Chamomile essential oil (CEO) is extracted from chamomile and mainly used in aromatherapy. The chemical constituents and its antitumor activity on Triple-negative breast cancer (TNBC) was explored in the present study. Gas chromatography-mass spectrometry (GC/MS) was employed to analyze the chemical constituents of CEO. The cell viability, migration and invasion of TNBC cell MDA-MB-231 were measured using MTT, wound scratch and Transwell assay, respectively. The protein expression of PI3K/Akt/mTOR signaling pathway was determined by Western blot. CEO is rich in terpenoids (63.51 %), among which the identified terpenoids and their derivatives are mainly Caryophyllene (29.57 %), d-Cadinene (12.81 %), Caryophyllene oxide (14.51 %), etc. Three concentration of CEO (1, 1.5, 2 μg/mL) significantly inhibited the proliferation, migration and invasion of MDA-MB-231 cells with a dose dependent manner. Moreover, the phosphorylation of PI3K, Akt and mTOR was inhibited by CEO. The results revealed that there was abundant terpenoids in the CEO which account for 63.51 %. CEO significantly inhibited the proliferation, migration and invasion of MDA-MB-231 cells, exhibiting antitumor effect on TNBC. The antitumor effect of CEO might attribute to its inhibition on PI3K/Akt/mTOR signaling pathway. However, further study should be conducted in more TNBC cell lines and animal models to provide further evidence for TNBC treatment by CEO.
The active compounds isolated from Black pepper have anticancer effects, but the bioactivity of Black pepper essential oil (BP‐EO) is rarely studied. BP‐EO has poor stability and a suitable dose form should be prepared for in vivo delivery. Triple negative breast cancer (TNBC) has attracted more and more attention due to its high mitotic index, high metastasis rate and poor prognosis. In this study, the composition of BP‐EO was analyzed by gas chromatography–mass spectrometry (GC–MS), and nanoparticles (NPs) loaded with BP‐EO were prepared by nanoprecipitation method using Eudragit L100 as a carrier. We investigated the preparation, characterization, stability and in vitro release of nanoparticles. MTT assay, cell wound healing, Transwell invasion assay and Western blot were used to study the anti‐tumor effect and mechanism of MDA‐MB‐231 cells. The GC–MS analysis identified a total of 33 compounds among which alkenes account for 63.55%. The prepared BP‐EO NPs exhibited nanoscale morphology, good stability and pH‐responsive and sustained release character which is suitable for in vivo delivery. BP‐EO NPs significantly inhibited the proliferation, migration and invasion of MDA‐MB‐231 cells. Furthermore, BP‐EO NPs significantly inhibited the expressions of Wnt and β‐catenin and significantly activated the expression of GSK‐3β in MDA‐MB‐231 cells. Therefore, BP‐EO NPs prepared in this study provide a new effective strategy for the treatment of TNBC. Practical applications Black pepper is rich in essential oil and has excellent antioxidant and antibacterial activities. However, the anti‐tumor activity of BP‐EO has not been studied. In this study, we found that BP‐EO has excellent anticancer activity. To achieve effective encapsulation of black pepper essential oil and an excellent anti‐triple negative breast cancer activity, nanoparticles loaded with BP‐EO were prepared using Eudragit L100 as the carrier by the nanoprecipitation method. The in vitro study revealed that BP‐EO NPs inhibited proliferation, migration and invasion of MDA‐MB‐231 cells via inhibiting the Wnt/β‐Catenin signaling pathway. This study provides new ideas and innovations for the treatment of invasive triple negative breast cancer in the future. At the same time, we will further reveal the application potential, pharmacokinetic characteristics and precise mechanism of BP‐EO NPs in vivo in subsequent studies.
Background: BRD4 is a member of the bromodomain and extra terminal domain (BET) family of proteins, containing two bromodomains and one extra terminal domain, and is overexpressed in several human malignancies. However, its expression in gastric cancer has not yet been well illustrated. Objective: This study aimed to elucidate the overexpression of BRD4 in gastric cancer and its clinical significance as a novel therapeutic target. Methods: Fresh gastric cancer tissues and paraffin-embedded specimens of gastric cancer patients were collected, and the BRD4 expression was examined by Western Blot Analysis (WB) and Immunohistochemistry Analysis (IHC), respectively. The possible relationship between BRD4 expression and the clinicopathological features as well as survival in gastric cancer patients was analyzed. The effect of BRD4 silencing on human gastric cancer cell lines was investigated by MTT assay, WB, wound healing assay, and Transwell invasion. Results: The results showed that the expression level in tumor tissues and adjacent tissues was significantly higher than that in normal tissues, respectively (P<0.01). BRD4 expression level in gastric cancer tissues was strongly correlated with the degree of tumor differentiated degree (P=0.033), regional lymph nodes metastasis (P=0.038), clinical staging (P=0.002), and survival situation (P=0.000), while the gender (P=0.564), age (P=0.926) and infiltrating depth (P=0.619) of patients were not associated. Increased BRD4 expression resulted in poor overall survival (p=0.003). In in vitro assays, BRD4 small interfering RNA resulted in significantly decreased BRD4 protein expression, therefore inhibiting proliferation, migration, and invasion of gastric cancer cells. Conclusion: BRD4 might be a novel biomarker for the early diagnosis, prognosis, and therapeutic target in gastric cancer.
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