Effect of combination treatment of protocatechuic acid with 5-fluorouracil and oxaliplatin on colon cancer Caco-2 cell line

Among the most common antitumor drugs used in the treatment of colon cancer are 5-fluorouracil and oxaliplatin (5-FU and OXA). However, both these drugs have many side effects, and hence there is a need for new treatment\approach to reduce the side effects aas well as drug concentration. In this context, here, we investigated the effect of addition of protocatechuic acid (PCA) onto either monotherapies or combination therapies of 5-FU and OXA on the human colon cancer (Caco-2) cell line. In addition, we did evaluate the synergistic effect of PCA with 5-FU and OXA. Further, we determined the suppressive effects of different doses of PCA alone or in combination with 5-FU/OXA on cell proliferation after 24 and 48 hours. We identified a suppressive effect of PCA on cell viability at 48 h starting from the dose of 50 µM Matrix metalloproteinase-2 (MMP-2) and MMP-9 gene expression levels and apoptotic effects showed significant increases and decreases depending on the dose and time applied in the experimental groups. The highest synergistic activity was seen at 2:1 concentration of 5-FU+ PCA. Our findings indicate the presence of the cytotoxic and apoptotic effects of PCA in Caco-2 cells at 48 h, increasing with a dose- and time-dependent manner.

Anticancer potential of Solanum lycopersicum L. extract in human lung epithelial cancer cells A549

The study aimed to reveal the phytochemical profile, free radical scavenging potential, and anticancer activity of Solanum lycopersicum L. leaf extract (SLLE). According to the study, SLLE contains plant secondary metabolites that are beneficial for health, like phenolics, flavonoids, ascorbic acid, alkaloids, and terpenoids. The SLLE has shown potential free radical scavenging potential in DPPH and ABTS free radical scavenging analysis and its EC50 values (concentration required to inhibit 50% of free radicals) were determined as 481.29 ± 33.82 and 527.56 ± 20.34 µg/mL, respectively. The SLLE has the ability to scavenge free radicals and could be used to treat illnesses brought on by oxidative stress. The anticancer activity of SLLE was assessed by MTT, LDH, micro-morphological, live/dead dual staining, and caspase-3 analysis. In the MTT assay, the IC50 value (concentration required to inhibit 50% of cell viability) of SLLE was determined as 190.41 ± 4.77 µg/mL. Furthermore, SLLE has shown potential anticancer activity by adversely affecting the plasma membrane integrity and escalating the caspase-3 levels. In the biomedical field, SLLE could be highly useful to treat cancer.

Antiproliferative and cytotoxic activities of Mentha x piperita L. essential oil in non-small cell lung cancer cells

Among 33 types of listed cancers worldwide, lung cancer with 2.2 million cases (12.2% of total cancer cases) ranks second next only to breast cancer. Globally, Turkey, with overall rate of 40.0 (41,264 cases), ranks 5th among top 10 countries in lung cancer. Currently used therapeutic agents and approaches have considerable side effects, and hence, there is a need for alternative agents for effective management of lung cancer. In this study, we explored the in vitro cytotoxic, antiproliferative and proapoptotic activities of Mentha x piperita L. (peppermint) essential oil in human non-small cell lung cancer (A549) cells. Cell viability was determined by MTT assay, morphological changes were determined by confocal microscopy and apoptosis promoting action was determined by flow cytometry technique. Peppermint essential oil found to effectively decrease the viability of non-small cell lung cancer cells and IC50 value was detected at low concentrations (2.12%) for 24 h. In addition, peppermint essential oil was found to alter the morphology of A549 cells, leading to changes that could describe programmed cell death. Apoptosis was the triggered cell death by Mentha x piperita essential oil. Results reveal that Mentha x piperita essential oil has antiproliferative and anticarcinogenic properties which could be attributed to the bioactive phytochemical contents and has the potential to be used as an anticancer agent and chemotherapeutic drug.

