scholarly journals Immunomodulatory Effects of Lycium barbarum Polysaccharide Extract and Its Uptake Behaviors at the Cellular Level

Molecules ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 1351 ◽  
Author(s):  
Le Feng ◽  
Xiao Xiao ◽  
Jing Liu ◽  
Junyan Wang ◽  
Nan Zhang ◽  
...  
Keyword(s):  
Cell Lines ◽  
Biological Activities ◽  
Cell Monolayer ◽  
Intestinal Transport ◽  
Cellular Level ◽  
Cell Polarization ◽  
Raw264.7 Cells ◽  
Immunomodulatory Effects ◽  
Lycium Barbarum ◽  
Wide Range

Lycium barbarum L. is a widely used functional food and medicinal herb in Asian countries. L. barbarium polysaccharides (LBP) are considered as one of the major medicinal components of L. barbarium fruit and exhibits a wide range of biological activities. Here, we investigated the immunomodulatory effects of LBP and its uptake behaviors at the cellular level. LBP was prepared by water extraction and ethanol precipitation, and divided into two fractions based on the molecular weight distribution by ultrafiltration (LBP > 10 kDa and LBP < 10 kDa). The physicochemical properties of LBP and LBP fractions were well characterized. The LBP > 10 kDa fraction greatly enhanced the viability of macrophages RAW264.7 cells and induced cell polarization, but had weak effects to other tested tumor cell lines and normal cell line. This fraction could regulate the production of NO, TNF-α, IL-6 and ROS in RAW264.7 cells, suggesting both pro-inflammatory and anti-inflammatory effects. The dye-labeled LBP could be internalized into all tested cell lines and accumulated in lysosomes. The internalization of LBP in RAW264.7 cells is mainly through the clathrin-mediated endocytosis pathway. The Caco-2 intestinal transport experiment demonstrated that the dye labeled LBP could be transported through the Caco-2 cell monolayer (mimic intestinal epithelium) through clathrin-mediated endocytosis. These results demonstrate the immunomodulatory effects of LBP and its effective uptake by macrophages and intestine.

Cytotoxic and Genotoxic Activities of Alkaloids from the Bulbs of Griffinia gardneriana and Habranthus itaobinus (Amaryllidaceae)

2019 ◽  
Vol 19 (5) ◽  
pp. 707-717 ◽  
Author(s):  
Eduardo R. Cole ◽  
Jean P. de Andrade ◽  
João F. Allochio Filho ◽  
Elisângela F. P. Schmitt ◽  
Anderson Alves-Araújo ◽  
...  
Keyword(s):  
Cell Lines ◽  
Caspase 3 ◽  
Biological Activities ◽  
Docking Studies ◽  
In Vitro Cytotoxicity ◽  
Cytotoxic Activities ◽  
Isolation And Identification ◽  
Wide Range

Background: Amaryllidaceae plants are known to be a great source of alkaloids, which are considered an extensive group of compounds encompassing a wide range of biological activities. The remarkable cytotoxic activities observed in most of the Amaryllidaceae alkaloids derivatives have prompt the chemical and biological investigations in unexplored species from Brazil. Objective: To evaluate the cytotoxic and genotoxic properties of alkaloids of Griffinia gardneriana and Habranthus itaobinus bulbs and study the role of caspase-3 as a molecular apoptosis mediator. Methods: Methanolic crude extracts of Griffinia gardneriana and Habranthus itaobinus bulbs were submitted to acid-base extraction to obtain alkaloid-enriched fractions. The obtained fractions were fractionated using chromatographic techniques leading to isolation and identification of some alkaloids accomplished via HPLC and 1H-NMR, respectively. Molecular docking studies assessed the amount of free binding energy between the isolated alkaloids with the caspase-3 protein and also calculated the theoretical value of Ki. Studies have also been developed to evaluate in vitro cytotoxicity and genotoxicity in such alkaloids and apoptosis activation via the caspase pathway using both tumor and normal cell lines. Results: Seven alkaloids were isolated and identified. Among these, 11-hydroxyvittatine and 2-α-7- dimethoxyhomolycorine were not cytotoxic, whereas tazettine, trisphaeridine, and sanguinine only showed activity against the fibroblast lineage. Lycorine and pretazettine were 10 to 30 folds more cytotoxic than the other alkaloids, including cancerous lines, and were genotoxic and capable of promoting apoptosis via the caspase-3 pathway. This result supports data obtained in docking studies wherein these two compounds exhibited the highest free energy values. Conclusion: The cytotoxicity assay revealed that, among the seven alkaloids isolated, only lycorine and pretazettine were active against different cell lines, exhibiting concentration- and time-dependent cytotoxic actions alongside genotoxic action and the ability to induce apoptosis by caspase-3, a result consistent with those obtained in docking studies.

