Yasir Anwar, Hisham Faiz Jaha, Mazhar Ul-Islam, Tahseen Kamal, Sher Bahadar Khan, Ihsan Ullah, Saleh M Al-Maaqar, Sameer Ahmed
{"title":"Development of silver-doped copper oxide and chitosan nanocomposites for enhanced antimicrobial activities.","authors":"Yasir Anwar, Hisham Faiz Jaha, Mazhar Ul-Islam, Tahseen Kamal, Sher Bahadar Khan, Ihsan Ullah, Saleh M Al-Maaqar, Sameer Ahmed","doi":"10.1515/znc-2023-0166","DOIUrl":"10.1515/znc-2023-0166","url":null,"abstract":"<p><p>Antimicrobial resistance (AMR) has emerged as a significant and pressing public health concern, posing serious challenges to effectively preventing and treating persistent diseases. Despite various efforts made in recent years to address this problem, the global trends of AMR continue to escalate without any indication of decline. As AMR is well-known for antibiotics, developing new materials such as metal containing compounds with different mechanisms of action is crucial to effectively address this challenge. Copper, silver, and chitosan in various forms have demonstrated significant biological activities and hold promise for applications in medicine and biotechnology. Exploring the biological properties of these nanoparticles is essential for innovative therapeutic approaches in treating bacterial and fungal infections, cancer, and other diseases. To this end, the present study aimed to synthesize silver@copper oxide (Ag@CuO) nanoparticles and its chitosan nanocomposite (Chi-Ag@CuO) to investigate their antimicrobial efficacy. Various established spectroscopic and microscopic methods were employed for characterization purposes, encompassing scanning electron microscopy (SEM), energy-dispersive X-ray spectroscopy (EDX), X-ray diffraction (XRD), and Fourier transform infrared spectroscopy (FTIR). Subsequently, the antimicrobial activity of the nanoparticles was assessed through MIC (minimum inhibitory concentration), MBC (minimum bactericidal concentration), and well-disk diffusion assays against <i>Pseudomonas aeruginosa</i>, <i>Acinetobacter baumannii Staphylococcus aureus</i>, <i>Staphylococcus epidermidis</i>, and <i>Candida albicans</i>. The size of the CuO-NPs, Ag@CuO, and Chi-Ag@CuO NPs was found to be 70-120 nm with a spherical shape and an almost uniform distribution. The nanocomposites were found to possess a minimum inhibitory concentration (MIC) of 5 μg/mL and a minimum bactericidal concentration (MBC) of 250 μg/mL. Moreover, these nanocomposites generated varying clear inhibition zones, with diameters ranging from a minimum of 9 ± 0.5 mm to a maximum of 25 ± 0.5 mm. Consequently, it is evident that the amalgamation of copper-silver-chitosan nanoparticles has exhibited noteworthy antimicrobial properties in the controlled laboratory environment, surpassing the performance of other types of nanoparticles.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":"137-148"},"PeriodicalIF":1.8,"publicationDate":"2024-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141184645","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Exploring chitin: novel pathways and structures as promising targets for biopesticides.","authors":"Malkiet Kaur, Manju Nagpal, Gitika Arora Dhingra, Ankit Rathee","doi":"10.1515/znc-2024-0027","DOIUrl":"10.1515/znc-2024-0027","url":null,"abstract":"<p><p>Chitin, the most prevalent polymer in nature, a significant structural polysaccharide that comes in second only to cellulose. Chitin is a crucial component of fungal cell walls and also present in many other creatures, such as viruses, plants, animals, insect exoskeletons, and crustacean shells. Chitin presents itself as a promising target for the development of biopesticides. It focuses on unraveling the unique structures and biochemical pathways associated with chitin, aiming to identify vulnerabilities that can be strategically leveraged for effective and environmentally sustainable pest control. It involves a comprehensive analysis of chitinase enzymes, chitin biosynthesis, and chitin-related processes across diverse organisms. By elucidating the molecular intricacies involved in chitin metabolism, this review seeks to unveil potential points