Polyphyllin G

Phytomedicine. 2016 Dec 1;23(13):1545-1554.

Polyphyllin G induces apoptosis and autophagy cell death in human oral cancer cells.[Pubmed: 27823618]

Polyphyllin G (also called polyphyllin VII), extract from rhizomes of Paris yunnanensis Franch, has been shown to have strong anticancer activities in a wide variety of human cancer cell lines. However, the underlying influences of autophagy in human oral squamous cell carcinoma (OSCC) remain unclear.
METHODS AND RESULTS:
In this study, the roles of apoptosis and autophagy in Polyphyllin G-induced death in human oral cancer cells were investigated. Moreover, the molecular mechanism of the anticancer effects of Polyphyllin G in human oral cancer cells was investigated. The results revealed that Polyphyllin G significantly inhibited cell proliferation in human oral cancer cells; it dose-dependently induced apoptosis in SAS and OECM-1 cells through caspase-3, -8, and -9 activation and poly (ADP-ribose) polymerase cleavage. In addition, changes were observed in Bcl-2 and proapoptosis-related protein expression in different human oral cancer cell lines. The expression of both LC3-II and beclin-1 was markedly increased, suggesting the induction of autophagy in Polyphyllin G-treated oral cells. To further clarify whether Polyphyllin G-induced apoptosis and autophagy depended on Akt/extracellular signal-regulated kinases (ERK)/c-Jun N-terminal kinases (JNK)/p38 mitogen-activated protein kinases (MAPK) signaling pathways, the cells were cotreated with inhibitors. The results demonstrated Polyphyllin G-induced apoptosis in oral cells through the activation of ERK, Akt, p38 MAPK, and JNK, whereas ERK and JNK accounted for Polyphyllin G-induced autophagy.
CONCLUSIONS:
This study is the first to demonstrate apoptosis and autophagy during Polyphyllin G-induced cell death in human oral cancer cell lines. These results suggest that Polyphyllin G is a promising candidate for developing antitumor drugs targeting human oral squamous cell carcinoma.

Arch Biochem Biophys . 2018 Apr 15;644:93-99.

Polyphyllin G exhibits antimicrobial activity and exerts anticancer effects on human oral cancer OECM-1 cells by triggering G2/M cell cycle arrest by inactivating cdc25C-cdc2[Pubmed: 29352966]

Abstract Plant natural products have long been considered to be important sources of bioactive molecules. A large number of antimicrobial and anticancer agents have been isolated form plants. In the present study we evaluated the antimicrobial and anticancer activity of a plant derived secondery metabolite, Polyphyllin G. The results of antibacterial assays showed that Polyphyllin G prevented the growth of both Gram-positive and Gram-negative bacteria with minimum inhibitory concentrations (MICs) ranging from 13.1 to 78 μg/ml. Antifungal activity measured as inhibition of mycelium growth ranged between 38.32 and 56.50%. Further Polyphyllin G was also evaluated against a panel of cancer cell lines. The IC50 of Polyphyllin G ranged from 10 to 65 μM. However the IC50 of Polyphyllin G was found to be comparatively high (120 μM) against the normal FR2 cancer cell line. The lowest IC50 of 10 μM was found against the oral cancer cell line OECM-1. Therefore further studies were carried out on this cell line only. Our results indicated that Polyphyllin G induced cell arrest in oral cancer OECM-1 cells by inactivation of cdc25C-cdc22 via ATM-Chk 1/2 stimulation. Therefore, we propose that Polyphyllin G might prove a lead molecule in the management of oral cancers and at the same time may prevent the growth of opportunistic microbes. Keywords: Anticancer; Antimicrobial; Cell cycle arrest; Metastasis; Oral cancer; Polyphyllin G.

Parasitology. 2013 Jul;140(8):952-8.

Identification of compounds from Paris polyphylla (ChongLou) active against Dactylogyrus intermedius.[Pubmed: 23552446]

The present study was designated to ascertain the anthelmintic activity of the rhizomes of Paris polyphylla and to isolate and characterize the active constituents.
METHODS AND RESULTS:
The methanol extract from rhizomes of P. polyphylla showed significant anthelmintic activity against Dactylogyrus intermedius with the median effective concentration (EC50) 22.5 mg L(-1). Based on this finding, the methanol extract was fractionated by silica gel column chromatography in a bioassay-guided fractionation yielding 2 bioactive compounds, the structures of these compounds were elucidated as formosanin C and polyphyllin VII(Polyphyllin G). The in vivo tests revealed that formosanin C and polyphyllin VII were significantly effective against D. intermedius with EC50 values of 0.6 and 1.2 mg L(-1), respectively. The acute toxicities (LC50) of formosanin C and polyphyllin VII for grass carp were 2.8 and 2.9 mg L(-1), respectively.
CONCLUSIONS:
The overall results provide important information for the potential application of formosanin C and polyphyllin VII in the therapy of serious infection caused by D. intermedius.

Biomed Chromatogr. 2013 Mar;27(3):343-8

Simultaneous determination and pharmacokinetic study of polyphyllin I, polyphyllin II, polyphyllin VI and polyphyllin VII (Polyphyllin G) in beagle dog plasma after oral administration of Rhizoma Paridis extracts by LC-MS-MS.[Pubmed: 22903625]

For the first time, a rapid and specific LC-MS-MS method has been developed for the analysis of polyphyllin I, polyphyllin II, polyphyllin VI and polyphyllin VII(Polyphyllin G) in beagle dog plasma.
METHODS AND RESULTS:
The method was applied to study the pharmacokinetics of Rhizoma Paridis extracts containing polyphyllin I, polyphyllin II, polyphyllin VI and polyphyllin VII. The analysis was carried out on an Agilent Zorbax XDB-C(18) reversed-phase column (100 × 2.1 mm, 1.8 μm) by isocratic elution with acetonitrile and water (50:50, v/v). The flow rate was 0.25 mL/min. All analytes including internal standards were monitored by selected reaction monitoring with an electrospray ionization source. Linear responses were obtained for polyphyllin I, polyphyllin II, polyphyllin VI and polyphyllin VII ranging from 10 to 5000 ng/mL. The intra-and inter-day precisions (RSDs) were less than 6.66 and 9.15%. The extraction recovery ranged from 95.53 to 104.21% with RSD less than 8.69%. Stability studies showed that polyphyllin I, polyphyllin II, polyphyllin VI and polyphyllin VII were stable in preparation and analytical process.
CONCLUSIONS:
The validated method was successfully used to determine the concentration-time profiles of polyphyllin I, polyphyllin II, polyphyllin VI and polyphyllin VII.