Niranthin | CAS:50656-77-4 | Manufacturer ChemFaces

Niranthin

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Description:

Niranthin is a potent anti-leishmanial agent, inhibits the relaxation activity of heterodimeric type IB topoisomerase of L. donovani and acts as a non-competitive inhibitor interacting with both subunits of the enzyme. Niranthin also exhibits anti-hepatitis B virus, antiinflammatory and antiallodynic actions.

Targets:

HBV | Topoisomerase | PAFR | Antifection

In vitro:

J Ethnopharmacol. 2014 Sep 11;155(2):1061-7.

In vitro and in vivo anti-hepatitis B virus activities of the lignan niranthin isolated from Phyllanthus niruri L.[Pubmed: 25009077]

This study was designed to evaluate the anti-hepatitis B virus activity of Niranthin using HepG2.2.15 cells and duck hepatitis B virus (DHBV) infected ducks as in vitro and in vivo models.
METHODS AND RESULTS:
: Niranthin was isolated from Phyllanthus niruri L. (Euphorbiaceae) by extraction and chromatographic procedures and the anti-hepatitis B virus activity was evaluated both in vitro and in vivo. The human HBV-transfected liver cell line HepG2.2.15 was used in vitro assay. And the in vivo anti-hepatitis B virus activity was evaluated on the expression of HBV replication, HBsAg, HBeAg, ALT and AST on day 0, 7, 14, 17 after Niranthin was dosed intragastricly (i.g.) once a day for 14 days at the dosages of 25, 50 and 100 mg/kg/day in the duck hepatitis B virus (DHBV) infected ducks. In the human HBV-transfected liver cell line HepG2.2.15, the secretion of HBsAg and HBeAg were significantly decreased after treatment with Niranthin for 144 h, with IC50 values for HBsAg of 15.6 µM, IC50 values for HBeAg of 25.1 µM. In DHBV-infected ducklings, Niranthin significantly reduced the serum DHBV DNA, HBsAg, HBeAg, ALT and AST. Furthermore, analysis of the liver pathological changes confirmed the hepatoprotective effect of Niranthin.
CONCLUSIONS:
The experimental data demonstrated that Niranthin exhibits anti-hepatitis B virus activity both in vitro and in vivo. values for HBsAg of 15.6 µM, IC50 values for HBeAg of 25.1 µM. In DHBV-infected ducklings, Niranthin significantly reduced the serum DHBV DNA, HBsAg, HBeAg, ALT and AST. Furthermore, analysis of the liver pathological changes confirmed the hepatoprotective effect of Niranthin. CONCLUSION: The experimental data demonstrated that Niranthin exhibits anti-hepatitis B virus activity both in vitro and in vivo.

In vivo:

EMBO Mol Med. 2012 Oct;4(10):1126-43.

The lignan niranthin poisons Leishmania donovani topoisomerase IB and favours a Th1 immune response in mice.[Pubmed: 23027614]

Niranthin, a lignan isolated from the aerial parts of the plant Phyllanthus amarus, exhibits a wide spectrum of pharmacological activities.
METHODS AND RESULTS:
In the present study, we have shown for the first time that Niranthin is a potent anti-leishmanial agent. The compound induces topoisomerase I-mediated DNA-protein adduct formation inside Leishmania cells and triggers apoptosis by activation of cellular nucleases. We also show that Niranthin inhibits the relaxation activity of heterodimeric type IB topoisomerase of L. donovani and acts as a non-competitive inhibitor interacting with both subunits of the enzyme. Niranthin interacts with DNA-protein binary complexes and thus stabilizes the 'cleavable complex' formation and subsequently inhibits the religation of cleaved strand. The compound inhibits the proliferation of Leishmania amastigotes in infected cultured murine macrophages with limited cytotoxicity to the host cells and is effective against antimony-resistant Leishmania parasites by modulating upregulated P-glycoprotein on host macrophages. Importantly, besides its in vitro efficacy, Niranthin treatment leads to a switch from a Th2- to a Th1-type immune response in infected BALB/c mice. The immune response causes production of nitric oxide, which results in almost complete clearance of the liver and splenic parasite burden after intraperitoneal or intramuscular administration of the drug.
CONCLUSIONS:
These findings can be exploited to develop Niranthin as a new drug candidate against drug-resistant leishmaniasis.

Niranthin Description

Source:	The herbs of Phyllanthus amarus
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Storage:	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. Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com
After receiving:	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.

