A Simple Liquid-Liquid Fractionation (LLF) Method for Isolating Deoxyandrographolide dan Andrographolide from Herbs of Andrographis paniculata (Burm., F) Ness and Its Cytotoxic Activity on 3T3-L1 Preadipocyte Cells

The main bitter constituents of sambiloto (Androgaphis paniculata (Burm., F) Ness) are diterpene lactones, namely andrographolide and deoxyandrographolide which have been reported to have antidiabetic, cytotoxic, antiatherosclerosis, anti-inflammatory, and antimicrobial activity. There are many studies that performed the isolation of deoxyandrographolide and andrographolide from A. paniculata herbs, but most of them included several steps that make them not efficient. This research was conducted to do an isolation of deoxyandrographolide and andrographolide through liquid-liquid fractionation (LLF) due to its simplicity, low cost, and time efficient. The extraction of deoxyandrographolide and andrographolide from the herbs was carried out using chloroform as the solvent by using Soxhlet apparatus, and LLF was performed to isolate the compounds. The identities of the compounds were confirmed by TLC scanner compared to its standard references. Hence, these present methods were successfully isolated and determined deoxyandrographolide and andrographolide of A. paniculata. The compounds were also showed relatively moderate cytotoxicity on 3T3-L1 cell lines using 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt (MTS) assay, with LC50 of deoxyandrographolide and andrographolide; 29.3173 µg/mL and 37.7011 µg/mL, respectively.

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Cytotoxic activity against tumour cell lines and anti-inflammatory effects of compounds isolated from Xylopia aromatica

Planta Medica ◽

10.1055/s-0033-1352067 ◽

2013 ◽

Vol 79 (13) ◽

Author(s):

O Estrada ◽

L González ◽

M Mijares ◽

Á Fernández ◽

M Ruiz ◽

...

Keyword(s):

Cytotoxic Activity ◽

Cell Lines ◽

Tumour Cell ◽

Tumour Cell Lines ◽

Anti Inflammatory

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Cytotoxicity to Five Cancer Cell Lines of the Respiratory Tract System and Anti-inflammatory Activity of Thai Traditional Remedy

Natural Product Communications ◽

10.1177/1934578x19845815 ◽

2019 ◽

Vol 14 (5) ◽

pp. 1934578X1984581

Author(s):

Thana Juckmeta ◽

Weerachai Pipatrattanaseree ◽

Wuttichai Jaidee ◽

Bhanuz Dechayont ◽

Jitpisute Chunthorng-Orn ◽

...

Keyword(s):

Respiratory Tract ◽

Cytotoxic Activity ◽

Cell Lines ◽

Cancer Cell ◽

Cancer Cell Lines ◽

Inhibitory Effect ◽

Inflammatory Activity ◽

Traditional Remedy ◽

Anti Inflammatory ◽

Minor Compounds

A Thai traditional remedy called Benchalokawichian (BLW) consists of 5 plant species, Ficus racemosa, Capparis micracantha, Clerodendrum petasites, Harrisonia perforata, and Tiliacora triandra. It has long been used in Thai traditional medicine to reduce fever in respiratory tract infection, but there is no report on either cytotoxicity against cancer cell lines of the respiratory tract system or anti-inflammatory effect. Thus, the objectives of this research were to investigate the cytotoxic activity of the ethanolic and water extracts of BLW, its single plant ingredients and its isolated compounds against 5 cancer cell lines of the respiratory tract, by SRB assay. Anti-inflammatory activity of all extracts and compounds was also tested by using lipopolysaccharide-induced nitric oxide (NO) in RAW 264.7 cells. The main compounds were isolated by high-performance liquid chromatography and compared with BLW and plant ingredients. A major compound of BLW and H. perforata ethanolic extracts is perforatic acid, which inhibited the growth of 2 lung cancer cell lines, A549 and H226, with IC50 values of 6.7 and 13.2 µg/mL. The ethanolic extract of BLW and T. triandra showed cytotoxic activity against all cancer cell lines with IC50 values in the range of 10.1 to 45.2 µg/mL. In contrast, all EtOH extracts showed moderate anti-inflammatory activity, but the water extract had no inhibitory effect on either activity. Pectolinarigenin and O-methyllaloptaeroxyrin, 2 minor compounds, exhibited NO inhibitory effect with IC50 values of 7.1 and 7.9 µg/mL, respectively, whereas perforatic acid was inactive (>50 µg/mL). Moreover, pectolinarigenin showed high cytotoxic activity against all cancer cell lines of the respiratory system with IC50 values in the range of 1.9 to 9.1 µg/mL. As a result, these 2 minor compounds can be used as markers for quality control of BLW for anti-inflammatory activity. Perforatic acid and pectolinarigenin are of interest for further study on their cytotoxic mechanism. Remarkably, T. triandra, one of the plant components of BLW, is possibly the source of the active cytotoxic compounds.