of intervention that can disrupt essential biological processes in target pests without harming non-target species. This holistic approach to understanding chitin-related pathways aims to inform the design and optimization of biopesticides with enhanced specificity and reduced ecological impact. The outcomes of this study hold great promise for advancing innovative and eco-friendly pest management strategies. By targeting chitin structures and pathways, biopesticides developed based on these findings may offer a sustainable and selective alternative to conventional chemical pesticides, contributing to the ongoing efforts towards more environmentally conscious and effective pest control solutions.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":"125-136"},"PeriodicalIF":1.8,"publicationDate":"2024-05-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140960572","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Ushasi Das, Devesh U Kapoor, Sudarshan Singh, Bhupendra G Prajapati
{"title":"Unveiling the potential of chitosan-coated lipid nanoparticles in drug delivery for management of critical illness: a review.","authors":"Ushasi Das, Devesh U Kapoor, Sudarshan Singh, Bhupendra G Prajapati","doi":"10.1515/znc-2023-0181","DOIUrl":"10.1515/znc-2023-0181","url":null,"abstract":"<p><p>Chitosan (CT), a natural, cationic, chemically stable molecule, biocompatible, biodegradable, nontoxic, polysaccharide derived from the deacetylation of chitin, has very uniquely surfaced as a material of promise for drug delivery and biomedical applications. For the oral, ocular, cutaneous, pulmonary, and nose-to-brain routes, CT-coated nanoparticles (CTCNPs) have numerous advantages, consisting of improved controlled drug release, physicochemical stability, improved cell and tissue interactions, and increased bioavailability and efficacy of the active ingredient. CTCNPs have a broad range of therapeutic properties including anticancer, antiviral, antifungal, anti-inflammatory, antibacterial properties, treating neurological disorders, and other diseases. This has led to substantial research into the many potential uses of CT as a drug delivery vehicle. CT has also been employed in a wide range of biomedical processes, including bone and cartilage tissue regeneration, ocular tissue regeneration, periodontal tissue regeneration, heart tissue regeneration, and wound healing. Additionally, CT has been used in cosmeceutical, bioimaging, immunization, and gene transfer applications. CT exhibits a number of biological activities, which are the basis for its remarkable potential for use as a drug delivery vehicle, and these activities are covered in detail in this article. The alterations applied to CT to obtain the necessary properties have been described.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":"107-124"},"PeriodicalIF":1.8,"publicationDate":"2024-05-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140900095","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Natalia Blicharska, Ziyad Ben Ahmed, Simon Jackson, Dino Rotondo, Veronique Seidel
{"title":"<i>In silico</i> studies on the anti-acne potential of <i>Garcinia mangostana</i> xanthones and benzophenones.","authors":"Natalia Blicharska, Ziyad Ben Ahmed, Simon Jackson, Dino Rotondo, Veronique Seidel","doi":"10.1515/znc-2023-0118","DOIUrl":"10.1515/znc-2023-0118","url":null,"abstract":"<p><p><i>Garcinia mangostana</i> fruits are used traditionally for inflammatory skin conditions, including acne. In this study, an <i>in silico</i> approach was employed to predict the interactions of <i>G. mangostana</i> xanthones and benzophenones with three proteins involved in the pathogenicity of acne, namely the human JNK1, <i>Cutibacterium acnes</i> KAS III and exo-β-1,4-mannosidase. Molecular docking analysis was performed using Autodock Vina. The highest docking scores and size-independent ligand efficiency values towards JNK1, <i>C. acnes</i> KAS III and exo-β-1,4-mannosidase were obtained for garcinoxanthone T, gentisein/2,4,6,3',5'-pentahydroxybenzophenone and mangostanaxanthone VI, respectively. To the best of our knowledge, this is the first report