scholarly journals Antiamylase, Antilipase, Antimicrobial, and Cytotoxic Activity of Nonea obtusifolia (Willd.) DC. from Palestine

2020 ◽  
Vol 2020 ◽  
pp. 1-8
Author(s):  
Nidal Jaradat ◽  
Murad N. Abualhasan ◽  
Mohammad Qadi ◽  
Linda Issa ◽  
Ahmad Mousa ◽  
...  
Keyword(s):  
Methylene Chloride ◽  
Research Work ◽  
Cancer Cell Line ◽  
Culture Collection ◽  
Bioactive Molecules ◽  
Diffusion Method ◽  
Cytotoxic Activities ◽  
Ic50 Values ◽  
Antibacterial And Antifungal ◽  
First Time

Background. Medicinal plants are widely used in many cultures, traditions, and civilizations worldwide. Plants with high contents of the valuable biological compounds can efficiently cure many diseases. This study is aimed at assessing, for the first time, the anti-α-amylase, antilipase, antimicrobial, and cytotoxic activities of Nonea obtusifolia (Willd.) DC. of five extracts from Palestine. Methods. The antimicrobial activity was estimated using well diffusion method for N. obtusifolia plant of five extracts against eight ATCC (American Type Culture Collection) and clinical isolates. The cytotoxic effects for these extracts were evaluated against HeLa (cervical) carcinoma cells using MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay. Moreover, the lipase and α-amylase inhibitory properties were determined using standard biomedical assays. Results. The acetone extract of N. obtusifolia plant showed a more potent α-amylase inhibitory compared with acarbose with IC50 values of 25.7 ± 0.08 and 28.18 ± 1.22   μ g / ml , respectively. Additionally, the acetone and methanol extracts revealed moderate antilipase activity compared to orlistat with IC50 values of 30.19 ± 0.11 , 33.11 ± 0.13 , and 12.3 ± 0.35   μ g / ml , respectively. The methylene chloride extract was found to inhibit the growth of all the tested bacterial and fungal strains and also found to have potential cytotoxic effect against HeLa cancer cell line. Conclusion. This research work reports for the first time the biological activity of N. obtusifolia from Palestine, and the results were promising indicating that N. obtusifolia extracts contain valuable bioactive molecules that have a potential anti-α-amylase, antilipase, antibacterial, and antifungal cytotoxic potentials. Therefore, N. obtusifolia could have a medical significance in the future.

scholarly journals Antibacterial, antioxidant and cytotoxic activities of different fractions of acetone extract from flowers of Dipterocarpus intricatus Dyer (Dipterocarpaceae)

2021 ◽  
Vol 8 (2) ◽  
pp. 273-277
Author(s):  
Hong Thia Le ◽  
Thao Nguyen Luu ◽  
Huynh Mai Thu Nguyen ◽  
Dang HoaiTrang Nguyen ◽  
Pham Tan Quoc Le ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Salmonella Enteritidis ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Acetone Extract ◽  
Cytotoxic Agents ◽  
Diffusion Method ◽  
Cytotoxic Activities ◽  
Ic50 Values ◽  
First Time

This study has shown for the first time the antimicrobial, antioxidant and cytotoxicity of 3 fractions of acetone extract, including hexane, chloroform and ethyl acetate from flowers of Dipterocarpus intricatus. Antibacterial test using disc diffusion method showed that the chloroform and ethyl acetate fractions inhibited the growth of all the tested bacteria, including Escherichia coli, Pseudomonas aeruginosa, Salmonella enteritidis, Salmonella typhimurium, Bacillus cereus and Staphylococcus aureus while the hexane fraction showed the antibacterial activity against B. cereus and S. enteritidis. Antioxidant activity and cancer cell resistance of those extracts were conducted using DPPH and MTT methods respectively. As a result, the DPPH radical scavenging activity of the hexane, chloroform and ethyl acetate fractions were determined with the IC50 values of 0.508, 0.22 and 0.075 mg/mL respectively while the cytotoxicity to HepG2 cell line of those fractions was 163.3 ppm, 106.7 ppm and 459.3 ppm. These results suggested the potential application of these fractions isolated from D. intricatus flowers as the natural antimicrobial, antioxidant and cytotoxic agents for medicine.

