Cytotoxic effect of Leurius quinquestratus (scorpion) venom in different human cancer cell lines in vitro

Purpose: In this study, the cytotoxicity of scorpion Leurius quinquestratus crude venom (LQCV) was evaluated in vitro in selected human cancer cell lines. Methods: Breast (MCF-7), hepatocellular (HepG-2), colon (CaCo-2), cervix (HeLa) and alveolar (A-549) adenocarcinoma cell lines were tested. MTT assay and median inhibition concentration (IC50), apoptotic assay, caspase 3, P53, Bcl-2 proteins and cell cycle were determined. Results: 24 hrs post-treatment, CaCo-2 represented the most sensitive cell line (IC50 of 4.12 μg/mL). Due to the exposure to 1/10 IC50 of LQCV, the percentage of the apoptotic cells, caspase 3, and P53 proteins were increased significantly (P<0.05) while Bcl-2 was decreased in comparison to untreated cells. Treatment with LQCV induced cell cycle arrest at G1 and G2/M phases. Conclusion: LQCV displays potent cytotoxicity against selected human cell lines in vitro. Thus, the material could become a potent agent for the management of some cancers.

Medicinal plants show remarkable antiproliferative potential in human cancer cell lines

Molecules isolated and identified from plant origin are used to manufacture most chemotherapeutic drugs for cancer treatment. We assumed that these plant extracts contain prolific bioactive compounds with potent antiproliferative activities and could be effective against different human cancer cells. Ethanolic extracts were prepared from Chelidonium majus, Myrica cerifera, Fumaria indica, Nigella sativa, and Silybum marianum, and the antiproliferative assay was performed in HepG2 and HeLa human cancer cell lines. All plants extract exhibited antiproliferative potential against studied cancer cell lines in the dose and time-dependent manner. Chelidonium majus and Silybum marianum have shown promising results against HepG2 and HeLa cells, respectively, followed by Myrica cerifera, Fumaria indica, and Nigella sativa. Results indicated that utilization of whole plant extract as anticancer compounds could be of great value in generating novel chemotherapeutic drugs.

Three-dimensional prints from 3-dimensional cell culture aggregates of human cancer cell lines

Objectives: Three-dimensional (3D) printing has gained significance for human health-care applications in recent years. Some of these applications include obtaining models which mimic anatomical parts. One other parallel development in the biological research area is the development of 3D cell cultures. Such cultures are now becoming the material of choice for in vitro experiments, fast replacing the traditional adherent/monolayer 2D culture approaches. We present here, a method to obtain 3D prints of 3D aggregates of three human cancer cell lines. Such 3D prints can be useful models to understand solid tumor morphologies and also as effective teaching models. Materials and Methods: Photomicrographs of the 3D aggregates of the human cancer cell lines SiHa, MCF-7, and A549 (human cervical cancer, breast cancer, and non-small cell lung cancer cell lines, respectively) were obtained using inverted phase contrast microscopy. Conversion of normal jpeg images into 3D files was performed using the lithophane method and CAD files obtained. The CAD files thus generated were used to print the objects using the Stratasys Polyjet J750 3D Printer. Results: We could obtain 3D prints of SiHa, MCF-7, and A549 (human cervical cancer, breast cancer, and non-small cell lung cancer cell lines, respectively) 3D aggregates/spheroids. Conclusion: It is hoped that this approach will be useful for studying solid tumor morphologies in finer details. Furthermore, other benefits of such 3D prints would be in them being excellent models for teaching purposes.