of the potential of xanthones and benzophenones to interact with <i>C. acnes</i> KAS III. Molecular dynamics simulations using GROMACS indicated that the JNK1-garcinoxanthone T complex had the highest stability of all ligand-protein complexes, with a high number of hydrogen bonds predicted to form between this ligand and its target. Petra/Osiris/Molinspiration (POM) analysis was also conducted to determine pharmacophore sites and predict the molecular properties of ligands influencing ADMET. All ligands, except for mangostanaxanthone VI, showed good membrane permeability. Garcinoxanthone T, gentisein and 2,4,6,3',5'-pentahydroxybenzophenone were identified as the most promising compounds to explore further, including in experimental studies, for their anti-acne potential.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":"47-60"},"PeriodicalIF":2.0,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140319634","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Dynamics of alkaloid accumulation in <i>Narcissus</i> cv. Hawera: a source of <i>Sceletium</i>-type alkaloids.","authors":"Borjana Sidjimova, Rumen Denev, Milena Nikolova, Jaume Bastida, Strahil Berkov","doi":"10.1515/znc-2023-0149","DOIUrl":"10.1515/znc-2023-0149","url":null,"abstract":"<p><p>The <i>Sceletium</i>-type alkaloids, known for their anxiolytic and antidepressant activities, have been recently found to be biosynthesized in <i>Narcissus</i> cv. Hawera, which is largely used as an ornamental plant. An alkaloid fraction enriched with <i>Sceletium</i>-type alkaloids from the plant has shown promising antidepressant and anxiolytic activities. In the present study, qualitative and quantitative analyses of the alkaloids in the plant organs were performed during one vegetation season by GC-MS. The alkaloid pattern and total alkaloid content was found to depend strongly on the stage of development and plant organ. The alkaloid content of bulbs was found to be highest during the dormancy period and lowest in sprouting bulbs. The leaves showed the highest alkaloid content during the intensive vegetative growth and lowest during flowering. In total, 13 alkaloids were detected in the methanol extracts of <i>Narcissus</i> cv. Hawera, six <i>Sceletium</i>-type and seven typical Amaryllidaceae alkaloids. Major alkaloids in the alkaloid pattern were lycorine, 6-<i>epi</i>-mesembrenol, mesembrenone, sanguinine, and galanthamine. The leaves of flowering plants were found to have the highest amount of 6-<i>epi</i>-mesembrenol. Mesembrenone was found to be dominant alkaloid in the leaves of sprouting bulbs and in the flowers. Considering the biomass of the plant, the dormant bulbs are the best source of alkaloid fractions enriched with 6-<i>epi</i>-mesembrenol. The flowers and the young leaves can be used for preparation of alkaloid fractions enriched with mesembrenone. The results indicates that <i>Narcissus</i> cv. Hawera is an emerging source of valuable bioactive compounds and its utilization can be extended as a medicinal plant.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":"73-79"},"PeriodicalIF":2.0,"publicationDate":"2024-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140186135","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Pyrane-based cembranoid and 2-dehydro-4-peroxy-sarcophine: two new diterpenes from <i>Sarcophyton glaucum</i>.","authors":"Mohamed Shaaban, Mohamed A Ghani","doi":"10.1515/znc-2024-0004","DOIUrl":"10.1515/znc-2024-0004","url":null,"abstract":"<p><p>Soft corals, particularly <i>Sarcophyton</i> sp. are rich in metabolites with variety of biological activities. In this study, a pyran-based 9-<i>exo</i>-methylene-10-hydroxy-sarcotrocheliol (<b>1</b>) and 2-dehydro-4-peroxy-sarcophine (<b>2</b>), two new cembranoide diterpenes, were isolated together with 9-hydroxy-10,11-dehydro-sarcotrocheliol, sarcotrocheliol, sarcotrocheliol acetate, sarcophine, (+)-7<i>α</i>,8<i>β</i>-dihydroxydeepoxysarcophine, (±)-sarcophytonine B, and peridinin from the organic extract of <i>Sarcophyton glaucum</i> collected at the coasts of Hurghada, Egypt. The structures of the new diterpenes <b>1-2</b> were identified based on cumulative analyses of HRESIMS and NMR (1D/2D NMR) spectra. The relative configurations of both compounds were verified by NOESY spectra and comparison with our recently reported analogues. The compounds showed no antimicrobial activity against a set of diverse tested microorganisms.