Evaluation of arjunolic acid against Brucella melitenis and in vitro cytotoxic study of lung adenocarcinomic cell line (A549)

Brucellosis, a neglected tropical disease of zoonotic nature, is caused by the genus Brucella, specifically by Brucella abortus and B. melitensis in cattle and humans, respectively. Arjunolic acid (AA) is a triterpenoid, isolated from Terminalia arjuna (Roxb.) Wight & Arn., a medicinally important plant used to treat various diseases in the Indian system of medicine. Here, we tried to evaluate AA for its antibacterial activity on Brucella and the in vitro cytotoxicity assay on human lung adenocarcinomic alveolar basal epithelial cell line (A549). Also, we assessed the synergistic effect of arjunolic acid and Tarenna asiatica (L.) Kuntze ex K.Schum. on B. melitensis. AA displayed a considerable antibacterial activity [zone of inhibition (9 mm) with a minimum inhibitory concentration of 30 ?g/mL] against B. melitensis. The rate of cell death for the cancer cells were at 100 ?g/mL concentration of AA was 82% which indicates that AA shows significant membrane disruption to cancer cells. The estimated IC50 of AA against the A549 cell line was 139.90 ?g/mL. The highest synergistic activity was exhibited forming a zone of inhibition measuring 10mm when arjunolic acid and AqE of T. asiatica was added in the concentration of 1:1, respectively.

Anticancer effect of Piper betle leaf extract on KB cell lines – an in vitro study

Background: Various researchers have stated a causal association of betle quid chewing with oral cancer and other potentially malignant disorders of oral cavity. On the contrary, Piper betle leaf when used alone has potential medicinal benefits including anticancer, anti-helminthic, hepato-protective and antioxidant activities. In this is study we examined the anti-cancer activity of Piper betle extract (aqueous) on KB- cancer cell lines Aims: To observe the anti- cancer activity of Piper betle leaf extract on KB cancer cell lines. Setting and Design: The study was conducted in Biogenix Research Centre, Thiruvananthapuram. The KB cancer cell lines were procured from NCCS, Pune. Methods and Material: The cancer cell lines were treated with increasing concentration of Piper betle leaf extract 6.25,12,25,50 & 100?g/ml. The cytotoxic effect of the extract on the cells was studied by physical indicators of cytotoxic changes by observing the cells under an inverted phase contrast microscope, for any detectable changes in the cell morphology and by MTT assay method to assess the percentage of viability of cells. Results: The cancer cells showed considerable changes in the cell morphology suggestive of cell cytotoxicity and apoptosis after the treatment with the extract. The results of the MTT assay showed that the percentage viability of the cancer cells decreased with increasing concentrations of the extract, The percentage of viability of cells was noted to be 43.42% with the highest concentration of 100?g/ml of Piper betle leaf extract which proves that Piper betle leaf extract has anticancer activity. Conclusion: The cytotoxic potential of Piper betle leaf may be used to develop chemotherapeutic agent, but further focused studies of anticancer properties and isolation of compounds from Piper betle leaf are necessary to prove its worth in the cancer therapy.

In vitro cytotoxic and genotoxic analysis of Garcinia humilis crude extract

Garcinia humilis, known commonly as achachairú or bacupari, has great medicinal value. Their fruits have pharmacological, antibacterial, antioxidant, and anticancer properties. Therefore, the objective of the present study was to evaluate the cytotoxicity and genotoxicity of G. humilis crude extract in breast tumor cells. Cytotoxicity was determined using the Resazurin reduction assay and genotoxicity by the single cell gel electrophoresis assay (Comet assay) on human MCF-7 cells. Crude extract of G. humilis was cytotoxic only when used at high concentrations (IC50 = 5.084 mg mL-1). The Comet assay showed that the crude extract did not induce genotoxicity at 1 and 5 mg mL-1 but did show signs of DNA fragmentation and DNA fragmentation at 10 mg mL-1. The cytotoxic activity against breast adenocarcinoma cells at high concentrations suggests that this medicinal plant could be used with caution and must be further studied to understand better its therapeutic and toxicological potential in the human body.

Broad-spectrum survey of medicinal plants as a potential source of anticancer agents / Estudio de amplio espectro de plantas medicinales como fuente potencial de agentes contra el cáncer

Cancer is an abnormal and uncontrolled growth of cells that spreads through cell division. There are different types of medicines available to treat cancers, but no drug is found to be fully effective and safe for humans. The major problem involved in the cancer treatments is the toxicity of the established drug and their side effects. Medicinal plants are used as folk medicines in Asian and African populations for thousands of years. 60% of the drugs for treating cancer are derived from plants. More than 3000 plants have anticancer activity. The present review aims at the study of a broad spectrum survey of plants having anticancer components for different type of cancers. This article consists of 364 medicinal plants and their different parts as potential Source of Anticancer Agents.

