Phosphorus–nitrogen compounds. Part 42. The comparative syntheses of 2-cis-4-ansa(N/O) and spiro(N/O) cyclotetraphosphazene derivatives: spectroscopic and crystallographic characterization, antituberculosis and cytotoxic activity studies

2019 ◽  
Vol 43 (18) ◽  
pp. 6856-6873 ◽  
Author(s):  
Arzu Binici ◽  
Aytuğ Okumuş ◽  
Gamze Elmas ◽  
Zeynel Kılıç ◽  
Nagehan Ramazanoğlu ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Structural Properties ◽  
Biological Activities ◽  
Nitrogen Compounds

Syntheses, structural properties and biological activities of ferrocenyl ansa- and spiro-cyclotetraphosphazenes were investigated.

Structural and Bioactive Studies of Halogenated Constituents from Sponges

2020 ◽  
Vol 27 (14) ◽  
pp. 2335-2360 ◽  
Author(s):  
Chao Li ◽  
Dayong Shi
Keyword(s):  
Microbial Communities ◽  
Organic Compounds ◽  
Biological Activities ◽  
Marine Sponges ◽  
Nitrogen Compounds ◽  
Halogenated Organic Compounds ◽  
Bioactive Natural Products ◽  
The Past ◽  
Tyrosine Derivatives ◽  
Polyunsaturated Lipids

: Marine organisms are abundant sources of bioactive natural products. Among metabolites produced by sponges and their associated microbial communities, halogenated natural compounds accounted for an important part due to their potent biological activities. The present review updates and compiles a total of 258 halogenated organic compounds isolated in the past three decades, especially brominated derivatives derived from 31 genera of marine sponges. These compounds can be classified as the following classes: brominated polyunsaturated lipids, nitrogen compounds, brominated tyrosine derivatives and other halogenated compounds. These substances were listed together with their source organisms, structures and bioactivities. For this purpose, 84 references were consulted.

scholarly journals Synergistic Action of Stilbenes in Muscadine Grape Berry Extract Shows Better Cytotoxic Potential Against Cancer Cells Than Resveratrol Alone

Biomedicines ◽  
2019 ◽  
Vol 7 (4) ◽  
pp. 96 ◽  
Author(s):  
Subramani Paranthaman Balasubramani ◽  
Mohammad Atikur Rahman ◽  
Sheikh Mehboob Basha
Keyword(s):  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Biological Activities ◽  
Grape Berry ◽  
Similar Response ◽  
Synergistic Activity ◽  
Anti Cancer ◽  
Muscadine Grape ◽  
Berry Extracts ◽  
Cancer Activity

Muscadine grape is rich in stilbenes, which include resveratrol, piceid, viniferin, pterostilbene, etc. Resveratrol has been extensively studied for its biological activities; however, the synergistic effect of stilbene compounds in berry extracts is poorly understood. The aim of this study was to evaluate the anti-cancer activity of stilbene-rich muscadine berry extract and pure resveratrol. Stilbenes were extracted from ripened berries of muscadine grape cultivars, Pineapple, and Southern Home. HPLC analysis was performed to determine quantity of stilbenes. The extracts were tested for their cytotoxic activity against A549 (lung carcinoma cells), triple negative breast cancer (HCC-1806) and HepG2 (human liver cancer) cells. The stilbene-rich extracts of the muscadine berry extracts showed cytotoxic activity against all of the cells tested. The extracts at 1 μg/mL induced death in 50–80% of cells by 72 h of treatment. About 50 μg/mL of resveratrol was required to induce a similar response in the cells. Further, modulation of genes involved in tumor progression and suppression was significantly (p < 0.0005) higher with the HepG2 cells treated with stilbene-rich berry extracts than the pure resveratrol. This shows that the synergistic activity of stilbenes present in muscadine grape berries have more potent anti-cancer activity than the resveratrol alone.

scholarly journals Phytochemical Screening and Biocidal Studies Of Stem Bark Chrysophyllum Albidum (Linn) And Straw Aristolochia Ringens from Nigeria.