scholarly journals New Acetophenones and Chromenes from the Leaves of Melicope barbigera A. Gray

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 688
Author(s):  
Kim-Thao Le ◽  
Jan J. Bandolik ◽  
Matthias U. Kassack ◽  
Kenneth R. Wood ◽  
Claudia Paetzold ◽  
...  
Keyword(s):  
Ovarian Cancer Cell Line ◽  
Hawaiian Island ◽  
Cancer Cell Line ◽  
2D Nmr ◽  
Cytotoxic Activities ◽  
2D Nmr Spectroscopy ◽  
Ic50 Values ◽  
New Compounds ◽  
First Time ◽  
Modified Mosher’S Method

The dichloromethane extract from leaves of Melicope barbigera (Rutaceae), endemic to the Hawaiian island of Kaua’i, yielded four new and three previously known acetophenones and 2H-chromenes, all found for the first time in M. barbigera. The structures of the new compounds obtained from the dichloromethane extract after purification by chromatographic methods were unambiguously elucidated by spectroscopic analyses including 1D/2D NMR spectroscopy and HRESIMS. The absolute configuration was determined by modified Mosher’s method. Compounds 2, 4 and the mixture of 6 and 7 exhibited moderate cytotoxic activities against the human ovarian cancer cell line A2780 with IC50 values of 30.0 and 75.7 µM for 2 and 4, respectively, in a nuclear shrinkage cytotoxicity assay.

In Vitro Human Dihydroorotate Dehydrogenase Inhibitory, Anti-inflammatory and Cytotoxic Activities of Alkaloids from the Seeds of Nigella glandulifera

Planta Medica ◽  
2018 ◽  
Vol 84 (14) ◽  
pp. 1013-1021 ◽  
Author(s):  
Jun-Bo Gao ◽  
Xing-Jie Zhang ◽  
Rui-Han Zhang ◽  
Li-Li Zhu ◽  
De-Bing Pu ◽  
...  
Keyword(s):  
Folk Medicine ◽  
Positive Control ◽  
Cytotoxic Activities ◽  
Dihydroorotate Dehydrogenase ◽  
X Ray Diffraction ◽  
Ic50 Values ◽  
Pharmacologically Active ◽  
Pharmacologically Active Compounds ◽  
First Time

AbstractFour new dolabellane-type diterpene alkaloids, glandulamines A – D (1 – 4), together with twelve known compounds (5 – 16), were isolated from the seeds of Nigella glandulifera using repeated column chromatography and semipreparative HPLC. The structures of 1 – 16 were elucidated based on NMR data analysis, HRMS experiments and other spectroscopic interpretations. The absolute configuration of 5 was determined by single-crystal X-ray diffraction data for the first time. Compounds 10 and 12 showed human dihydroorotate dehydrogenase inhibitory activity with IC50 values of 61.1 ± 5.3 and 45.9 ± 3.0 µM, respectively. Molecular docking of the active compound 12 and positive control teriflunomide on the inhibitor-binding site of human dihydroorotate dehydrogenase was subsequently performed to visualize the interaction pattern. In addition, compounds 8 and 10 exhibited inhibitory effects against lipopolysaccharide-induced nitric oxide production with inhibition rates of 61 and 41%, respectively, at the concentration of 10 µM. Compounds 9 and 12 showed cytotoxic activities with cell viability varying from 29 ~ 57% at 100 µM against T98G, U87, U251, and GL261 glioma cancer cell lines. These data provide new insights on the pharmacologically active compounds of this plant widely used in folk medicine.

scholarly journals Synthesis of Trichodermin Derivatives and Their Antimicrobial and Cytotoxic Activities

Molecules ◽  
2019 ◽  
Vol 24 (20) ◽  
pp. 3811
Author(s):  
Javier E. Barúa ◽  
Mercedes de la Cruz ◽  
Nuria de Pedro ◽  
Bastien Cautain ◽  
Rosa Hermosa ◽  
...  
Keyword(s):  
Human Hepatocytes ◽  
Bioactive Molecules ◽  
Cytotoxic Activities ◽  
Terpene Cyclase ◽  
Trichodiene Synthase ◽  
Specific Step ◽  
Ic50 Values ◽  
Selective Antimicrobial Activity ◽  
Tumorigenic Cell Line ◽  
Mcf 7