El cáncer es un crecimiento anormal y descontrolado de células que se disemina a través de la división celular. Hay diferentes tipos de medicamentos disponibles para tratar el cáncer, pero no se ha encontrado ningún medicamento que sea completamente efectivo y seguro para los seres humanos. El principal problema involucrado en los tratamientos del cáncer es la toxicidad del fármaco establecido y sus efectos secundarios. Las plantas medicinales se utilizan como medicinas populares en poblaciones asiáticas y africanas durante miles de años. El 60% de los medicamentos para el tratamiento del cáncer se derivan de plantas. Más de 3000 plantas tienen actividad anticancerígena. La presente revisión tiene como objetivo el estudio de un estudio de amplio espectro de plantas que tienen componentes anticancerígenos para diferentes tipos de cánceres. Este artículo consta de 364 plantas medicinales y sus diferentes partes como fuente potencial de agentes anticancerígenos.

The phytochemical, biological, and medicinal attributes of phytoecdysteroids: An updated review

The phytoecdysteroids (PEs) comprise a large group of biologically-active plant steroids, which have structures similar to those of insect-molting hormones. PEs are distributed in plants as secondary metabolites that offer protection against phytophagus (plant-eating) insects. When insects consume the plants containing these chemicals, they promptly molt and undergo metabolic destruction; the insects eventually die. Chemically, ecdysteroids are a group of polyhydroxylated ketosteroids that are structurally similar to androgens. The carbon skeleton of ecdysteroids is termed as cyclopentanoperhydro-phenanthrene with a

Recent advances in novel anticancer agents targeting β-catenin/TCF4 interaction for molecular cancer therapeutics / 药学学报

Wnt/β-catenin signaling pathway plays an important role in the proliferation, growth, invasion, and metastasis of human cancers. Moreover, β-catenin/T-cell factor 4 (TCF4) interaction regulates the transcription of the key oncogenes in Wnt/β-catenin signaling pathway. Therefore, β-catenin/TCF4 interaction would be a promising therapeutic target for the development of highly selective anticancer agents. At present, most ongoing small-molecule inhibitors targeting β-catenin/TCF4 interaction, including PKF222-815, iCRT3/5/14, LF3, and sanguinarine, have been developed in preclinical studies for human cancer therapeutics. In this review, we summarized the research advances of up-to date inhibitors targeting β-catenin/TCF4 interaction, including the molecular structure and cellular functions of β-catenin in canonical Wnt signaling pathway. This review holds a hopeful avenue for the development of novel and highly selective Wnt inhibitors targeting β-catenin/TCF4 interaction for future anticancer strategy.

Protopine inhibits the growth of hepatocellular carcinoma through a mitochondrially mediated apoptosis pathway / 药学学报

Hepatocellular carcinoma (HCC) is a serious threat for human health, the incidence of HCC in China accounts for more than 50% worldwide. There is an urgent need to develop novel anticancer agents for the treatment of HCC patients. Here we characterized the inhibitory effect and the molecular mechanism of protopine on HCC cancer cells. The results of a CCK-8 assay indicated that protopine displays anticancer activities on HCC cells. Flow cytometry and JC-1 staining confirmed that treatment with protopine decreased the mitochondrial membrane potential and induced apoptosis in HCC cells. Western blot analysis showed that protopine was able to increase protein expression in the mitochondrial apoptotic pathway; the level of cytochrome C, apoptotic protease activating factor-1 (Apaf-1), Bax, cleaved-poly ADP-ribose polymerase (cleaved-PARP), cleaved-caspase-3, and cleaved-caspase-9 were increased while the expression of Bcl-2 was suppressed significantly. An in vivo study revealed that protopine significantly suppressed the growth of tumors in nude mice bearing HepG2 cells. Administration of protopine intraperitoneally at a concentration of 50 mg·kg-1 inhibited tumor growth by 72.46%. Animal experiments were carried out according to the Regulation of the Animal Ethics Committee of Southwest Medical University. This study provides preliminary evidence that there is potential to develop protopine as a lead compound for the treatment of HCC.

