems for the majority of the population. The development of medicinal diet restaurants has certain regional restrictions and is associated with the local climate environment and dietary culture. The data revealed by this study provided useful information for commercial exploitation of medicinal diets and their components and serve as a basis for further studies on various aspects of medicinal diets.