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Aspirin-Based Organoiron Dendrimers as Promising Anti-Inflammatory, Anticancer, and Antimicrobial Drugs

Biomolecules ◽

10.3390/biom11111568 ◽

2021 ◽

Vol 11 (11) ◽

pp. 1568

Author(s):

Alaa S. Abd-El-Aziz ◽

Maysun R. Benaaisha ◽

Amani A. Abdelghani ◽

Rabin Bissessur ◽

Laila H. Abdel-Rahman ◽

...

Keyword(s):

Antimicrobial Activity ◽

Anticancer Activity ◽

Cell Lines ◽

Cancer Cell ◽

Inflammatory Activity ◽

Breast Cancer Cell Lines ◽

Cell Viability Assay ◽

Reference Drug ◽

Anti Inflammatory

Designing nanocarriers with actions directed at a specific organ or tissue is a very promising strategy since it can significantly reduce the toxicity of a bioactive drug. In this study, an organometallic dendrimer was used to synthesize a biocompatible drug delivery system by attaching aspirin to the periphery of the dendrimer. Our goal is to enhance the bioavailability and anticancer activity of aspirin and reduce its toxicity through successive generations of organoiron dendrimers. The biological activity of aspirin-based dendrimer complexes was evaluated. The result of antimicrobial activity of the synthesized dendrimers also demonstrated an increase in their antimicrobial activity with increased generation of the dendrimers for most types of microorganisms. This study reveals for the first time that organoiron dendrimers linked with aspirin exhibit an excellent Gram-negative activity comparable to the reference drug Gentamicin. All synthesized dendrimers were tested for their anticancer activity against breast cancer cell lines (MCF-7), hepatocellular cell lines (Hep-G2), and a non-cancer cell line, Human Embryonic Kidney (HEK293), using the MTT cell viability assay and compared against a standard anticancer drug, Doxorubicin. Compounds G3-D9-Asp and G4-D12-Asp exhibited noticeable activity against both cell lines, both of which were more effective than aspirin itself. In addition, the in vivo anti-inflammatory activity and histopathology of swollen paws showed that the designed aspirin-based dendrimers displayed significant anti-inflammatory activity; however, G2-D6-Asp showed the best anti-inflammatory activity, which was more potent than the reference drug aspirin during the same period. Moreover, the coupling of aspirin to the periphery of organoiron dendrimers showed a significant reduction in the toxicity of aspirin on the stomach.

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INDICATORS OF CELL METABOLISM IN VITRO IN RESEARCHES OF ANTI-INFLAMMATORY AND CYTOTOXIC EFFECTS OF FULLEROPYRROLIDINES С60 AND THEIR INITIAL SUBSTRATES

THE BULLETIN ◽

10.32014/2020.2518-1467.139 ◽

2020 ◽

Vol 5 (387) ◽

pp. 25-33

Author(s):

S. D. Fazylov ◽

◽

O. A. Nurkenov ◽

A. E. Arinova ◽

A. M. Gazaliev ◽

...