In vitro screening for growth inhibition activity on cancer cell lines of northern Chile highlands shrubs / Triagem in vitro da atividade de inibição do crescimento em linhagens celulares de câncer em arbustos das montanhas do norte do Chile

ABSTRACT: Cancer is still one of the leading causes of death worldwide. Many chemotherapeutics from plants have been tested in cancer, such as vinblastine and paclitaxel. The north of Chile, Arica & Parinacota region, is characterized by its vegetal biodiversity due to its unique geographical and climatological conditions, offering an unexplored and unique source of naturally-derived compounds. The present research has considered a screening of 26 highland herbs using an in vitro growth inhibition model in a panel of six cancer cell lines from different tissues. 5 of the 26 studied ethanolic extracts shows strong activity at least in one cell line when tested at 10 µg mL-1. We present a group of plants worthy to be evaluated as promissory extracts. This work is part of the systematic attempt to find new candidates to be used in cancer therapies.

RESUMO: O câncer ainda é uma das principais causas de morte no mundo. Muitos quimioterápicos de plantas foram testados em câncer, como vinblastina e paclitaxel. O norte do Chile, região de Arica e Parinacota, caracteriza-se por sua biodiversidade vegetal devido às suas condições geográficas e climatológicas únicas, oferecendo uma fonte inexplorada e única de compostos de origem natural. A presente pesquisa considerou uma triagem de 26 ervas das terras altas usando um modelo de inibição de crescimento in vitro em um painel de seis linhas celulares de câncer de diferentes tecidos. Cinco, dos 26 extratos etanólicos estudados, mostram forte atividade pelo menos em uma linhagem celular quando testados a 10 µg mL-1. Apresentamos um grupo de plantas dignas de serem avaliadas como extratos promissórios. Este trabalho faz parte da tentativa sistemática de encontrar novos candidatos para serem usados ​​em terapias contra o câncer.

Design, synthesis, and cytotoxicity evaluation of new 2,4-disubstituted quinazolines as potential anticancer agents

A series of new 2, 4-disubstituted quinazolines were synthesized by an analog design approach. The synthesis oftitle compounds (3a–f, 4a–c, 5a–c, and 6a–c) was achieved from the corresponding key intermediates 2-(pyridin3-yl) quinazolin-4(3H)-one(2a), 2-(pyridin-3-yl) quinazolin-4(3H)-one (2b) and 2-(pyrazin-2-yl)quinazolin-4(3H)-one (2c) with appropriate amines. The synthesized compounds were characterized by the spectral studies. All thesynthesized compounds were evaluated for in vitro anticancer activity employing 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay against human adenocarcinoma (HT-29), breast cancer (MDA-231), and Ehrlichascites carcinoma cell lines. Among the tested compounds, 5a has a significant anticancer activity (5.33 µM/ml)against the human adenocarcinoma cell line. Other compounds have shown a moderate anticancer activity against thetested cell lines.

Cytotoxicity activity of geldanamycin derivatives against various cancer cell lines

Geldanamycin (1) was isolated as a major compound from Streptomyces zerumbet W14. It was then used as a precursor tosynthesize two new geldanamycins: 17-(tryptamine)-17-demethoxygeldanamycin (2) and 17-(5′-methoxytryptamine)-17-demethoxygeldanamycin (3). The cytotoxicity activity of these two new compounds was evaluated and comparedwith the cytotoxicity of compound 1. Cytotoxicity activity was evaluated against a normal cell line, and three cancercell lines using an 3-(4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) colorimetric assay. Thesolubility of these compounds was also determined. The solubility of compounds 2 and 3 in water was 290.69and 348.18 µM, higher than that of compound 1 by about 1.91 and 2.29 times, respectively. Compounds 2 and 3showed moderate cytotoxic activity on Vero and human cervical carcinoma cells with IC50 values of >200.00 µg/ml. The strongest cytotoxicity of compound 3 was observed in human breast carcinoma cells (MCF-7) and humanhepatocellular carcinoma cell line (HepG2) cells with IC50 values of 82.50 and 114.35 µg/ml, respectively, while theIC50 values of compound 2 against MCF-7 and HepG2 cells were 105.62 and 124.57 µg/ml, respectively. The findingsshowed that these new geldanamycin derivatives exhibited selective cytotoxicity toward some cancer cells at a lowerconcentration. Therefore, future studies on these compounds could be useful for the management of some cancers

