Cytotoxic Flavonoids from the Aerial Parts of Stachys lavandulifolia Vahl

Background: Stachys lavandulifolia Vahl is a herbaceous plant distributed in the west and south western Asia. Despite of the wide medicinal uses, there are some reports on toxicity potential of this plant. In present study we attempted to evaluate the toxicity and to characterize the cytotoxic principles of S. lavandulifolia. Methods: Brine shrimp lethality test (BSLT) was used to evaluate the general toxicity of the extracts and essential oil obtained from the aerial parts of S. lavandulifolia. Phytochemical constituents of the active extract were investigated using various chromatographic and spectroscopic methods. GC and GC-MS were also used to analyze the plant essential oil. GC and GC-MS were used to analyze the plant essential oil. Cytotoxic activities of the isolated compounds were also evaluated using MTT assay method. Results: In brine shrimp lethality test (BSLT), chloroform extract and the plant essential oil exhibited the most toxicity against Artemia salina larvae (LD50: 121.8±5.6 and 127.6±14.7 µg ml-1, respectively). GC and GC-MS analyses of essential oil led to the characterization of forty compounds of which α-bisabolol (23.85%) and thymol (17.88%) were identified as the main constituents. Nine flavonoids, Pachypodol (1), chrysosplenetin (2), kumatakenin (3), velutin (4), penduletin (5), viscosine (6), chrysoeriol (7), hydroxygenkwanin (8) and apigenin (9) were isolated from the chloroform extract of S. lavandulifolia. Among the isolated compounds, chrysosplenetin (2), a polymethoxylated flavonoid, was found as the most toxic compound toward MDA-MB-23 and HT-29 cells, with IC50 values of 88.23 and 116.50 µg ml-1, respectively. Furthermore, chrysosplenetin (2), kumatakenin (3) and viscosine (6) with selectivity indices of 2.70, 2.59 and 3.33, respectively, showed higher preferential toxicity against MDA-MB-23 cells in comparison with tamoxifen (SI:2.45). Conclusion: This study reports methoxylated flavonoids as compounds which could be involved in toxicity of S. lavandulifolia. The results of MTT assay also suggest some of these compounds as appropriate candidates for anti-cancer drug development research

Analysis and evaluation of the antimicrobial and anticancer activities of the essential oil isolated from <i>Foeniculum vulgare</i> from Hamedan, Iran

<p>In this study, biological properties of the essential oil isolated from seeds of <i>Foeniculum vulgare</i> (<i>F. vulgare</i>) were evaluated. GC-MS analysis revealed Trans-Anethole (80.63%), L-Fenchone (11.57%), Estragole (3.67%) and Limonene (2.68%) were the major compounds of the essential oil. Antibacterial activity of the essential oil against nine Gram-positive and Gram-negative strains was studied using disc diffusion and micro-well dilution assays. Essential oil exhibited the antibacterial activity against three Gram-negative strains of <i>Pseudomonas aeruginosa</i>, <i>Escherichia coli</i>, and <i>Shigella dysenteriae</i>. The preliminary study on toxicity of seed oil was performed using Brine Shrimp lethality test (BSLT). Results indicated the high toxicity effect of essential oil (LC50 = 10 μg/mL). <i>In vitro</i> anticancer activity of seed oil was investigated against human breast cancer (MDA-Mb) and cervical epithelioid carcinoma (Hela) cell lines by MTT assay. Results showed the seed oil behave as a very potent anticancer agent with IC50 of lower than 10 μg/mL in both cases.</p

Imperatorin attenuates the proliferation of MCF-7 cells in combination with radiotherapy or hyperthermia