Keyword(s):

Antifungal Activity ◽

Cytotoxic Activity ◽

Cell Lines ◽

Neutrophil Elastase ◽

Cytotoxic Effect ◽

Fullerene C60 ◽

Elastase Activity ◽

Anti Inflammatory ◽

C60 Derivatives

The article considers data on the in vitro study of new fulleropyrrolidine compounds for anti-inflammatory and cytotoxic activity in cultures of human monocyte cell lines MonoMac-6 and THP-1Blue and also as inhibitors of human neutrophil elastase. This enzyme is a regulator of inflammation. In different situations, it can act both as a pro-inflammatory and as an anti-inflammatory agent. An imbalance in the regulation of elastase activity plays an important role in the pathogenesis of cystic fibrosis, acute respiratory distress syndrome, bronchiectasis, chronic obstructive pulmonary disease, type 2 diabetes mellitus, atherosclerosis and hypertension. In the future, such studies should lead to the creation of optimal in vitro models that most adequately reflect the situation in vivo and establish the relationship between the structure and activity of the studied drugs. It is noted that the presence of lipophilic properties in fullerene C60 derivatives is especially important in the development of pharmaceuticals for the control of pathogens of various infectious diseases. Fullerene C60 derivatives have the ability to easily penetrate lipid membranes, overcome the blood-brain barrier, and modulate ion transport. Compounds were tested for anti-inflammatory and cytotoxic activity (in vitro) on cultures of human monocytic cell lines MonoMac-6 and THP-1Blue. Modified fullerene compounds of various structures were tested for their inhibitory ability against neutrophil elastase enzyme (in vitro). Elastase activity was evaluated by the ability of fulleropyrrolidine compounds to hydrolyze the synthetic substrate N-methylsuccinyl-Ala-Ala-Pro-Val-7-amino-4-me-thylcoumarin (Calbiochem). The results of studies of fullerene compounds in relation to their anti-inflammatory and cytotoxic activity are obtained. The analysis of the fluorescence kinetics of the compounds was carried out. The cytotoxic activity of the samples was investigated in the Brine Schrimp test using Artemia salina. All compounds have cytotoxicity, which suggests a lack of selectivity of chemotherapeutic action. In general, the presence of a cytotoxic effect confirms the reality of antimicrobial action. The results of the study of the antibacterial and antifungal activity of the synthesized new fulleropyrrolidines and their starting substrates are described (S. aureus 505, Bacillus subtilis, Str.agalactiae, E. Coli M-17, Ps.aeruginosa, Candida аlbicans, Penicillium citrinum, Aspergillus niger, Aspergillus flavus, Trichophyton mentagraphytos, Epidermophyton fioccosum). As a result of the study of the potential antifungal activity of the compounds, it was found that only two drugs inhibit the growth of test cultures in vitro. All other studied samples have practically no activity against the yeast fungi Candida albicans. In general, the presence of a cytotoxic effect in the studied fullerene compounds confirms the reality of the antimicrobial action.

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Sivas İlinde Kültürü Yapılan Kenger (Gundellia tournefortii L.) Bitkisi Tohumlarının Besin Elementlerinin ve Biyolojik Aktivitelerinin Değerlendirilmesi

Turkish Journal of Agriculture - Food Science and Technology ◽

10.24925/turjaf.v7isp2.52-58.3126 ◽

2019 ◽

Vol 7 (sp2) ◽

pp. 52

Author(s):

Handan Saraç ◽

Ahmet Demirbaş ◽

Sevgi Durna Daştan ◽

Mehmet Ataş ◽

Özge Çevik ◽

...

Keyword(s):