scholarly journals New Hybrid Compounds Combining Fragments of Usnic Acid and Monoterpenoids for Effective Tyrosyl-DNA Phosphodiesterase 1 Inhibition

Biomolecules ◽  
2021 ◽  
Vol 11 (7) ◽  
pp. 973
Author(s):  
Nadezhda S. Dyrkheeva ◽  
Aleksandr S. Filimonov ◽  
Olga A. Luzina ◽  
Alexandra L. Zakharenko ◽  
Ekaterina S. Ilina ◽  
...  
Keyword(s):  
Cell Lines ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Usnic Acid ◽  
Topoisomerase 1 ◽  
Binding Domains ◽  
Promising Therapeutic Target ◽  
Wide Range ◽  
Ic50 Values ◽  
Low Cytotoxicity

Usnic acid (UA) is a secondary metabolite of lichens that exhibits a wide range of biological activities. Previously, we found that UA derivatives are effective inhibitors of tyrosyl-DNA phosphodiesterase 1 (TDP1). It can remove covalent complex DNA-topoisomerase 1 (TOP1) stabilized by the TOP1 inhibitor topotecan, neutralizing the effect of the drugs. TDP1 removes damage at the 3′ end of DNA caused by other anticancer agents. Thus, TDP1 is a promising therapeutic target for the development of drug combinations with topotecan, as well as other drugs for cancer treatment. Ten new UA enamino derivatives with variation in the terpene fragment and substituent of the UA backbone were synthesized and tested as TDP1 inhibitors. Four compounds, 11a-d, had IC50 values in the 0.23–0.40 μM range. Molecular modelling showed that 11a-d, with relatively short aliphatic chains, fit to the important binding domains. The intrinsic cytotoxicity of 11a-d was tested on two human cell lines. The compounds had low cytotoxicity with CC50 ≥ 60 μM for both cell lines. 11a and 11c had high inhibition efficacy and low cytotoxicity, and they enhanced topotecan’s cytotoxicity in cancerous HeLa cells but reduced it in the non-cancerous HEK293A cells. This “protective” effect from topotecan on non-cancerous cells requires further investigation.

scholarly journals Functional Features of Alginates Recovered from Himanthalia elongata Using Subcritical Water Extraction

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4726
Author(s):  
Noelia Flórez-Fernández ◽  
Herminia Domínguez ◽  
María Dolores Torres
Keyword(s):  
Cell Lines ◽  
Subcritical Water ◽  
Biological Activities ◽  
Water Extraction ◽  
Size Exclusion ◽  
Subcritical Water Extraction ◽  
Wide Range ◽  
Himanthalia Elongata ◽  
Functional Features ◽  
Acetone Fractionation

Subcritical water extraction of Himanthalia elongata and the subsequent acetone fractionation to precipitate crude fucoidans generated a liquid phase which was used to recover alginates with a wide range of viscoelastic features and other soluble extracts with potential biological activities. The precipitated alginate was converted to sodium alginate using an environmentally friendly treatment before being characterized by Fourier transform infrared attenuated total reflectance, nuclear magnetic resonance, high performance size exclusion chromatography and rheological measurements. The cell viability of three human cell lines (A549, HCT-116, T98G) in the presence of the extracts obtained before and after acetone fractionation was assessed. Fractionation with different acetone volumes showed a slight effect in the behavior of the different tested cell lines. Results also indicated a notable effect of the processing conditions on the block structure and molar mass of the extracted biopolymer, with the subsequent impact on the rheological properties of the corresponding gelled matrices.

