Phytochemicals and Estrogen-Receptor Agonists from the Aerial Parts of Liriope platyphylla.

One new benzofuran, (2R)-(2',4'-dihydroxybenzyl)-6,7-methylenedioxy-2,3-dihydrobenzofuran (1), one new phenylisocoumarin, 3-(2'-hydroxyphenyl)-6,8-dihydroxy-7-methoxy-isocoumarin (2), and one new benzofuroisocoumarin, platyphyllarin C (3), were isolated from the ethanolic extract of Liriope platyphylla aerial parts, along with seventeen known compounds. The structures of the isolates were established by spectroscopic analysis and comparison with the literature data. The results indicated that structures 1-3 are uncommon in Nature. Benzofuroisocoumarin 4, flavonoids 9, 10, and 13-15, and homoisoflavonoids 19 and 20 exhibited significant binding activity to estrogen-receptor α and/or ß as demonstrated by the SEAP reporter assay system in an MCF-7 cell-line.

Classification of lung cancer subtypes based on autofluorescence bronchoscopic pattern recognition: A preliminary study.

BACKGROUND AND OBJECTIVES: Lung cancer is the leading cause of cancer deaths worldwide. With current use of autofluorescent bronchoscopic imaging to detect early lung cancer and limitations of pathologic examinations, a computer-aided diagnosis (CAD) system based on autofluorescent bronchoscopy was proposed to distinguish different pathological cancer types to achieve objective and consistent diagnoses. METHODS: The collected database consisted of 12 adenocarcinomas and 11 squamous cell carcinomas. The corresponding autofluorescent bronchoscopic images were first transformed to a hue (H), saturation (S), and value (V) color space to obtain better interpretation of the color information. Color textural features were respectively extracted from the H, S, and V channels and combined in a logistic regression classifier to classify malignant types by machine learning. RESULTS: After feature selection, the proposed CAD system achieved an accuracy of 83% (19/23), a sensitivity of 73% (8/11), a specificity of 92% (11/12), a positive predictive value of 89% (8/9), a negative predictive value of 79% (11/14), and an area under the receiver operating characteristic curve of 0.81 for distinguishing lung cancer types. CONCLUSIONS: The proposed CAD system based on color textures of autofluorescent bronchoscopic images provides a diagnostic method of malignant types in clinical use.

Anti-viral effect of a compound isolated from Liriope platyphylla against hepatitis B virus in vitro.

The compound LPRP-Et-97543 was isolated from Liriope platyphylla roots and was observed to have potential anti-viral effects in HepG2.2.15 cells against hepatitis B virus (HBV). The antiviral mode was further clarified, and the HBV-transfected Huh7 cells were used as the platform. During viral gene expression, LPRP-Et-97543 treatment had apparent effects on the viral precore/pregenomic and S/preS RNA. Promoter activity analysis demonstrated that LPRP-Et-97543 significantly reduced Core, S, and preS but not X promoter activities. Further examination showed that putative signaling pathways were involved in this inhibitory effect, indicating that NF-κB may serve a putative mediator of HBV gene regulation with LPRP-Et-97543. In addition, the nuclear expression of p65/p50 NF-κB member proteins was attenuated with LPRP-Et-97543 and augmented cytoplasmic IκBα protein levels but without affecting the expression of these proteins in HBV non-transfected cells during treatment. Moreover, LPRP-Et-97543 reduced the binding activity of NF-κB protein to CS1 element of HBV surface gene in a gel retardation analysis and inhibited CS1 containing promoter activity in HBV expressed cells. However, HBV transfection significantly enhances CS1 containing promoter activity without compound treatment in cells. Finally, transfection of the p65 expression plasmid significantly reversed the inhibitory effect of LPRP-Et-97543 on the replicated HBV DNA level in HBV positive cells. In conclusion, this study suggests that the mechanism of HBV inhibition by LPRP-Et-97543 may involve the feedback regulation of viral gene expression and viral DNA replication by HBV viral proteins, which interferes with the NF-κB signaling pathway.

The oestrogenic and anti-platelet activities of dihydrobenzofuroisocoumarins and homoisoflavonoids from Liriope platyphylla roots.

The ethanolic extract of Liriope platyphylla (Liliaceae) roots showed potential oestrogenic and anti-platelet activities. Twenty-six compounds were isolated and classified as 10 skeletons, including two unusual new dihydrobenzofuroisocoumarins, (+)-platyphyllarin A (1) and B (2), one new butanoate, ethyltributanoate (3), and two new homoisoflavanones, (-)-liriopein A (4) and B (5), along with 21 known compounds, including six homoisoflavonoids, one chalcone, six amides, one lignan, one fatty acid derivative, one alkaloid, three benzenoids, and two steroids. The biosynthetic pathway of compounds 1 and 2 was proposed in the current investigation. The oestrogenic activity of the isolates was evaluated utilising the pER8:GUS reporter assay system in transgenic Arabidopsis plant as well as the SEAP reporter assay system in MCF-7 breast cancer cell-line; the anti-platelet activity was evaluated using the anti-platelet aggregation assay. Several components exhibited significant oestrogenic and anti-platelet activities; demonstrating for the first time the potential use of L. platyphylla as a nutritional supplement for cardiovascular and endocrine diseases.

Active Constituents from Liriope platyphylla Root against Cancer Growth In Vitro.

Liriope spicata is a well-known herb in traditional Chinese medicine, and its root has been clinically demonstrated to be effective in the treatment of metabolic and neural disorders. The constituents isolated from Liriope have also recently been shown to possess anticancer activity, although the mechanism of which remains largely unknown. Here, we illustrate the anticancer activity of LPRP-9, one of the active fractions we fractionated from the Liriope platyphylla root part (LPRP) extract. Treatment with LPRP-9 significantly inhibited proliferation of cancer cell lines MCF-7 and Huh-7 and down-regulated the phosphorylation of AKT. LPRP-9 also activates the stress-activated MPAK, JNK, p38 pathways, the p53 cell-cycle checkpoint pathway, and a series of caspase cascades while downregulating expression of antiapoptotic factors Bcl-2, Bcl-XL, and survivin. Such activities strongly suggest a role for LPRP-9 in apoptosis and autophagy. We further purified and identified the compound (-)-Liriopein B from LPRP-9, which is capable of inhibiting AKT phosphorylation at low concentration. The overall result highlights the anticancer property of LPRP-9, suggests its mechanism for inhibition of proliferation and promotion of cell death for cancer cells via regulation of multitarget pathways, and denotes the importance of purifying components of fraction LPRP-9 to aid cancer therapy.