Animal Research:

Eur J Pharmacol. 2006 Sep 28;546(1-3):182-8.

Antiinflammatory and antiallodynic actions of the lignan niranthin isolated from Phyllanthus amarus. Evidence for interaction with platelet activating factor receptor.[Pubmed: 16925995]

METHODS AND RESULTS:
The local administration of nirtetralin, phyltetralin or Niranthin (30 nmol/paw), similar to WEB2170 (a PAF receptor antagonist, 30 nmol/paw), significantly inhibited PAF-induced paw oedema formation in mice. The extracts of P. amarus (100 microg/ml) and Niranthin (30 microM), but not nirtetralin or phyltetralin (30 microM), decreased the specific binding of [(3)H]-PAF in mouse cerebral cortex membranes. Furthermore, both Niranthin and WEB2170 displaced, in a concentration-dependent manner, the [(3)H]-PAF binding sites. The mean IC(50) values from these effects were 6.5 microM and 0.3 microM, respectively. Additionally, both Niranthin and WEB2170 (30 nmol/paw) inhibited the increase of myeloperoxidase activity induced by PAF injection in the mouse paw. When assessed the mouse model of pleurisy induced by PAF, pretreatment with Niranthin (100 micromol/kg, p.o.) or WEB2170 (1.7 micromol/kg, i.p.) significantly inhibited PAF-induced protein extravasations. Moreover, in the rat model of PAF-induced allodynia, both Niranthin (30 nmol/paw) and WEB2170 (30 nmol/paw) treatment significantly inhibited PAF-induced allodynia. In addition, Niranthin had a rapid onset and long-lasting antiallodynic action when compared with WEB2170.
CONCLUSIONS:
Collectively, the present findings suggest that Niranthin exhibits antiinflammatory and antiallodynic actions which are probably mediated through its direct antagonistic action on the PAF receptor binding sites.

Product Name	Niranthin
Price:	$318 / 5mg
CAS No.:	50656-77-4
Catalog No.:	CFN98798
Molecular Formula:	C₂₄H₃₂O₇
Molecular Weight:	432.5 g/mol
Purity:	>=98%
Type of Compound:	Lignans
Physical Desc.:	Powder
Source:	The herbs of Phyllanthus amarus
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Download:	COA MSDS SDF Manual
Similar structural:	Comparison (Web) (SDF)
Guestbook:

Size /Price /Stock	10 mM * 100 uL in DMSO / Inquiry / In-stock 10 mM * 1 mL in DMSO / Inquiry / In-stock
Related Libraries	Anti-inflammatory Compound Library Antiviral Compound Library Analgesia Compound Library Anti-leishmanial Compound Library Lignans Compound Library Topoisomerase Inhibitor Library PAFR Inhibitor Library HBV Inhibitor Library Antifection Inhibitor Library

	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	2.3121 mL	11.5607 mL	23.1214 mL	46.2428 mL	57.8035 mL
5 mM	0.4624 mL	2.3121 mL	4.6243 mL	9.2486 mL	11.5607 mL
10 mM	0.2312 mL	1.1561 mL	2.3121 mL	4.6243 mL	5.7803 mL
50 mM	0.0462 mL	0.2312 mL	0.4624 mL	0.9249 mL	1.1561 mL
100 mM	0.0231 mL	0.1156 mL	0.2312 mL	0.4624 mL	0.578 mL

CFN99050	Phyllanthin	10351-88-9	418.5	C₂₄H₃₄O₆
CFN98798	Niranthin	50656-77-4	432.5	C₂₄H₃₂O₇
CFN99046	Dehydroheliobuphthalmin	103001-05-4	412.4	C₂₂H₂₀O₈
CFN97133	Dihydroguaiaretic acid	66322-34-7	330.4	C₂₀H₂₆O₄
CFN98539	Anwulignan	107534-93-0	328.41	C₂₀H₂₄O₄
CFN95501	erythro-Austrobailignan-6	114127-24-1	328.4	C₂₀H₂₄O₄
CFN92717	Schineolignin B	1352185-26-2	374.5	C₂₂H₃₀O₅
CFN95245	Sphenanlignan	866347-36-6	358.4	C₂₁H₂₆O₅
CFN95221	Arisanschinin E	1333378-33-8	360.5	C₂₁H₂₈O₅
CFN96694	Pregomisin	66280-26-0	390.47	C₂₂H₃₀O₆