scholarly journals Exploration of Benzenesulfonamide-Bearing Imidazole Derivatives Activity in Triple-Negative Breast Cancer and Melanoma 2D and 3D Cell Cultures

2021 ◽  
Vol 14 (11) ◽  
pp. 1158
Author(s):  
Benas Balandis ◽  
Vytautas Mickevičius ◽  
Vilma Petrikaitė
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cell Lines ◽  
Triple Negative Breast Cancer ◽  
Heterocyclic Compounds ◽  
Triple Negative ◽  
Biological Activities ◽  
Human Malignant Melanoma ◽  
Imidazole Derivatives ◽  
Wide Range

Heterocyclic compounds are one of the main groups of organic compounds possessing wide range of applications in various areas of science and their derivatives are present in many bioactive structures. They display a wide variety of biological activities. Recently, more and more attention has been focused to such heterocyclic compounds as azoles. In this work, we have synthesized a series of new imidazole derivatives incorporating a benzenesulfonamide moiety in their structure, which then were evaluated for their cytotoxicity against human triple-negative breast cancer MDA-MB-231 and human malignant melanoma IGR39 cell lines by MTT assay. Benzenesulfonamide-bearing imidazole derivatives containing 4-chloro and 3,4-dichlorosubstituents in benzene ring, and 2-ethylthio and 3-ethyl groups in imidazole ring have been determined as the most active compounds. Half-maximal effective concentration (EC50) of the most cytotoxic compound was 27.8 ± 2.8 µM against IGR39 cell line and 20.5 ± 3.6 µM against MDA-MB-231 cell line. Compounds reduced cell colony formation of both cell lines and inhibited the growth and viability of IGR39 cell spheroids more efficiently compared to triple-negative breast cancer spheroids.

scholarly journals Triterpenic Acid Content and Cytotoxicity of Some Salvia Species From Iran

2019 ◽  
Vol 14 (5) ◽  
pp. 1934578X1984272 ◽  
Author(s):  
Hoda Abdollahi-Ghehi ◽  
Ali Sonboli ◽  
Samad Nejad Ebrahimi ◽  
Mohammad Ali Esmaeili ◽  
Mohammad Hossein Mirjalili
Keyword(s):  
Cell Lines ◽  
High Performance ◽  
Human Cancer ◽  
Biological Activities ◽  
Dry Weight ◽  
Leaf Length ◽  
Array Detector ◽  
Human Cancer Cell Lines ◽  
Wide Range ◽  
Commercial Species

For prosperous domestication, breeding, and cultivation of a herbal species, it is important to screen its medicinally valuable compounds as well as its referred biological activity. Salvia L. species (Lamiaceae), distributed throughout the world, contain a wide range of secondary metabolites including terpenoids and phenolic derivatives. Betulinic acid (BA), oleanolic acid (OA), and ursolic acid (UA) are highly valuable triterpenic acids (TAs) because of their wide range of biological activities. The objective of the present work was to evaluate the BA, OA, and UA contents among 22 Salvia species native to Iran. TA content in the studied Salvia species was compared with that in Salvia officinalis as a commercial species. High-performance liquid chromatography with photodiode array detector results showed that the maximum content of BA (3.12 ± 0.03 mg/g dry weight [DW]) and OA (1.96 ± 0.05 mg/g DW) was determined in Salvia multicaulis. The highest content of UA (4.34 ± 0.1 mg/g DW) was quantified in S. officinalis L. followed by S. multicaulis (3.71 ± 0.08 mg/g DW). Salvia multicaulis exhibited significantly higher agro-morphological values than S. officinalis in traits related to plant width, leaf length, internode length, and inflorescence length. The cytotoxicities of both species were determined against human cancer cell lines using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. The methanolic extract of S. multicaulis and S. officinalis showed cytotoxic effects against SH-SY5Y and MCF-7 cell lines, respectively. Both species were equally cytotoxic against the HL-60 cell line. This study provides scope for the selection of high-yielding species and genetic improvement through breeding and biotechnological programs in the future.

scholarly journals Fructus lycii: A Natural Dietary Supplement for Amelioration of Retinal Diseases

