Diphyllin
Diphyllin could be characterized as a new V-ATPase inhibitor in treating gastric cancer and inhibiting the phosphorylation of LRP6 in Wnt/β-catenin signaling. Diphyllin has anti-inflammatory activities, it shows 50% inhibition of NO production from peritoneal macrophages. Diphyllin also has in vitro antileishmanial activity, it exerts a strong specific inhibitory activity (IC50 = 0.2 microM) resulting from the inhibition of parasite internalization within macrophages.
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Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to
24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
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J Ethnopharmacol. 2006 Jan 16;103(2):181-6.
Anti-inflammatory activities of constituents isolated from Phyllanthus polyphyllus.[Pubmed:
16169167 ]
Four compounds, including one benzenoid, 4-O-methylgallic acid (1), together with three arylnaphthalide lignans, namely phyllamyricin C (2), justicidin B (3) and Diphyllin (4) were isolated from the whole plants of Phyllanthus polyphyllus L. (Euphorbiaceae). This was the first isolation report of compounds 1-4 from this plant species.
METHODS AND RESULTS:
The in vitro inhibitory effects of these compounds were evaluated on the production of nitric oxide (NO) and cytokines (tumor necrosis factor (TNF)-alpha and interleukin (IL)-12), from LPS/IFN-gamma activated murine peritoneal macrophages. The results indicated that the 50% inhibition concentration (IC(50)) values of NO production from activated peritoneal macrophages by compounds 1-4 were 100, 25, 12.5 and 50 microM, respectively. In parallel, these dilutions were approximately inhibited in a similar manner to that observed for cytokines (TNF-alpha, and IL-12) production. On the other hand, at 100 microM concentration compounds 3 and 4 showed 50% inhibition of NO production from peritoneal macrophages that had been pre-activated with LPS/IFN-gamma for 24h, whereas compounds 1 and 2 inhibited only about 20 and 10%, respectively.
CONCLUSIONS:
These results support the use of this plant for the treatment of inflammatory diseases in oriental traditional medicine.
Eur J Pharmacol. 2011 Sep 30;667(1-3):330-8.
Effects of diphyllin as a novel V-ATPase inhibitor on gastric adenocarcinoma.[Pubmed:
21645513]
The natural compound Diphyllin, a cytostatic lignan isolated from Cleistanthus collinus, can dramatically inhibit the proliferation and induce the apoptosis of human gastric cancer cells, SGC7901.
METHODS AND RESULTS:
Our study found that Diphyllin can inhibit the expression of V-ATPases in a dose-dependent manner, decrease the internal pH (pHi) and reverse the transmembrane pH gradient in SGC7901 cells. Changes of the pH gradient were positively correlated with Diphyllin concentration. Further study found that Diphyllin treatment caused a decrease in phospho-LRP6, but not in LRP6. β-catenin in Wnt/β-catenin signaling and its target genes, c-myc and cyclin-D1, were also decreased with the inhibition of V-ATPases.
CONCLUSIONS:
Therefore, Diphyllin could be characterized as a new V-ATPase inhibitor in treating gastric cancer and inhibiting the phosphorylation of LRP6 in Wnt/β-catenin signaling.