Background: Breast cancer is one of the most common types of malignancies in the world. Cancer resistance is an unavoidable consequence of therapy with radiation or other modalities. On-going research aims to improve cancer response to therapy. Aim: The aim of this study was to evaluate the possible sensitization effect of imperatorin (IMP) in combination with external radiotherapy (ERT) or HT. Methods: After treatment of MCF-7 breast cancer cells with IMP, cells were exposed to 4 Gy X-rays or HT (42 °C for 1 hour). The viability of MCF-7 cells was measured using an MTT assay. Further-more, the expression of pro-apoptotic genes, including Bax, Bcl-2, caspase-3, caspase-8, and caspase-9, was investigated using real-time PCR. The sensitizing effect of IMP in combination with ERT or HT was calculated and compared to ERT or HT alone. Results: Results showed an increase in the expression of pro-apoptotic genes and downregulation of anti-apoptotic Bcl-2 following ERT and HT. Furthermore, cell viability was reduced following these treatments. IMP was able to augment these effects of ERT and HT. Conclusion: IMP could increase the efficiency of HT and ERT. This effect of IMP may suggest it as an adjuvant for increasing the therapeutic efficiency of ERT

Suberosin attenuates the proliferation of MCF-7 breast cancer cells in combination with radiotherapy or hyperthermia

Aim: The aim of this study was to determine the proliferation of MCF-7 following irradi-ation or hyperthermia as alone or pre-treatment with suberosin. Background: Radiotherapy is a major therapeutic modality for the control of breast cancer. Howev-er, hyperthermia can be prescribed for relief of pain or enhancing cancer cell death. Some studies have attempted its use as an adjuvant to improve therapeutic efficiency. Suberosin is a cumar-in-derived natural agent that has shown anti-inflammatory properties. Objective: In this in vitro study, possible sensitization effect of suberosin in combination with radiation or hyperthermia was evaluated. Methods: MCF-7 breast cancer cells were irradiated or received hyperthermia with or without treatment with suberosin. The incidence of apoptosis as well as viability of MCF-7 cells were observed. Furthermore, the expressions of pro-apoptotic genes such as Bax, Bcl-2, and some caspases were evaluated using real-time PCR. Results: Both radiotherapy or hyperthermia reduced the proliferation of MCF-7 cells. Suberosin amplified the effects of radiotherapy or hyperthermia for induction of pro-apoptotic genes and re-ducing cell viability. Conclusion: Suberosin has a potent anti-cancer effect when combined with radiotherapy or hyper-thermia. It could be a potential candidate for killing breast cancer cells as well as increasing the therapeutic efficiency of radiotherapy or hyperthermia

Bioactive coumarins from the roots and fruits of <i>Ferulago trifida</i> Boiss.<i>,</i> an endemic species to Iran

<p>Phytochemical analysis of the <i>Ferulago trifida</i> Boiss. from Apiaceae family led to the isolation and identification of suberosin (<b>1</b>), isoimperatorin (<b>2</b>), prantschimgin (<b>3</b>), oxypeucedanin (<b>4</b>), oxypeucedanin methanolate (<b>5</b>), suberenol (<b>6</b>), 6-hydroxymethylherniarin (<b>7</b>), oxypeucedanin hydrate (<b>8</b>), ulopterol (<b>9</b>), bergapten (<b>10</b>), xanthotoxin (<b>11</b>), imperatorin (<b>12</b>) and grandivittin (<b>13</b>) from chloroform extracts of the roots (<b>1–9</b>) and fruits (<b>1</b>, <b>2</b>, <b>8</b>, <b>10–13</b>) of this species. Oxypeucedanin methanolate and suberenol demonstrated a potent antioxidant power with 268.2 ± 5.4 and 251.2 ± 6.2 mmol FSE/100 g, respectively, compared by BHT (267.2 ± 4.2 mmol FSE/100 g) in FRAP method. The potent antibacterial effects were found for oxypeucedanin methanolate on <i>S. epidermidis</i> (IZ; 26 mm, MIC; 250 μg mL⁻¹) an oxypeucedanin hydrate on <i>K. pneumoniae</i> (IZ: 21 mm, MIC: 250 μg mL⁻¹). Moreover, suberosin showed higher preferential toxicity against MDA-MB-23 cells (IC₅₀: 0.21 mM, SI: 5.0), in comparison with tamoxifen (IC₅₀: 0.012 mM, SI: 2.45) in MTT assay.</p