Nutrients ◽  
2021 ◽  
Vol 13 (1) ◽  
pp. 246
Author(s):  
Kumari Neelam ◽  
Sonali Dey ◽  
Ralene Sim ◽  
Jason Lee ◽  
Kah-Guan Au Eong
Keyword(s):  
Bioactive Compounds ◽  
Biological Activities ◽  
Complex Mixture ◽  
The Body ◽  
Age Related Macular Degeneration ◽  
Retinal Diseases ◽  
Lycium Barbarum ◽  
Wide Range ◽  
Fructus Lycii ◽  
Functional Components

Fructus lycii (F. lycii) is an exotic “berry-type” fruit of the plant Lycium barbarum that is characterized by a complex mixture of bioactive compounds distinguished by their high antioxidant potential. F. lycii is used in traditional Chinese home cooking and in the Chinese Pharmacopeia as an aid to vision and longevity as well as a remedy for diabetes to balance “yin” and “yang” in the body for about two centuries. Although a myriad of bioactive compounds have been isolated from F. lycii, polysaccharides, carotenoids, flavonoids, and phenolics represent the key functional components of F. lycii. F. lycii has been shown to exhibit a wide range of biological activities in experimental settings including antioxidant, anti-inflammatory, antiapoptotic, and neuroprotective effects. Despite its medicinal role dating back to the eighteenth century in the Far East and robust evidence of beneficial effects on ocular health and retinal diseases originating mainly from studies in animal models, the role of F. lycii in the clinical management of retinal diseases is yet to be established. This article comprehensively reviews the literature germane to F. lycii and retinal diseases with particular emphasis on age-related macular degeneration, diabetic retinopathy, and retinitis pigmentosa, which are commonly seen in clinical practice.

scholarly journals Non-Linear Optical Property and Biological Assays of Therapeutic Potentials Under In Vitro Conditions of Pd(II), Ag(I) and Cu(II) Complexes of 5-Diethyl amino-2-({2-[(2-hydroxy-Benzylidene)-amino]-phenylimino}-methyl)-phenol

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 5089 ◽  
Author(s):  
Laila H. Abdel-Rahman ◽  
Mohamed S. Adam ◽  
Ahmed M. Abu-Dief ◽  
Hanan El-Sayed Ahmed ◽  
Ayman Nafady
Keyword(s):  
Schiff Base ◽  
Cell Lines ◽  
Density Functional ◽  
Energy Gap ◽  
Biological Activities ◽  
Good Growth ◽  
Nlo Property ◽  
Wide Range ◽  
Non Linear ◽  
Linear Optical

Herein, we report facile procedures for synthesis of a new Schiff base ligand (H2L,5-Diethylamino-2-({2-[(2-hydroxy-benzylidene)-amino]-phenylimino}-methyl)-phenol) and its Ag(I), Pd(II) and Cu(II) complexes. The structure of the H2L ligand as well as its metal complexes was deduced based on wide range of analytical, structural and spectroscopic tools, along with theoretical evidence via density functional theory (DFT) calculations. The obtained results indicated that the Schiff base (H2L) ligand acts as a tetradentate N2O2 donor with two azomethine nitrogen’s (N1, N2) and two deprotonated phenolic oxygens (O1, O2) atoms. A distorted octahedral structure is assigned to [CuL(OH2)2]·3/2H2O complex and square planar structure for PdL and AgL complexes. The electronic structure and non-linear optical (NLO) property of the prepared compounds were discussed theoretically by the B3LYP/GENECP program. Results revealed that all complexes have non-planner geometries as indicated from the dihedral angles. The charge transfer occurs within the synthesized complexes as indicated from the calculated energy gap between HOMO and LUMO energies. The H2L ligand and its complexes are excellent candidates for NLO materials as implied from their hyperpolarizabilities and polarizabilities values. The biological activities of the prepared complexes against selected microorganisms and cancer cell lines gave good growth inhibitory effect. The biocidal potencies of the ligand and its complexes can be arranged as follows: AgL > CuL > PdL > H2L, as compared to the used standard drugs. The antiproliferative activity of the studied complexes against different carcinoma cell lines such as liver (Hep-G2), breast (MCF-7) and colon (HCT-116) followed the order H2L < AgL< PdL < CuL < vinblastine. Probing the binding interactions of prepared complexes with calf thymus (CT)-DNA using electronic absorption, gel electrophoresis and viscosity measurements revealed strong interaction via intercalation modes, as also evidenced by their molecular docking study.