Effect of Puta on in vitro anticancer activity of Shataputi AbhrakBhasma on lung, leukemia and prostate cancer cell lines

Background: Rasashastra needs to be upgraded using the technological advances, with regards to drugprocessing, development and therapeutics. The potential of Rasaaushadhis need to be explored by subjecting them against newer life threatening diseases like cancer where contemporary medicine haslimitations. Abhrak Bhasma, one of the drugs of Rasashastra, has some peculiar attributes. According toclassical Rasashastra texts, Shataputi Abhrak Bhasma is regarded as a Rasayan, whose efficacy is in directproportion to the number of Putas. Thus increasing number of Putas not only has a significant effect onthe physical, analytical aspects but also the therapeutic effect of the Abhrak Bhasma.Objectives: To screen in vitro anticancer activity of Abhrak Bhasma at various stages of Putas (20, 50, 100).To evaluate and thus validate the principle from classical Rasashastra texts, which explains direct relationof number of Putas with therapeutic efficacy.Materials and methods: Shataputi Abhrak Bhasma, at various stages of its preparation was subjected toin vitro anticancer activity on three different cancer cell lines (LungHOP62, LeukemiaU937, ProstateDU145) at Tata Memorial Centre- Advanced Centre for Treatment, Research Education in Cancer, NaviMumbai. SRB assay was followed to evaluate the anti-proliferative activity.Results: It was found that Abhrak Bhasma shows concentration dependent positive in vitro anticanceractivity on all three cell lines with highly significant activity on prostate cancer cell lines. Anticanceractivity of Abhrak Bhasma is in the order 100 Puti > 50 Puti > 20 Puti. Shataputi Abhrak Bhasma hadmaximum activity on prostate cancer cell lines almost equivalent to positive control drug adriamycin.Conclusion: The in vitro anticancer activity of Shataputi Abhrak Bhasma increases with increasing numberof Putas, thus revalidating the direct relation between number of Putas and efficacy of the drug.© 2017 Transdisciplinary University, Bangalore and World Ayurveda Foundation. Publishing Services byElsevier B.V

Mikania cordata leaves extract promotes activity against pathogenic bacteria and anticancer activity in EAC cell-bearing swiss albino mice

This study was aimed to screen the activity of the methanolic extract of Mikania cordata leaves (MLME) againstpathogenic bacteria and Ehrlich ascites carcinoma (EAC)-induced cancer in mice. Antibacterial activity was testedagainst some Gram-positive (Bacillus subtilis IFO 3026 and Sarcina lutea IFO 3232) and Gram-negative (Klebsiellapneumoniae ATTC 10031, Proteus vulgaris MTTC 321, Pseudomonas denitrificans KACC 32026, and Xanthomonascampestris IAM 1671) bacteria by disk diffusion and liquid microdilution assay. The anticancer activity wasassessed by EAC cell death, apoptosis, hematological parameters determination, and 3-(4, 5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide test. The MLME exhibited prominent antibacterial activity against the test strains.The minimum inhibitory concentrations were ranged from 1.25 to 20 mg/ml for the bacterial strains that were foundampicillin resistant. The MLME exhibited remarkable anticancer activity on EAC in a dose-dependent manner. Oralintake of MLME at the dosage of 400 mg/kg body weight (b.w) exhibited the highest EAC cell death with remarkableapoptotic features including chromatin condensation, nuclear fragmentation, and accumulation of apoptotic bodies.The MLME-treated EAC-bearing mice showed dose-dependently restored altered hematological parameters towardthe normal level. The IC50 value was 6.6 ± 1.91 µg/ml. These findings suggest that the M. cordata leaves have strongantibacterial and anticancer properties.

Preparation and in vitro evaluation of lactobionic acid modified polyamide-amine dendrimer grafted resveratrol nanoparticles / 中草药