2017 ◽  
Vol 4 (1) ◽  
Author(s):  
Moses Owolabi
Keyword(s):  
Medicinal Plants ◽  
Cytotoxic Activity ◽  
Biological Activities ◽  
Stem Bark ◽  
Breast Tumour ◽  
Tumour Cells ◽  
Bacterial Activity ◽  
Liver Tumour ◽  
Phytochemical Screening ◽  
Health Maintenance

Introduction: Medicinal plants play a significant role in the health maintenance in underdeveloped countries, herbs and spices continue serve as a new sources for herbal medicines. Aim: The objective was to investigate phytochemical screening and biocidal activity on stem bark Chrysophyllum albidum (Linn) and straw Aristolochia ringens using chloroform. Methods: Chloroform extracts of C. albidum and A. ringens were obtained and screened for phytochemical constituents. The colour intensity or the precipitate formation was used as analytical responses to these tests. The Antimicrobial activities crude extracts were evaluated against some microorganisms with broth microdilution test. The extracts were screened for in-vitro cytotoxic activity against breast tumour and liver tumour cells. Results: The results of the phytochemical screening revealed the presence of alkaloids, saponins, steroids, anthraquinone and glycosides. C. albidum and A. ringens chloroform extracts revealed high quantities of alkaloid and flavonoid respectively. While cardiac glycoside and anthraquinone were found with low quantity in C. albidum and A. ringens extracts respectively. C. albidum showed promising bacterial activity against Escherichia coli and cytotoxic activity to liver tumour cells. While A. ringens, showed excellent bacterial activity against Bacillus cereus and good fungal activity against Candida albicans. A. ringens also showed cytotoxic to liver tumour and breast tumour cells. The observed antimicrobial and cytotoxic effects may be due to the antagonist or synergistic effect of the secondary metabolites identified in the extracts. Conclusion: Medicinal plants studied showed good potential biological activities that support the idea that traditional medicines remain useful healthcare in developing countries

scholarly journals Metabolic Profile and Evaluation of Biological Activities of Extracts from the Stems of Cissus trifoliata

2020 ◽  
Vol 21 (3) ◽  
pp. 930
Author(s):  
Luis Fernando Méndez-López ◽  
Elvira Garza-González ◽  
María Yolanda Ríos ◽  
M. Ángeles Ramírez-Cisneros ◽  
Laura Alvarez ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Antibacterial Activity ◽  
Cytotoxic Activity ◽  
Metabolic Profile ◽  
Biological Activities ◽  
Cytotoxic Activities ◽  
Aqueous Extracts ◽  
Antitumor Effects ◽  
Anticancer Compounds ◽  
High Cytotoxic Activity

Cissus trifoliata (L.) L belongs to the Vitaceae family and is an important medicinal plant used in Mexico for the management of infectious diseases and tumors. The present study aimed to evaluate the metabolic profile of the stems of C. trifoliata and to correlate the results with their antibacterial and cytotoxic activities. The hexane extract was analyzed using gas chromatography coupled with mass spectrometry (GC-MS) and the CHCl3-MeOH and aqueous extracts by ultraperformance liquid chromatography quadrupole time of fly mass spectrometry (UPLC-QTOF-MS). The antibacterial activity was determined by broth microdilution and the cytotoxicity was evaluated using MTS cell proliferation assay. Forty-six metabolites were putatively identified from the three extracts. Overall, terpenes, flavonoids and stilbenes characterize the metabolic profile. No antibacterial activity was found in any extract against the fifteen bacteria strains tested (MIC >500 µg/mL). However, high cytotoxic activity (IC50 ≤ 30 µg/mL) was found in the hexane and aqueous extracts against hepatocarcinoma and breast cancer cells (Hep3B, HepG2 and MCF7). This is the first report of the bioactive compounds of C. trifoliata stems and their antibacterial and cytotoxic properties. The metabolic profile rich in anticancer compounds correlate with the cytotoxic activity of the extracts from the stems of C. trifoliata. This study shows the antitumor effects of this plant used in the traditional medicine and justifies further research of its anticancer activity.