Trichothecene mycotoxins are recognized as highly bioactive compounds that can be used in the design of new useful bioactive molecules. In Trichoderma brevicompactum, the first specific step in trichothecene biosynthesis is carried out by a terpene cyclase, trichodiene synthase, that catalyzes the conversion of farnesyl diphosphate to trichodiene and is encoded by the tri5 gene. Overexpression of tri5 resulted in increased levels of trichodermin, a trichothecene-type toxin, which is a valuable tool in preparing new molecules with a trichothecene skeleton. In this work, we developed the hemisynthesis of trichodermin and trichodermol derivatives in order to evaluate their antimicrobial and cytotoxic activities and to study the chemo-modulation of their bioactivity. Some derivatives with a short chain at the C-4 position displayed selective antimicrobial activity against Candida albicans and they showed MIC values similar to those displayed by trichodermin. It is important to highlight the cytotoxic selectivity observed for compounds 9, 13, and 15, which presented average IC50 values of 2 μg/mL and were cytotoxic against tumorigenic cell line MCF-7 (breast carcinoma) and not against Fa2N4 (non-tumoral immortalized human hepatocytes).

scholarly journals Nimesulide Based Novel Glycolamide Esters: Their Design, Synthesis, and Pharmacological Evaluation

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Kavitha Kankanala ◽  
Vangala Ranga Reddy ◽  
Yumnam Priyadarshini Devi ◽  
Lakshmi Narasu Mangamoori ◽  
Khagga Mukkanti ◽  
...  
Keyword(s):  
Cancer Cell Line ◽  
Human Colon ◽  
Colon Cancer Cell Line ◽  
Cytotoxic Activities ◽  
Step Method ◽  
Human Colon Cancer ◽  
Cytotoxic Effects ◽  
Design Synthesis ◽  
First Time

The nimesulide based novel glycolamide esters were designed and synthesized for the first timeviaa three-step method starting from nimesulide. Structures of the synthesized compounds were confirmed by spectroscopic analysis. All the synthesized compounds were examined for their cytotoxic effectsin vitro,some of which showed significant cytotoxic activities against HCT-15 human colon cancer cell line.

scholarly journals Microbial Transformation of neo-Clerodane Diterpenoid, Scutebarbatine F, by Streptomyces sp. CPCC 205437

2021 ◽  
Vol 12 ◽  
Author(s):  
Dewu Zhang ◽  
Xiaoyu Tao ◽  
Guowei Gu ◽  
Yujia Wang ◽  
Wenxia Zhao ◽  
...  
Keyword(s):  
Influenza A ◽  
Microbial Transformation ◽  
Cancer Cell Line ◽  
Antibacterial Activities ◽  
Positive Control ◽  
Cytotoxic Activities ◽  
Ionization Mass ◽  
Nmr Data ◽  
First Time ◽  
New Metabolites

Biotransformation of the neo-clerodane diterpene, scutebarbatine F (1), by Streptomyces sp. CPCC 205437 was investigated for the first time, which led to the isolation of nine new metabolites, scutebarbatine F1–F9 (2–10). Their structures were determined by extensive high-resolution electrospray ionization mass spectrometry (HRESIMS) and NMR data analyses. The reactions that occurred included hydroxylation, acetylation, and deacetylation. Compounds 2–4 and 8–10 possess 18-OAc fragment, which were the first examples of 13-spiro neo-clerodanes with 18-OAc group. Compounds 7–10 were the first report of 13-spiro neo-clerodanes with 2-OH. Compounds 1–10 were biologically evaluated for the cytotoxic, antiviral, and antibacterial activities. Compounds 5, 7, and 9 exhibited cytotoxic activities against H460 cancer cell line with inhibitory ratios of 46.0, 42.2, and 51.1%, respectively, at 0.3 μM. Compound 5 displayed a significant anti-influenza A virus activity with inhibitory ratio of 54.8% at 20 μM, close to the positive control, ribavirin.

scholarly journals Anthraquinone Derivatives from a Marine-Derived Fungus Sporendonema casei HDN16-802