Objective: To prepare resveratrol (Res) nanoparticles grafted with polyamide-amine dendrimer (PAMAM) modified by lactose acid (LA) and evaluate them in vitro. Methods: After partial carboxylation of G3.0 PAMAM terminal (PAMAM-COOH) which synthesized by divergence method. Res was bonded through esterification reaction and LA was grafted on the surface of the carrier through amidation reaction. Nuclear magnetic resonance (1H-NMR) and infrared spectroscopy (IR) were used for characterization. La-PAMAM-Res/Res nanoparticles were prepared by physical encapsulation using LA-PAMAM-Res and Res, and the encapsulation rate was detected by dialysis method. The drug load of the two kinds of nanoparticles was detected by high performance liquid chromatography (HPLC), the particle size was investigated by laser particle size analysis method, the drug release performance in vitro was determined by dialysis method, and the biosafety was evaluated by hemolytic experiment. The cytotoxicity and anticancer activity of PAMAM, PAMAM-COOH, Res, LA-PAMAM-Res and LA-PAMAM-Res/Res were investigated by MTT assay. Results: LA- PAMAM-Res and La-PAMAM-Res/Res nanoparticles were prepared. The encapsulation rate of LA-PAMAM-Res/Res was (75.1 ±2.2) %, the drug loading rates of LA-PAMAM-Res and LA-PAMAM-Res/Res were (7.2 ± 0.9) % and (18.4 ± 1.1) %, respectively. The particle size was (126.3 ± 3.4) nm and (251.0 ± 15.7) nm, respectively. After 72 h, the drug release in vitro was (23.83 ± 0.43)% and (35.28 ± 0.72)%, respectively. The hemolysis rate of both nanoparticles was less than 5%, and the carrier PAMAM-COOH showed less cytotoxicity than PAMAM, and both LA-PAMAM-Res and LA-PAMAM-Res/Res maintained anti-tumor proliferative activity. Conclusion: LA-PAMAM-Res and LA-PAMAM-Res/Res nanoparticles with sustained drug release, good biocompatibility, low cytotoxicity and anticancer activity were prepared, and LA-PAMAM-Res/Res increased the drug load of Res.

In Vitro Study Of An Aqueous Extract Of Eclipta Alba Hassk. For Hepg2 Cell Line

It is the need of the day to identify the new anticancer herbal drug, which not only in possession of good anticancer effects but also cost effective. Here we are presenting such an anticancer Ayurvedic herb which is used since the centuries for the treatment of different diseases of diverse origin. Eclipta alba Hassk., also called as Bhringraj is very important medicinal herb in many medicinal formulations. Though it is commonly used for hair growth, many evidences found its hepatoprotective activity. Here we are presenting all aspects about Bhringraj in terms of qualitative and quantitative values and we have also tried to prove the anticancer activity of it for hepatic cancer. We have used the aqueous extract of Eclipta alba Hassk. for phytochemical analysis, TLC, HPLC analysis to test active chemical components in it. Extract showed presence of many active chemical components which were responsible for its anticancer activity. In vitro study we used the aqueous extract of Eclipta alba Hassk. for the evaluation of its effects on HepG2 (Human liver cancer cell line). The SRB assay results were used to evaluate the anti-cancer activity of the extract. The effects of whole plant extract on cancer cell line were studied. Percentage of cell growth and cell viability were calculated from tabulated result values of srb assay. The experiment revealed that the average percentage of growth inhibition was 68.74%. Cell viability SRB assay also showed significant growth inhibition, at the same time statistical analysis of SRB assay also proved significant results. The research performed here is very useful for set up of different extract studies of Bhringraj for its anticancer activity.

Evaluation Of In-Vitro Anticancer Activity And Quantitation Of Active Ingredient Of Adansonia Digitata L. Fruit

In the world cancer is the major cause of death. Adansonia digitata L is commonly called as baobab belongs to Family Bombacaceae. Due to the high cost and toxic side effects like Bone marrow suppression, hepatotoxicity, nephrotoxicity, Immunosuppression, teratogenicity etc. of chemotherapeutic agents. So, for the proper controlling on cancer the trends of people are moving towards natural therapies. In light to above, in present research A. digitata L is selected for evaluation of in-vitro anticancer activity based on its reported phytoconstituents of fruit and quantitation of active principle of it. The extracts of fruit pulp, seed, and its combination were obtained using solvents like water, ethanol and n-hexane by maceration technique (Aqueous) and Soxhlet extraction method (organic). This extracts were used for further research possesses phytochemical constituents like Carbohydrates, tannins, Saponins, vitamins, alkaloids, terpenoids, phenol, glycoside flavonoids, steroids, etc. in-vitro antioxidant activity were evaluated via free scavenging assay by using DPPH assay method. Further in-vitro anticancer activity was evaluated against three human cancer cell lines MCF-7 (breast cancer cell line), Hep-G2 (liver cancer cell line) and COLO-205 (colon cancer cell line) using Brine Shrimp Lethality Assay (BSLA), Tryphan Blue Dye Cell Exclusion Assay (TBDCEA) and MTT assay. The quantitation of active ingredients Vit. C and Squalene from extracts was done by using titration method and HPLC method respectively. Formulation possesses highest percent antioxidant capacity (49.36). In BSLA formulation possesses highest rate of percent mortality than other extracts. In TBCE assay and in MTT assay formulation gives more significant effect in Hep-G2 liver cancer cell line than remaining cell lines. These findings introduce A. digitata L as potentially useful as anti-cancer agent. Further research is required to elucidate its specific mechanism of action and exact active principle responsible for action.