scholarly journals PYRIMIDINES AS POTENT CYTOTOXIC AND ANTI-INFLAMMATORY AGENTS

2017 ◽  
Vol 10 (6) ◽  
pp. 237 ◽  
Author(s):  
Ishwar Bhat K ◽  
Abhishek Kumar
Keyword(s):  
Acetic Acid ◽  
Cytotoxic Activity ◽  
Glacial Acetic Acid ◽  
Antimalarial Activity ◽  
Biological Activities ◽  
Cytotoxic Agents ◽  
Pyrimidine Derivatives ◽  
Pharmacological Activities ◽  
Anti Inflammatory ◽  
Derivatives Of

Objective: Many derivatives of pyrimidine are known for the broad-spectrum biological activities such as antimicrobial, antitumor, antibacterial, antitubercular, anti-inflammatory, and cytotoxic activity. Chalcones with an enone group show potent pharmacological activities such as antiinflammatory, antibacterial, antifungal, and antimalarial activity. A series of pyrimidines from chalcones have been synthesized and screened for anti-inflammatory and cytotoxic activity studies.Methods: Chalcones [1-(4-nitrophenyl)-3-substituted-phenylprop-2-en-1-one] were synthesized from various substituted aldehydes with 4-nitroacetophenone and cyclized with urea and glacial acetic acid to give pyrimidine derivatives [4-(4-nitrophenyl)-6-substituted-phenylpyrimidin-2-ol].Results: Anti-inflammatory and cytotoxic activity studies revealed that some of the synthesized compounds have shown significant activity.Conclusion: The observed results proved that pyrimidines are found to be interesting lead molecules for the synthesis of anti-inflammatory and cytotoxic agents

scholarly journals Fused 1,5-Naphthyridines: Synthetic Tools and Applications

Molecules ◽  
2020 ◽  
Vol 25 (15) ◽  
pp. 3508
Author(s):  
Carme Masdeu ◽  
Maria Fuertes ◽  
Endika Martin-Encinas ◽  
Asier Selas ◽  
Gloria Rubiales ◽  
...  
Keyword(s):  
Organic Chemistry ◽  
Biological Activity ◽  
Metal Complexes ◽  
Biological Activities ◽  
Nitrogen Heterocycles ◽  
Diels Alder ◽  
Nitrogen Compounds ◽  
Wide Range ◽  
Oxygen Heterocycles ◽  
Optical Applications

Heterocyclic nitrogen compounds, including fused 1,5-naphthyridines, have versatile applications in the fields of synthetic organic chemistry and play an important role in the field of medicinal chemistry, as many of them have a wide range of biological activities. In this review, a wide range of synthetic protocols for the construction of this scaffold are presented. For example, Friedländer, Skraup, Semmlere-Wolff, and hetero-Diels-Alder, among others, are well known classical synthetic protocols used for the construction of the main 1,5-naphthyridine scaffold. These syntheses are classified according to the nature of the cycle fused to the 1,5-naphthyridine ring: carbocycles, nitrogen heterocycles, oxygen heterocycles, and sulphur heterocycles. In addition, taking into account the aforementioned versatility of these heterocycles, their reactivity is presented as well as their use as a ligand for metal complexes formation. Finally, those fused 1,5-naphthyridines that present biological activity and optical applications, among others, are indicated.

scholarly journals Biological Activities and Structural Properties of the Atypical Bacteriocins Mesenterocin 52B and Leucocin B-TA33a

2001 ◽  
Vol 67 (4) ◽  
pp. 1418-1422 ◽  
Author(s):  
C. Corbier ◽  
F. Krier ◽  
G. Mulliert ◽  
B. Vitoux ◽  
A.-M. Revol-Junelles
Keyword(s):  
Circular Dichroism ◽  
Structural Properties ◽  
Sequence Homology ◽  
Synthetic Peptides ◽  
Biological Activities ◽  
Modes Of Action ◽  
Amphiphilic Helix ◽  
High Sequence Homology ◽  
Circular Dichroïsm