Marine Drugs ◽  
2019 ◽  
Vol 17 (6) ◽  
pp. 334 ◽  
Author(s):  
Xueping Ge ◽  
Chunxiao Sun ◽  
Yanyan Feng ◽  
Lingzhi Wang ◽  
Jixing Peng ◽  
...  
Keyword(s):  
Chlorine Atom ◽  
Anticoagulant Activity ◽  
Antitubercular Activity ◽  
Antibacterial Activities ◽  
Cytotoxic Activities ◽  
Spectroscopic Techniques ◽  
Addition Compound ◽  
Anthraquinone Derivatives ◽  
Ic50 Values ◽  
First Time

Five new anthraquinone derivatives, auxarthrols D–H (1–5), along with two known analogues (6–7), were obtained from the culture of the marine-derived fungus Sporendonema casei. Their structures, including absolute configurations, were established on the basis of NMR, HRESIMS, and circular dichroism (CD) spectroscopic techniques. Among them, compound 4 represents the second isolated anthraquinone derivative with a chlorine atom, which, with compound 6, are the first reported anthraquinone derivatives with anticoagulant activity. Compounds 1 and 3 showed cytotoxic activities with IC50 values from 4.5 μM to 22.9 μM, while compounds 1, 3–4, and 6–7 showed promising antibacterial activities with MIC values from 12.5 μM to 200 μM. In addition, compound 7 was discovered to display potential antitubercular activity for the first time.

Preliminary Evaluation of Antimicrobial and Cytotoxic Activities of Extracts from Actinidia macrosperma

2012 ◽  
Vol 455-456 ◽  
pp. 1200-1203 ◽  
Author(s):  
Yin Lu ◽  
Yun Peng Zhao ◽  
Cheng Xin Fu
Keyword(s):  
Inhibitory Concentration ◽  
Chloroform Extract ◽  
Diffusion Method ◽  
Cytotoxic Activities ◽  
Preliminary Evaluation ◽  
Minimum Fungicidal Concentration ◽  
Antibacterial And Antifungal Activities ◽  
Brine Shrimp Lethality Assay ◽  
Antibacterial And Antifungal

The petroleum ether, chloroform, ethyl acetate, n-hexane and aqueous successive extracts from the stems of Actinidia macrosperma C. F. Liang have been screened for antibacterial and antifungal activities in vitro using the disc diffusion method, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC)/minimum fungicidal concentration (MFC). General toxicity of these extracts has also been assessed by brine shrimp lethality assay. The chloroform extract exhibited the most significant antimicrobial (MIC in the range of 60–500μg/ml, MBC in the range of 150–1000μg/ml, MFC in the range of 170–600μg/ml) and cytotoxic activities (LC50=16.82μg/ml at 24 hours).

scholarly journals In vitro evaluation of anticaries, antimycobacterial, antileishmanial and cytotoxic activities of essential oils from Eremanthus erythropappus and of α-bisabolol, their major sesquiterpene

2020 ◽  
pp. 236-243
Author(s):  
Cassia Cristina Fernandes ◽  
Priscila Mileide de Andrade ◽  
Tainá Caroline Lucena dos Santos ◽  
Mariana Brentini Santiago ◽  
Antônio Eduardo Miller Crotti ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Essential Oils ◽  
Peritoneal Macrophages ◽  
Culture Collection ◽  
Cytotoxic Activities ◽  
Therapeutic Effects ◽  
Herbaceous Plant ◽  
Microdilution Method ◽  
Ic50 Values