Lawsone (2-hydroxy-1,4-naphthaquinone) derived anticancer agents

2022 ◽  
Vol 0 (0) ◽  
Author(s):  
Arvind Singh ◽  
Amartya Basu ◽  
Aditi Sharma ◽  
Anu Priya ◽  
Manmmet Kaur ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Cancer Cell Lines ◽  
Biologically Active ◽  
Synthetic Methods ◽  
Lawsonia Inermis ◽  
Wide Range ◽  
Tree Leaf

Abstract 2-Hydroxy-1,4-naphthaquinone, commonly known as lawsone, represents an extremely important biologically active naturally occurring compound. It can easily be isolated from Lawsonia inermis (henna) tree leaf extract. Last decade has seen tremendous applications of lawsone as a starting component for the preparation of various organic scaffolds. Many of these synthesized scaffolds showed a wide range of biological activities including potential activities towards several cancer cell lines. This review deals with diverse synthetic methods of lawsone derived scaffolds and their screening against different anti-cancer cell lines along with promising results.

scholarly journals Anticancer Activities of the Quinone-Methide Triterpenes Maytenin and 22-β-hydroxymaytenin Obtained from Cultivated Maytenus ilicifolia Roots Associated with Down-Regulation of miRNA-27a and miR-20a/miR-17-5p

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 760
Author(s):  
Camila Hernandes ◽  
Lucyene Miguita ◽  
Romario Oliveira de Sales ◽  
Elisangela de Paula Silva ◽  
Pedro Omori Ribeiro de Mendonça ◽  
...  
Keyword(s):  
Head And Neck ◽  
Cell Line ◽  
Cell Lines ◽  
Squamous Cell ◽  
Biological Activities ◽  
Intraperitoneal Administration ◽  
Kidney Tissue ◽  
Quinone Methide ◽  
Wide Range ◽  
Maytenus Ilicifolia

Natural triterpenes exhibit a wide range of biological activities. Since this group of secondary metabolites is structurally diverse, effects may vary due to distinct biochemical interactions within biological systems. In this work, we investigated the anticancer-related activities of the quinone-methide triterpene maytenin and its derivative compound 22-β-hydroxymaytenin, obtained from Maytenus ilicifolia roots cultivated in vitro. Their antiproliferative and pro-apoptotic activities were evaluated in monolayer and three-dimensional cultures of immortalized cell lines. Additionally, we investigated the toxicity of maytenin in SCID mice harboring tumors derived from a squamous cell carcinoma cell line. Both isolated molecules presented pronounced pro-apoptotic activities in four cell lines derived from head and neck squamous cell carcinomas, including a metastasis-derived cell line. The molecules also induced reactive oxygen species (ROS) and down-regulated microRNA-27a and microRNA-20a/miR-17-5p, corroborating with the literature data for triterpenoids. Intraperitoneal administration of maytenin to tumor-bearing mice did not lead to pronounced histopathological changes in kidney tissue, suggesting low nephrotoxicity. The wide-ranging activity of maytenin and 22-β-hydroxymaytenin in head and neck cancer cells indicates that these molecules should be further explored in plant biochemistry and biotechnology for therapeutic applications.

Pharmacologically potentials of different substituted coumarin derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Benzene Ring ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Pharmacological Properties ◽  
Coumarin Derivatives ◽  
Wide Range ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
Coumarin Compounds

Coumarin and its derivatives are widely spread in nature. Coumarin goes to agroup as benzopyrones, which consists of a benzene ring connected to a pyronemoiety. Coumarins displayed a broad range of pharmacologically useful profile.Coumarins are considered as a promising group of bioactive compounds thatexhibited a wide range of biological activities like anti-microbial, anti-viral,antiparasitic, anti-helmintic, analgesic, anti-inflammatory, anti-diabetic, anticancer,anti-oxidant, anti-proliferative, anti-convulsant, and antihypertensiveactivities etc. The coumarin compounds have immense interest due to theirdiverse pharmacological properties. In particular, these biological activities makecoumarin compounds more attractive and testing as novel therapeuticcompounds.

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