ABSTRACT The antibacterial spectra and modes of action of synthetic peptides corresponding to mesenterocin 52B and leucocin B-TA33a greatly differ despite their high sequence homology. Circular dichroism experiments establish the capacity of each of these two peptides to partly fold into an amphiphilic helix that might be crucial for their adsorption at lipophilic-hydrophilic interfaces.

scholarly journals Actinidia macrospermaC. F. Liang (a Wild Kiwi): Preliminary Study of Its Antioxidant and Cytotoxic Activities

2012 ◽  
Vol 2012 ◽  
pp. 1-7
Author(s):  
Yin Lu ◽  
Xiangtao Du ◽  
Lidan Lai ◽  
Hao Jin
Keyword(s):  
Antioxidant Activity ◽  
Cytotoxic Activity ◽  
Biological Activities ◽  
Positive Control ◽  
Total Phenolic ◽  
Cytotoxic Activities ◽  
Dependent Manner ◽  
Etoac Extract ◽  
Total Antioxidant

The antioxidant potential ofActinidia macrospermaC. F. Liang (Actinidiaceae) was investigated in vitro for total phenolic content, along with total antioxidant activity (TAA), 1,1-diphenyl 2-picryl hydrazyl (DPPH), and lipid peroxidation (LP). The results indicated that different polarity extracts ofA. macrospermaexhibit different biological activities, which depends mainly on the presence of phenolic compounds. The antioxidant activity was in the following decreasing order: MeOH extract > EtOAc extract > aqueous extract > CHCl3extract > Hexane extract. Moreover, the cytotoxic activity of this plant by MTT dye assay using SMMC-7721 has been determined also. The hexane, EtOAc, and CHCl3extracts showed cytotoxicity in a dose-dependent manner. Methanol and aqueous extracts, however, showed weak activities in this test. And a very significant cytotoxic activity, not significantly different from the positive control of quercetin, was observed in CHCl3extract.

scholarly journals Study on biological activities of extracted fractions from Typhonium flagelliforme (Lodd.) Blume

2017 ◽  
Vol 33 (2S) ◽  
Author(s):  
Le Quy Thuong ◽  
Bach Tuyet Mai ◽  
Nguyen Minh Chau ◽  
Le Thi Phuong Hoa ◽  
Nguyen Quang Huy
Keyword(s):  
Ethyl Acetate ◽  
Cytotoxic Activity ◽  
Biological Activities ◽  
Ethyl Acetate Fraction ◽  
Positive Control ◽  
Chemical Compositions ◽  
Active Components ◽  
Stomach Pain ◽  
Ic50 Values

Typhonium flagelliforme is a medicinal plant that has variety of uses. In medicinal traditional T. flagelliforme is used to treatment cough, headache, stomach pain chronic, and tracheitis. Moreover, use fresh bulbs treatment furuncle, the bites of poisonous insects. The active components in T. flagelliforme are flavonoids. In this study, the T. flagelliforme extract was obtained by methanol  to determine the chemical composition. Then, The extracts of methanol are extracted with polarization increases gradually solvents such as haxane, dichloromethane and ethyl acetate. Determination of antioxidant activity, cytotoxic activity of extracted fractions. Results obtained showed that the chemical compositions by the qualitative reaction preliminary were identified from T. flagelliforme containing reducing sugars, amino acids, organic acids, flavonoids, alcaloids, sterols. The antioxidant capacity of the ethyl acetate fraction reached 94.76 μg/ml, 10 times higher than the positive control is Quercetin. Cytotoxic activity of the haxane and diclomethane extracted fractions from T. flagelliforme exhibited cytotoxic activity on all three experimental cancers cell lines: KB, HepG2, Lu after 72h of culture with IC50 values ​​range from 92.8 to 107.76 μg/ml. From dichlomethane extracted of T. flagelliforme was purified TF1 as Stigmast-4-en- 3-on.    

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