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":"81-87"},"PeriodicalIF":2.0,"publicationDate":"2024-03-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140177396","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Chitosan in cancer therapy: a dual role as a therapeutic agent and drug delivery system.","authors":"Harika Atmaca, Ferdi Oguz, Suleyman Ilhan","doi":"10.1515/znc-2023-0148","DOIUrl":"10.1515/znc-2023-0148","url":null,"abstract":"<p><p>Although chemotherapy is still the most preferred treatment for cancer, most chemotherapeutic agents target both cancer cells and healthy cells and cause serious side effects due to high toxicity. Improved drug delivery systems (DDSs), which enhance the efficacy of current chemotherapeutic drugs while reducing their toxicity, offer potential solutions to these challenges. Chitosan (CS) and its derivatives are biopolymers with biodegradable, biocompatible, and low-toxicity properties, and their structure allows for convenient chemical and mechanical modifications. In its role as a therapeutic agent, CS can impede the proliferation of tumor cells through the inhibition of angiogenesis and metastasis, as well as by triggering apoptosis. CS and its derivatives are also frequently preferred as DDSs due to their properties such as high drug-carrying capacity, polycationic structure, long-term circulation, and direct targeting of cancer cells. Various therapeutic agents linked to CS and its derivatives demonstrate potent anticancer effects with advantages such as reduced side effects compared to the original drugs, owing to factors like targeted distribution within cancer tissues and sustained release. This review emphasizes the utilization of CS and its derivatives, both as therapeutic agents and as carriers for established chemotherapeutic drugs.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":"95-105"},"PeriodicalIF":1.8,"publicationDate":"2024-03-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140121199","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Isolation, structural elucidation, and biological activity of a novel isocoumarin from the dark septate endophytic fungus <i>Phialocephala fortinii</i>.","authors":"Kei Bando, Ryoga Kushibe, Naoki Kitaoka, Yutaka Tamai, Kazuhiko Narisawa, Hideyuki Matsuura","doi":"10.1515/znc-2023-0139","DOIUrl":"10.1515/znc-2023-0139","url":null,"abstract":"<p><p>A novel isocoumarin was isolated from the mycelia of the dark septate endophytic fungus <i>Phialocephala fortinii</i>. The chemical structure was determined to be 8-hydroxy-6-methoxy-3,7-dimethyl-1<i>H</i>-2-benzopyran-1-one based on mass spectrometry, <sup>1</sup>H-nuclear magnetic resonance (NMR), and <sup>13</sup>C-NMR spectroscopic analyses, including 2D-NMR experiments. The isolated compound inhibited root growth of <i>Arabidopsis thaliana</i>, suggesting its potential as a plant growth regulator.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":"89-92"},"PeriodicalIF":2.0,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139991640","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Getachew Tegegn, Yadessa Melaku, Muhdin Aliye, Abiy Abebe, Negera Abdissa, Asfaw Meresa, Sileshi Degu, Mo Hunsen, Ahmed A Hussein, Milkyas Endale
{"title":"<i>In vitro</i> antimicrobial and antioxidant activities, essential oil composition, and <i>in silico</i> molecular modeling analysis of secondary metabolites from roots of <i>Verbascum sinaiticum</i>.","authors":"Getachew Tegegn, Yadessa Melaku, Muhdin Aliye, Abiy Abebe, Negera Abdissa, Asfaw Meresa, Sileshi Degu, Mo Hunsen, Ahmed A Hussein, Milkyas Endale","doi":"10.1515/znc-2023-0157","DOIUrl":"10.1515/znc-2023-0157","url":null,"abstract":"<p><p><i>Verbascum sinaiticum</i> is locally used to treat wound, stomachache, viral infection, cancer, sunstroke fever, abdominal colic, diarrhea, hemorrhage, anthrax, and