Two New Triterpenes from Basidiomata of the Medicinal and Edible Mushroom, Laetiporus sulphureus

In the search for novel anti-infectives from natural sources, fungi, in particular basidiomycetes, have proven to still harbor so much potential in terms of secondary metabolites diversity. There have been numerous reports on isolating numerous secondary metabolites from genus Laetiporus. This study reports on two new triterpenoids, laetiporins C and D, and four known triterpenes from the fruiting body of L. sulphureus. The structures of the isolated compounds were elucidated based on their 1D and 2D nuclear magnetic resonance (NMR) spectroscopic data in combination with high-resolution electrospray mass spectrometric (HR-ESIMS) data. Laetiporin C exhibited weak antifungal activity against Mucor hiemalis. Furthermore, the compounds showed weak antiproliferative activity against the mouse fibroblast L929 and human cancer cell lines, including KB-3-1, A431, MCF-7, PC-3 and A549.

Diaportones A–C: Three New Metabolites From Endophytic Fungus Diaporthe foeniculina BZM-15

Phytochemical investigation of Diaporthe foeniculina BZM-15 led to one new γ-butyrolactone derivative, diaportone A (1), one cyclopentenone derivative, diaportone B (3), and one monoterpene derivative, diaportone C (5), along with six known compounds (2, 4, and 6–9). Their structures as well as the absolute configurations were characterized by means of NMR, HRESIMS, and ECD spectroscopy and quantum chemistry calculation, respectively. Furthermore, all compounds were evaluated for their cytotoxic activity and antibacterial activity, and compounds 7 and 8 displayed significant antiproliferative effects on three human cancer cell lines (SF-268, MCF-7, and HepG2) with IC50 values ranging from 3.6 to 15.8 μM.

Design, Synthesis and Evaluation of Novel Derivatives of Curcuminoids with Cytotoxicity

Curcumin and curcuminoids have been discussed frequently due to their promising functional groups (such as scaffolds of α,β-unsaturated β-diketone, α,β-unsaturated ketone and β′-hydroxy-α,β-unsaturated ketone connected with aromatic rings on both sides) that play an important role in various bioactivities, including antioxidant, anti-inflammatory, anti-proliferation and anticancer activity. A series of novel curcuminoid derivatives (a total of 55 new compounds) and three reference compounds were synthesized with good yields using three-step organic synthesis. The anti-proliferative activities of curcumin derivatives were examined for six human cancer cell lines: HeLaS3, KBvin, MCF-7, HepG2, NCI-H460 and NCI-H460/MX20. Compared to the IC50 values of all the synthesized derivatives, most α,β-unsaturated ketones displayed potent anti-proliferative effects against all six human cancer cell lines, whereas β′-hydroxy-α,β-unsaturated ketones and α,β-unsaturated β-diketones presented moderate anti-proliferative effects. Two potent curcuminoid derivatives were found among all the novel derivatives and reference compounds: (E)-5-hydroxy-7-phenyl-1- (3,4,5-trimethoxyphenyl)hept-1-en-3-one (compound 3) and (1E,4E)-1,7-bis (3,4,5-trimethoxyphenyl)hepta-1,4-dien-3-one (compound MD12a). These were selected for further analysis after the evaluation of their anti-proliferative effects against all human cancer cell lines. The results of apoptosis assays revealed that the number of dead cells was increased in early apoptosis and late apoptosis, while cell proliferation was also decreased after applying various concentrations of (E)-5-hydroxy-7-phenyl-1- (3,4,5-trimethoxyphenyl)hept-1-en-3-one (compound 3) and (1E,4E)-1,7-bis (3,4,5-trimethoxyphenyl)hepta-1,4-dien-3-one (compound MD12a) to MCF-7 and HpeG2 cancer cells. Analysis of the gene expression arrays showed that three genes (GADD45B, SESN2 and BBC3) were correlated with the p53 pathway. From the quantitative PCR analysis, it was seen that (1E,4E)-1,7-bis (3,4,5-trimethoxyphenyl) hepta-1,4-dien-3-one (compound MD12a) effectively induced the up-regulated expression of GADD45B, leading to the suppression of MCF-7 cancer cell formation and cell death. Molecular docking analysis was used to predict and sketch the interactions of the GADD45B-α,β-unsaturated ketone complex for help in drug design.