Oxidative Stress ◽

Antimicrobial Activity ◽

Cytotoxic Activity ◽

Cell Lines ◽

Water Extract ◽

Mass Spectrometry Analysis ◽

Stress Index ◽

Aureus Strain ◽

Klebsiella Pneumonia ◽

Oxidative Stress Index

The aim of the present study is to conduct a general content evaluation of water extract obtained from the seeds of Gundellia tournefortii by GC-MS (Gas chromatography–Mass spectrometry) analysis, to determine its macro and micro element concentrations, antimicrobial activity and total antioxidant level (TAS), total oxidant level (TOS), oxidative stress index (OSI) values, and to reveal its anti-carcinogenic properties on various cell lines. Rel Assay Diagnostics kits were used to determine TAS, TOS and OSI values. By determining the minimum inhibition concentration (MIC) value by Microdilution Broth method, antimicrobial activity analyses were performed on microorganisms which are Staphylococcus aureus (ATCC 29213), Enterococcus faecalis (ATCC 29212), Pseudomonas aeruginosa (ATCC 27853), Escherichia coli (ATCC 25922), Bacillus cereus (ATCC11778), Klebsiella pneumonia (ATCC 13883), Candida albicans (ATCC 10231) and Candida tropicalis (DSM11953), respectively. By MTT method, cytotoxic activity was determined on normal mouse fibroblast cell line, HUVEC and 3 different human cancer cell lines. As a result, it was determined that Gundelia tournefortii plant extract has a rather weak antimicrobial activity except for on S. aureus strain, a good antioxidant activity, and a cytotoxic activity in some cells. As for the oxidative stress index of the plant, it was found to be low. In addition, in terms of macro and micro nutrient content of the plant Gundellia tournefortii has concentrations of 3.64% N, 0.11% P, 3.78% K, 0.22% Ca, 0.57% Mg, 268.4 mg/kg Fe, 16.7 mg/kg Zn, 19.4 mg/kg Mn and 8.3 mg/kg Cu.

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Metabolites Profiling, In Vitro, In Vivo, Computational Pharmacokinetics and Biological Predictions of Aloe perryi Resins Methanolic Extract

Plants ◽

10.3390/plants10061106 ◽

2021 ◽

Vol 10 (6) ◽

pp. 1106

Author(s):

Rasha Saad Suliman ◽

Sahar Saleh Alghamdi ◽

Rizwan Ali ◽

Dimah A. Aljatli ◽

Sarah Huwaizi ◽

...

Keyword(s):

Cytotoxic Activity ◽

Cell Lines ◽

Cancer Cell ◽

Methanolic Extract ◽

Bioactive Constituents ◽

Pharmacokinetic Properties ◽

Anti Inflammatory ◽

Aloe Perryi

Background: Aloe perryi is a traditional herb that has various biological and pharmacological properties such as anti-inflammatory, laxative, antiviral, antidiabetic, and antitumor effects, which have not been deliberated before. The current investigation aims to evaluate in vitro cytotoxicity against several cancer cell lines in addition to in vivo anti-inflammatory activities of Aloe perryi extract using a rat animal model. Moreover, the pharmacokinetic properties of bioactive constituents and possible biological targets were assessed and evaluated. The methanolic extract of Aloe perryi was prepared by maceration, to tentatively identify the biomolecules of the Aloe perryi extract, analytical LC–QTOF-MS method was employed for Aloe perryi methanolic extract. The cytotoxic activity was examined in six cancer cell lines using Titer-Glo assay and the IC50s were calculated in addition to in silico target predictions and in vivo anti-inflammatory activity assessment. Subsequently, the pharmacokinetics of the identified active components of Aloe perryi were predicted using SwissADME, and target prediction using the Molinspiration webserver. The cytotoxic activity on HL60 and MDA-MB-231 was moderately affected by the Aloe perryi extract with IC50 of 63.81, and 89.85 μg/ml, respectively, with no activity on other cells lines. Moreover, the Aloe perryi extract exhibited a significant increase in wound contraction, hair growth, and complete re-epithelization when compared with the negative control. The pharmacokinetic properties of the bioactive constituents suggested a good pharmaceutical profile for the active compounds and nuclear receptors and enzymes were the two main possible targets for these active compounds. Our results demonstrated the promising activity of Aloe perryi extract with cytotoxic and anti-inflammatory properties, indicating a potential therapeutic utility of this plant in various disease conditions.

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Analgesic, Anti-Inflammatory, Cytotoxic Activity Screening and UPLC-PDA-ESI-MS Metabolites Determination of Bioactive Fractions of Kleinia pendula

Molecules ◽

10.3390/molecules25020418 ◽

2020 ◽

Vol 25 (2) ◽

pp. 418 ◽

Cited By ~ 1

Author(s):

Mohammad Alfaifi ◽

Abdulrhman Alsayari ◽

Narasimman Gurusamy ◽

Justin Louis ◽

Serag Eldin Elbehairi ◽

...