Interest in researches into medicinal plants and therapeutic effects of essential oils (EOs) on humans has increased over the last few years. Eremanthus erythropappus, known as candeia, is a Brazilian aromatic herbaceous plant whose α-bisabolol-rich oil has been used in several cosmetic preparations. This paper reports in vitro anticaries, antimycobacterial, antileishmanial and cytotoxic activities of EOs from E. erythropappus leaves (EL-EO) and stalks (ES-EO), besides α-bisabolol, their main sesquiterpene. EL-EO and ES-EO were extracted by hydrodistillation and analyzed by GC-FID and GC-MS. α-Bisabolol, cis-α-bisabolene and β-bisabolene were identified as their major constituents. Antibacterial activity of EOs was evaluated against eight standard strains of pathogens from the American Type Culture Collection (ATCC) by determining minimum inhibitory concentrations (MICs) with the use of the microdilution method. Antibacterial activity was evaluated against Streptococcus mutans, S. mitis, S. sanguinis, S. sobrinus, S. salivarius, Mycobacterium tuberculosis, M. avium and M. kansasii. EL-EO, ES-EO and α-bisabolol exhibited high leishmanicidal activity against promastigote forms of Leishmania amazonensis; IC50 values were 9.22 µg/mL, 6.00 µg/mL and 3.12 µg/mL, respectively. The 50% cytotoxic concentrations (CC50) of EL-EO, ES-EO and α-bisabolol against mouse peritoneal macrophages were 24.65 µg/mL, 8.87 µg/mL and 1021.00 µg/mL, respectively. These results suggest that EOs from E. erythropappus seem to be very promising for the development of new bactericidal and leishmanicidal agents.

scholarly journals Benzylated Dihydroflavones and Isoquinoline-Derived Alkaloids from the Bark of Diclinanona calycina (Annonaceae) and Their Cytotoxicities

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3714
Author(s):  
Emmanoel V. Costa ◽  
Liviane do N. Soares ◽  
Jamal da Silva Chaar ◽  
Valdenizia R. Silva ◽  
Luciano de S. Santos ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
2D Nmr ◽  
Cytotoxic Activities ◽  
2D Nmr Spectroscopy ◽  
Cancerous Cell ◽  
Ic50 Value ◽  
Ic50 Values ◽  
Low Cytotoxicity ◽  
First Time

Diclinanona calycina R. E. Fries popularly known as “envira”, is a species of the Annonaceae family endemic to Brazil. In our ongoing search for bioactive compounds from Annonaceae Amazon plants, the bark of D. calycina was investigated by classical chromatography techniques that yielded thirteen compounds (alkaloids and flavonoids) described for the first time in D. calycina as well as in the genus Diclinanona. The structure of these isolated compounds were established by extensive analysis using 1D/2D-NMR spectroscopy in combination with MS. The isolated alkaloids were identified as belonging to the subclasses: simple isoquinoline, thalifoline (1); aporphine, anonaine (2); oxoaporphine, liriodenine (3); benzyltetrahydroisoquinolines, (S)-(+)-reticuline (4); dehydro-oxonorreticuline (3,4-dihydro-7-hydroxy-6-methoxy-1-isoquinolinyl)(3-hydroxy-4-methoxyphenyl)-methanone) (5); (+)-1S,2R-reticuline Nβ-oxide (6); and (+)-1S,2S-reticuline Nα-oxide (7); tetrahydroprotoberberine, coreximine (8); and pavine, bisnorargemonine (9). While the flavonoids belong to the benzylated dihydroflavones, isochamanetin (10), dichamanetin (11), and a mixture of uvarinol (12) and isouvarinol (13). Compound 5 is described for the first time in the literature as a natural product. The cytotoxic activity of the main isolated compounds was evaluated against cancer and non-cancerous cell lines. Among the tested compounds, the most promising results were found for the benzylated dihydroflavones dichamanetin (10), and the mixture of uvarinol (12) and isouvarinol (13), which presented moderate cytotoxic activity against the tested cancer cell lines (<20.0 µg·mL−1) and low cytotoxicity against the non-cancerous cell line MRC-5 (>25.0 µg·mL−1). Dichamanetin (11) showed cytotoxic activity against HL-60 and HCT116 with IC50 values of 15.78 µg·mL−1 (33.70 µmol·L−1) and 18.99 µg·mL−1 (40.56 µmol·L−1), respectively while the mixture of uvarinol (12) and isouvarinol (13) demonstrated cytotoxic activity against HL-60, with an IC50 value of 9.74 µg·mL−1, and HCT116, with an IC50 value of 17.31 µg·mL−1. These cytotoxic activities can be attributed to the presence of one or more hydroxybenzyl groups present in these molecules as well as the position in which these groups are linked. The cytotoxic activities of reticuline, anonaine and liriodenine have been previously established, with liriodenine being the most potent compound.

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