Exploring the in vitro and in vivo anticancer activity of lasiokaurin on nasopharyngeal carcinoma

Objective: To evaluate the anticancer activity of the natural diterpenoid lasiokaurin (LAS) against nasopharyngeal carcinoma (NPC) both in vitro and in vivo, along with investigating its underlying mechanism. Methods: MTT and colony formation assays were used to assess cell viability. Flow cytometry was utilized for the analysis of cell cycle arrest and apoptosis. Additionally, wound healing and transwell invasion assays were conducted separately to investigate cell migration and invasion. To uncover potential targets and pathways of LAS within NPC, a network pharmacological study based on RNA-sequencing (RNA-seq) was performed. Immunoblotting was subsequently used to determine protein levels. Furthermore, the anti-NPC activity of LAS was evaluated in vivo using a xenograft mouse model. Results: Based on in vitro investigations, it is evident that LAS exerted substantial inhibitory effects on NPC cells. Notably, LAS demonstrated significant reductions in cell viability, migration, and invasion capabilities, while simultaneously inducing apoptosis and G2/M cell cycle arrest. Furthermore, LAS suppressed the activation of MAPK, mTOR, STAT3, and NF-κB pathways within NPC cells. Additionally, in vivo experiments underscored LAS's capacity to attenuate NPC tumor growth without eliciting any discernible impact on body weight. Conclusion: Our data clearly demonstrate the anticancer activity of LAS against NPC, both in vitro and in vivo. These findings firmly position LAS as a potential candidate for the treatment of NPC

Assessing the therapeutic potential of Elephantopus scaber extract in hepatocellular carcinoma by inhibiting the PI3K/Akt pathway

Elephantopus scaber, globally acknowledged for its edible and medicinal uses, remains underexplored despite the identification of active compounds. This research explores Elephantopus scaber extract's therapeutic capabilities in hepatocellular carcinoma (HCC). Initial in vitro screenings using the MTT assay revealed that ethanol extract (EEES) inhibited HCC cell proliferation while exhibiting low toxicity to normal cells. Further explorations showed EEES induced cell cycle arrest, apoptosis, and inhibited cell metastasis. A bioinformatics analysis using a network pharmacology approach identified the PI3K/Akt pathway as a key modulation for EEES's anti-HCC activities, validated through western blot analysis. In animal studies, EEES demonstrated the ability to inhibit HCC tumor growth in vivo with a high level of safety. In summary, our research positions Elephantopus scaber as a potent herb with anti-HCC activities and remarkable safety, offering promising prospects for the prevention and treatment of liver diseases, including HCC

In Vitro and In Vivo Anti-Cancer Activity of Lasiokaurin in a Triple-Negative Breast Cancer Model

Due to its intricate heterogeneity, high invasiveness, and poor prognosis, triple-negative breast cancer (TNBC) stands out as the most formidable subtype of breast cancer. At present, chemotherapy remains the prevailing treatment modality for TNBC, primarily due to its lack of estrogen receptors (ERs), progesterone receptors (PRs), and human epidermal growth receptor 2 (HER2). However, clinical chemotherapy for TNBC is marked by its limited efficacy and a pronounced incidence of adverse effects. Consequently, there is a pressing need for novel drugs to treat TNBC. Given the rich repository of diverse natural compounds in traditional Chinese medicine, identifying potential anti-TNBC agents is a viable strategy. This study investigated lasiokaurin (LAS), a natural diterpenoid abundantly present in Isodon plants, revealing its significant anti-TNBC activity both in vitro and in vivo. Notably, LAS treatment induced cell cycle arrest, apoptosis, and DNA damage in TNBC cells, while concurrently inhibiting cell metastasis. In addition, LAS effectively inhibited the activation of the phosphatidylinositol-3-kinase/protein kinase B/mammalian target of rapamycin (PI3K/Akt/mTOR) pathway and signal transducer and activator of transcription 3 (STAT3), thus establishing its potential for multitarget therapy against TNBC. Furthermore, LAS demonstrated its ability to reduce tumor growth in a xenograft mouse model without exerting detrimental effects on the body weight or vital organs, confirming its safe applicability for TNBC treatment. Overall, this study shows that LAS is a potent candidate for treating TNBC

Development of an in-line HPLC fingerprint ion-trap mass spectrometric method for identification and quality control of Radix Scrophulariae

Chromatographic fingerprinting has been widely accepted as a crucial method for qualitative and quantitative analyses of bioactives within traditional Chinese medicine. A fingerprint provides detailed information, specific for any given herb, thus facilitating the quality control measures of a given traditional Chinese medicine. In this article, quality assessment of Radix Scrophulariae was achieved by using high performance liquid chromatography combining diode-array detection and electrospray ionization mass spectrometry (HPLC-DAD-ESI/MS). Eight batches of sample obtained from different origins in China were used to establish the fingerprint and quantitative analyses. By comparing the retention times, UV and MS spectral data with reference standards, four characteristic peaks in the chromatograms were confirmed as corresponding to acetoside, angoroside C, cinnamic acid, and harpagoside. In addition, other two characteristic peaks were tentatively identified, following the literature interpretation of HPLC-ESI-MS and LC-MS/MS (affording structural information) to be sibirioside A and scrophuloside B(4), respectively. The results indicated that the newly developed HPLC-DAD-MS fingerprint method would be suitable for quality control of Radix Scrophulariae. (C) 2011 Elsevier B.V. All rights reserved