Eryngium billardieri Extract and Fractions Induces Apoptosis in Cancerous Cells

Background: Eryngium is genus flowering plants in the Umbelliferae family having pharmacological properties such as anti-inflammatory and anti-diabetic. Given the nature of melanoma and breast cancers in recent years and the fact that the anti-cancer properties of Eryngium billardieri on mentioned cell lines have not been studied, the present study conducted to explore these properties. Objective: The mechanisms of cytotoxicity and apoptosis of aerial parts of various extracts and fractions of E. billardieri on cancerous cells and normal cells were investigated. Methods: Samples were collected from natural habitats, dried and then extracted by Soxhlet apparatus with solvents of n-Hex, DCM and methanol, respectively. The cytotoxic effects of the extracts were investigated by MTT method on MCF7, B16 and HFF-2 classes for 24 and 48 hours. Flowcytometry, was also used to investigate the mechanism of cytotoxicity and confirming by Real-time PCR of p53 and Bax genes, which codes apoptosis regulator proteins. Meanwhile, volatile compounds of extracts were identified by GC-MS method. Results: The obtained data showed that the n-Hex extract of E. billardieri on B-16 and MCF7 cell lines and dichromethane extract on MCF7 cell line had the most significant cytotoxic effect compared to DMSO control (p value <0.001). Our finding showed that the mechanism of n-Hex extract with 80% and 100% vlc fractions on B16 induced apoptotic compared to HFF-2 control cells, moreover, n-Hex extract and 80% vlc fraction on MCF7 was apoptotic. The major compounds of n-Hex, DCM and 80% and 100% fractions of n-Hex extract obtained from GC-MS are non-terpenoid. Conclusion: Non-terpenoids compounds of E. billardieri can be the responsible for showing the most cytotoxic effects on MCF7 and B16 cell lines with apoptotic mechanism and n-Hex extract had the most significant inhibitory effect on cancerous cells compared to the HFF-2 control cells by the mechanism of apoptosis.

Transcriptome analysis and connectivity mapping of Cissampelos pareira L. provides molecular links of ESR1 modulation to viral inhibition

Bioactive fractions obtained from medicinal plants which have been used for the treatment of multiple diseases could exert their effects by targeting common pathways. Prior knowledge of their usage could allow us to identify novel molecular links. In this study, we explored the molecular basis of action of one such herbal formulation Cissampelos pareira L. (Cipa), used for the treatment of female hormone disorders and fever. Transcriptomic studies on MCF7 cell lines treated with Cipa extract carried out using Affymetrix arrays revealed a downregulation of signatures of estrogen response potentially modulated through estrogen receptor α (ERα). Molecular docking analysis identified 38 Cipa constituents that potentially bind (ΔG < − 7.5) with ERα at the same site as estrogen. The expression signatures in the connectivity map (https://clue.io/;) revealed high positive scores with translation inhibitors such as emetine (score: 99.61) and knockdown signatures of genes linked to the antiviral response such as ribosomal protein RPL7 (score: 99.92), which is a reported ERα coactivator. Further, gene knockdown experiments revealed that Cipa exhibits antiviral activity in dengue infected MCF7 cells potentially modulated through estrogen receptor 1. This approach reveals a novel pathway involving the ESR1-RPL7 axis which could be a potential target in dengue viral infection.

Phytochemical Analysis of Anvillea garcinii Leaves: Identification of Garcinamines F–H and Their Antiproliferative Activities

Anvillea garcinii is a medicinal plant used in the Arab region for intestinal diseases, lung and liver diseases, digestive problems, and as an antidiabetic agent. Repeated chromatographic purifications of A. garcinii leaves led to the isolation of three undescribed guaiane sesquiterpene derivatives, named garcinamines F–H, characterized by the presence of an amino acid unit, along with five known sesquiterpene lactones (garcinamines B–E and 9β-hydroxyparthenolide). The structures of the new compounds were established using spectroscopic (1D and 2D NMR) and spectrometric methods (ESIMS). Garcinamine H possesses a double bond at the Δ1,10 position, a structural feature rarely reported in guaianolide-type sesquiterpenes. The antiproliferative activity of the isolated sesquiterpenes was screened against three different cancer cell lines, and 9β-hydroxyparthenolide and garcinamines C and D displayed significant effects against lung carcinoma (A549), colon carcinoma (LoVo), and breast carcinoma (MCF7) cell lines.

Morphomolecular identification, metabolic profile, anticancer, and antioxidant capacities of Penicillium sp. NRC F1 and Penicillium sp. NRC F16 isolated from Egyptian remote cave

Searching for remote locations to screen for microorganisms, identify their metabolites, and investigate their bioactivities against lethal diseases such as cancer is of critical importance. In the current study, two fungal strains where isolated from a remote cave in Asyut governorate, Egypt. These isolates were morphologically and molecularly identified through sequencing their ITS region as Penicillium sp. NRC F1, and Penicillium sp. NRC F16. Investigating the metabolic profiles of the silylated ethyl acetate extracts of these fungi through conducting GC-Ms analysis revealed presence of 114 compounds belonging to different chemical classes. On the other hand, studying the in vitro bioactivity of both extracts showed moderate antioxidant activities. Penicillium sp. NRC F1 extract exhibited higher DPPH scavenging activity (74.41 ± 0.59%) at concentration of 200 µg/ml, in comparison with that exerted by Penicillium sp. NRC F16 extract at the same concentration (65.58 ± 1.55%). Moreover, studying the cytotoxicity of extracts against human colon cancer (HCT116), and human breast cancer (MCF7) cell lines revealed that cytotoxicity of both extracts was dose dependent. Promising cytotoxic effect was achieved against human colon cancer HCT116 using 200 µg/ml of Penicillium sp. NRC F1 extract (95.72 ± 1.13 % cytotoxicity), while Penicillium sp. NRC F16 ethyl acetate extract caused a cytotoxicity of 95.43 ± 1.4 %. Similarly, investigating the in vitro cytotoxicity of the extracts against human breast cancer MCF7 cell line resulted in observing promising activity of Penicillium sp. NRC F1 and Penicillium sp. NRC F16 extracts, and they exhibited 97.29 ± 0.61 %; and 97.08 ± 1.07 % cytotoxicity, respectively. Results from this study nominate those strains as promising isolates and encourage for conducting further in vivo investigations to evaluate their potency.

New Bioactive Sesquiterpeniods From the Plant Endophytic Fungus Pestalotiopsis theae

Three new secondary metabolites pestalothenins A–C (1–3), including two new humulane-derived sesquiterpeniods (1 and 2) and one new caryophyllene-derived sesquiterpeniod (3), together with five known compounds (4–8) were isolated from the crude extract of the plant endophytic fungus Pestalotiopsis theae (N635). Their structures were elucidated by the extensive analyses of HRESIMS and NMR spectroscopic data. The absolute configurations of 1–3 were determined by comparison of experimental and calculated electronic circular dichroism (ECD) spectra. The cytotoxic effects of these compounds were evaluated in vitro. Compound 6 showed moderate cytotoxicity against T24 and MCF7 cell lines. In addition, compounds 1–8 were also evaluated for antibacterial activity.