Keyword(s):

Ethyl Acetate ◽

Cytotoxic Activity ◽

Cell Lines ◽

Cancer Cell ◽

Cancer Cell Lines ◽

Plant Metabolites ◽

Esi Ms ◽

Anti Inflammatory

Kleinia pendula (Forssk.) DC. is a prostrate or pendent dark green succulent herb found in the southwestern mountain regions of Saudi Arabia. The literature survey of the plant reveals a lack of phytochemical and pharmacological studies, although traditional uses have been noted. The objective of the present work was to assess the in vivo analgesic and anti-inflammatory activities, as well as, the in vitro cytotoxic potential of the fractions of Kleinia pendula, and correlate these activities to the plant metabolites. The methanolic extract of Kleinia pendula was subjected to fractionation with n-hexane, ethyl acetate, chloroform, n-butanol, and water. The fractions were screened for their analgesic and anti-inflammatory activities, as well as cytotoxic activity against breast, liver, and colon cancer cell lines. The n-hexane and chloroform fractions of Kleinia pendula showed significant cytotoxic activity against all three cancer cell lines tested. The ethyl acetate and chloroform fractions showed significant analgesic and anti-inflammatory activities. The metabolites in these three active fractions were determined using UPLC-PDA-ESI-MS. Thus, the analgesic and anti-inflammatory activities of the plant were attributed to its phenolic acids (caffeoylquinic acid derivatives, protocatechuic, and chlorogenic acids). While fatty acids and triterpenoids such as (tormentic acid) in the hexane fraction are responsible for the cytotoxic activity; thus, these fractions of Kleinia pendula may be a novel source for the development of new plant-based analgesic, anti-inflammatory, and anticancer drugs.

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Benefits of Cardamom (Elettaria cardamomum (L.) Maton) and Turmeric (Curcuma longa L.) Extracts for Their Applications as Natural Anti-Inflammatory Adjuvants

Plants ◽

10.3390/plants10091908 ◽

2021 ◽

Vol 10 (9) ◽

pp. 1908

Author(s):

Gustavo R. Cárdenas Garza ◽

Joel H. Elizondo Luévano ◽

Aldo F. Bazaldúa Rodríguez ◽

Abelardo Chávez Montes ◽

Raymundo A. Pérez Hernández ◽

...

Keyword(s):

Cytotoxic Activity ◽

Cell Lines ◽

Hela Cells ◽

Curcuma Longa ◽

Experimental Studies ◽

Chemical Components ◽

No Production ◽

Elettaria Cardamomum ◽

Peritoneal Cells ◽

Anti Inflammatory

The genus Zingiberaceae has been widely used for phytotherapeutic purposes in traditional medicine throughout the world for its anti-inflammatory activity. Experimental studies have established that inflammation caused by chronic infections represents a risk factor for different forms of cancer. The objective of this study was focused on determining the anti-inflammatory capacity and cytotoxic activity of aqueous extracts of Elettaria cardamomum (cardamom) and Curcuma Longa (turmeric). The extracts were obtained by maceration and, through GC-MS/MS, a total of 11 different chemical components were determined in the aqueous extract of cardamom and 7 in the extract of turmeric. The main compounds found in cardamom and turmeric were α-terpinyl acetate (54.46%) and β-turmerone (33.45%), respectively. RT-qPCR results showed significantly lower gene expression levels of innate inflammatory cytokines (IL-6 and TNF-α) compared to the control (LPS). Also, it was observed that the extracts do not possess cytotoxic activity against different cell lines, where E. cardamomum showed EC50 (µg/mL) of 473.84 (HeLa cells), 237.36 (J774A.1 cells), 257.51 (Vero E6 cells), and 431.16 (Balb/C peritoneal cells) and C. longa showed EC50 (µg/mL) of 351.17 (HeLa cells), 430.96 (J774A.1 cells), 396.24 (Vero E6 cells), and 362.86 (Balb/C peritoneal cells). The results of this research suggest that natural extracts of E. cardamomum and C. longa possess anti-inflammatory effects and no cytotoxic activity against HeLa, J774A.1, Vero E6, and Balb/C peritoneal cell lines. Finally, it was observed that the extracts also decreased nitric oxide (NO) production in peritoneal macrophages.

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