hepatitis. The objective of this study was to identify the compounds and to evaluate the antimicrobial and antioxidant activity of the extracts and isolated compounds from <i>V. sinaiticum</i>. The <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, and DEPT-135 were used to elucidate the structures of isolated compounds. Essential oils were extracted by hydrodistillation method and their chemical analyses were performed by GC-MS. The broth microdilution method was used to evaluate the antimicrobial activity. The radical scavenging activity of the extracts and isolated compounds were evaluated using DPPH method. Silica gel column chromatographic separation of root extracts afforded seven known compounds: 3'-(4''-methoxy phenyl)-3'-oxo-propionyl hexadecanoate (<b>1</b>), harpagoside (<b>2</b>), pulverulentoside I (<b>3</b>), scrophuloside B4 (<b>4</b>), scropolioside A (<b>5</b>), scropolioside-D2 (<b>6</b>), and harpagide 6-<i>O</i>-β-glucoside (<b>7</b>), which are all reported from this species for the first time. The EO extracts from leaves and roots were the most susceptible to <i>Streptococcus agalactiae</i>, with a 2 mg/mL MIC. The EO from roots was effective against <i>Candida albicans</i> and <i>Trichophyton mentagrophytes</i>, with a MIC of 8 mg/mL. The MeOH and CH<sub>2</sub>Cl<sub>2</sub>/CH<sub>3</sub>OH (1:1) root extracts showed the maximum activity against <i>S. epidermidis</i> with MIC values of 0.25 mg/mL. The strongest antibacterial effects were demonstrated against <i>Staphylococcus epidermidis</i>, which exhibited a 0.0625 mg/mL MIC for compound <b>1</b>. The strongest radical scavenging activity was exhibited by the methanol extract (IC<sub>50</sub> = 3.4 μg/mL), and compounds <b>4</b>, <b>6</b>, <b>5</b>, <b>3</b>, <b>7</b>, and <b>2</b> with IC<sub>50</sub> values of 3.2, 3.38, 3.6, 3.8, 4.2, and 4.7 μg/mL, respectively, in comparison with ascorbic acid (IC<sub>50</sub> = 1.3 μg/mL). The results of the molecular docking analysis of compounds revealed minimal binding energies range from -38.5 to -43.1 kJ/mol, -33.1 to -42.7 kJ/mol, -34.7 to -39.3.7 kJ/mol, -25.5 to -37.6 kJ/mol against human myeloperoxidase (PDB ID: 1DNU), murA enzyme (PDB ID: 1UAE), human topoisomerase II<i>β</i> (PDB ID: 4fm9), <i>S. epidermidis</i> FtsZ (PDB number: 4M8I) proteins, respectively. The docking results and the <i>in vitro</i> antibacterial activity are in good agreement. These findings show that the isolated compounds <b>2</b>-<b>7</b> can act as potential antioxidants and strong antibacterials against <i>Staphylococcus aureus</i> and <i>S. epidermidis</i>. As a result, <i>V. sinaiticum</i> root extracts have the potential to be effective in treating diseases caused by bacteria and free radicals, as long as further investigation has been suggested for the ultimate decision of this plan","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":"25-39"},"PeriodicalIF":2.0,"publicationDate":"2024-02-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139984306","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Mustafa M El-Abadelah, Ahmad H Abdullah, Jalal A Zahra, Salim S Sabri, Sanaa K Bardaweel, Mutasem O Taha
{"title":"Synthesis and antitumor activity of model cyclopentene-[<i>g</i>]annelated isoindigos.","authors":"Mustafa M El-Abadelah, Ahmad H Abdullah, Jalal A Zahra, Salim S Sabri, Sanaa K Bardaweel, Mutasem O Taha","doi":"10.1515/znc-2023-0119","DOIUrl":"10.1515/znc-2023-0119","url":null,"abstract":"<p><p>A set of cyclopenten-[<i>g</i>]annelated isoindigos (<b>5a-g</b>) has been prepared and tested for their <i>in vitro</i> antiproliferative activities against MCF-7 and HL60 cells. Among, the <i>N</i>-1-methyl-5'-nitro derivative (<b>5g</b>) displayed the highest activity against HL60 cells (IC<sub>50</sub> = 67 nM) and acted as the most potent Flt3 inhibitor. Compounds <b>5d-g</b> exhibited moderate activity against MCF-7 (IC<sub>50</sub> = 50-80 μM).</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":"41-46"},"PeriodicalIF":2.0,"publicationDate":"2024-02-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139984307","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}