Two Novel Flavone C-Glycosides Isolated From Afrocarpus Gracilior: Pom Analyses And In Vitro Cytotoxic Activity Aganist Hepatocellular Carcinoma

Objective: Cancer is considered as one of the top reasons of death and the number of cases increasing gradually. Cancer is severe clinical difficulty to the health caution system. This study explored two novel polyphenols of Afrocarpus gracilior Pilger growing in Egypt and evaluated their cytotoxic activity. Methods: Methanolic (80%) extract of the leaves of A. gracilior was subjected to column chromatography; the chemical structures of the isolated compounds were established by advanced spectral techniques: UV, 1H, 13C NMR, two dimensional NMR (2D NMR) and electron spray ionization mass spectroscopy (ESI-MS). Compounds 1 and 2 were studied for their cytotoxic activity against hepatocellular carcinoma (Hep-G2) using sulforhodamine B (SRB) assay. Furthermore the pharmacokinetics profiles of these molecules were accessed by employing Petra/Osiris/Molinspiration (POM) analyses. Results: Two novel C-flavonoid glycosides were isolated [1: Apigenin 8-C-β-D-glucopyranosyl-(1```→4``)-O-β-D-glucopyranoside] and [2: 7-O methyl-luteolin 8-C-β-glucopyranosyl-(1```→4``)-O-β-D-glucopyranoside]. They exhibited significant cytotoxic activity (IC50 = 9.02 and 15.61 µg/ml, respectively) against Hep-G2 cells. The POM analyses revealed that the activity of these two compounds depends on the presence of glucosyl and alkyl groups at the internal and terminal atmosphere of the compounds. Conclusion: These findings demonstrated that the leaves of A. gracilior contain a series of bioactive polyphenolic compounds with significant cytotoxic properties against hepatocellular carcinoma and may be used as alternative anticancer agents for doxorubicin. On the basis of POM calculations, it will be interesting to develop some alternative flavones because the deglucosylated derivatives have a better drug score than parent molecules. This preliminary study will be extended to other strains of cancer.

Enhanced production of prodigiosin by Serratia marcescens FZSF02 in the form of pigment pellets

Background: Prodigiosin has been demonstrated to be an important candidate in investigating anticancer drugs and in many other applications in recent years. However, industrial production of prodigiosin has not been achieved. In this study, we found a prodigiosin-producing strain, Serratia marcescens FZSF02, and its fermentation strategies were studied to achieve the maximum yield of prodigiosin. Results: When the culture medium consisted of 16.97 g/L of peanut powder, 16.02 g/L of beef extract, and 11.29 mL/L of olive oil, prodigiosin reached a yield of 13.622 ± 236 mg/L after culturing at 26 °C for 72 h. Furthermore, when 10 mL/L olive oil was added to the fermentation broth at the 24th hour of fermentation, the maximum prodigiosin production of 15,420.9 mg/L was obtained, which was 9.3-fold higher than the initial level before medium optimization. More than 60% of the prodigiosin produced with this optimized fermentation strategy was in the form of pigment pellets. To the best of our knowledge, this is the first report on this phenomenon of pigment pellet formation, which made it much easier to extract prodigiosin at low cost. Prodigiosin was then purified and identified by absorption spectroscopy, HPLC, and LCMS. Purified prodigiosin obtained in this study showed anticancer activity in separate experiments on several human cell cultures: A549, K562, HL60, HepG2, and HCT116. Conclusions: This is a promising strain for producing prodigiosin. The prodigiosin has potential in anticancer medicine studies.