• Journal of Microbiology and Biotechnology
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• v.12 no.4
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• pp.679-682
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• 2002

The alkaloids, piperlongumine, piperine, pipernonaline, and piperoctadecalidine, isolated from Piper longum L., were found to inhibit the biosynthesis of aflatoxin $B_1$ (AF$B_1$) in Aspergillus flavus WRRC 3-90-42-12. Piperlongumine was the most active among the compounds tested, with a 96% inhibition of AF$B_1$biosynthesis at 0.2% (w/v) supplement in a potato dextrose agar (PDA) medium. The three other piperidine alkaloids, pipeline, pipernonaline, and piperoctadecalidine, also inhibited the biosynthesis of AF$B_1$. Of these three alkaloids, piperoctadecalidine exhibited a potent inhibitory activity with a 100% inhibition of AF$B_1$ production at 0.7% (w/v) supplement in a PDA medium. Therefore, piperlongumine and piperoctadecalidine could be used as antiaflatoxigenic agents in agricultural industries. To determine the antiaflatoxigenic mode of action of piperlongumine, further studies are needed.

• Advances in Traditional Medicine
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• v.3 no.1
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• pp.8-17
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• 2003

Water extract (kwath) of six different widely used Ayurvedic medicinal plants were tested in mice for possible neuropharmacological efficacy. In the present experiments it was observed that a number of plant tested causes a significant level of Central Nervous System (CNS) depression, in that it significantly decreased the spontaneous Motor activity, and also lowered the exploratory behavior of the treated animals. Terminalia chebula (HAA), Terminalia bellerica (BHA), Emblica officinalis (AA), Piper longum 1. (PP). exhibited depressant action of on the CNS. Apart from them a mild to moderate degree of depression was evident as a consequence of administration of Zingiber officinale Rosc (SUT), Piper nigrum L. (MRC). However, none of the plant tested did not exhibit significant effects on pentobarbital induced narcosis, and this indicated that the sedating effects of the drug was not associated with the risk of fatal consequences on overdose.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.201.1-201.1
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• 2003

Study of Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors from medicinal plants, we found strong inhibitory activity of ACAT enzyme from rat liver microsome by the CHC1$_3$ extract of Piper longum. Bioactivity-guided fractionation led to the isolation of Guineensine (1), its structure was elucidated by spectroscopic (IR, UV, MS and NMR) means. It inhibited ACAT activity in a dose-dependent manner with IC$\sub$50/ values of 1.2 $\mu\textrm{g}$/ml on in vitro assay using rat liver microsome.

• Microbiology and Biotechnology Letters
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• v.41 no.2
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• pp.253-262
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• 2013

In this study, we analyzed the anti-oxidative and anti-inflammatory activities of seven medicinal herbs. All extracts of the tested herbs, Euryale ferox Salisbury, Echinops setifer Iljin, Amomum cardamomum Linne, Tetrapanax papyriferus, Illicium verum Hook. f., Typha orientalis Presl, and Piper longum Linne, exhibited potent anti-oxidative activity as confirmed by DPPH radical scavenging capacity. Lipopolysaccharide (LPS) induced nitric oxide (NO) production, in the RAW 264.7 cell line, was also ameliorated by all extracts' treatments in a dose dependent manner. NO suppressive activity originated from the inhibition of inducible nitric oxide synthase (iNOS) protein expression by the extracts. Three extracts, E. ferox S., I. verum Hook. f., and P. longum L., possessed suppressive activity against, not only iNOS, but also cycloxygenase 2 (COX-2) protein expression. These three extracts may then serve as potential candidates for non steroidal analgesic inflammation drugs (NSAIDs). Furthermore, all extracts induced anti-oxidative enzyme, heme oxygenase 1, protein expression. Taken together, these results provide an important new insight into the fact that various medicinal herbs possess potent anti-oxidative and anti-inflammatory activities and might be utilized as promising agents in the field of health products. Further studies for the identification of the active compounds from medicinal herbs are clearly needed.

• Proceedings of the Korean Society of Food Hygiene and Safety Conference
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• 2003.11a
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• pp.53-57
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• 2003

• Applied Biological Chemistry
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• v.43 no.2
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• pp.141-147
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• 2000

Interrelation between the antioxidative activity of hot-water extracts of 130 medicinal plants and their cellular antimutagenic activity was investigated. Antioxidative activity was evaluated by assaying electron-donation to DPPH free radical and scavenging of hydroxyl radical $({\cdot}OH)$ generated through Fenton rection, respectively. All medicinal plants examined in this study exhibited markedly electron-donating ability and radical scavenging ability in each assay system. The results demonstrated the fact that Pilbal (Piper longum L.) is the strongest in electron-donating activity, on the other hand, that Seokgok (Dendrobium moniliforme L.) is the strongest in ${\cdot}OH$ scavenging activity. When evaluated their antioxidative activities, 24 medicinal plants including Jimo (Anemarrhena asphodeloides Bunge) were found to be the medicinal plants carrying strong antioxidative activity, which exhibited more than 50% activity compared to the control group in both electron-donating and free radical scavenging. The experiment was also performed to examine whether 11 medicinal plants having significant antimutagenicity damage DNA in the presence of $Cu^{2+}$, showing the fact that all samples tested, except Taeksa (Alisma canaliculatum All. Br.), Paekjain (Nitraria sibirica Pall) and Ohyak (Lindera strychifolia Sieb. et Zucc. Villar) are capable of inducing DNA strand break. We also found that Taeksa and Paekjain strongly block DNA strand break induced by chemical mutagen mitomycin C.

• Applied Biological Chemistry
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• v.46 no.4
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• pp.361-366
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• 2003

Anti-aflatoxigenic studies on synthetic pyridione alkaloids were conducted. Seven derivatives using piperlongumine as a leading compound were prepared from 3,4,5-trimethoxycinnamic acid (TMCA). These derivatives were analyzed for their structural confrmation and purity by HPLC, GC, GC/MS and $1^H-NMR$. 1-piperidin-1-yl-3-(3,4,5-trimethoxyphenyl)propenone (1) reaction with piperidine; 1-morpholin-4-yl-3-(3,4,5-trimethoypenyl)propenone (2) with morpholine; 1-(3,5-dimethylpiperidin-1-yl)-3-(3,4,5-trimethoxyphenyl)propenone (3) with 3,5-dimethylpiperdine; 1-(2-methylpiperidine-1-yl)-3-(3,4,5-trimethoxyphenyl)propenone (4) with 2-methylpiperidine; 1-(3-hydroxypiperidin-1-yl)-3- (3,4,5-trimethoxyphenyl)propenone (5) with 3-hydroxypiperidine hydrochloride; 1-[3- (3,4,5-trimethoxyphenyl)acryloyl]piperidin-2-one (6) with ${\delta}-valerolactam;\; and\;ethyl\;1-[3-(3,4,5-trimethoxyphenyl)acyloyl]piperidine-4-carboxylate$ (7) with ethyl isonipectotate were synthesized respectively. All derivatives showed an inhibitory activity on aflatoxin $B_1$ production. In conclusion, we believe that they might be an agent for the control of mycotoxin in agricultural commodities.

• Journal of the Korean Society of Food Science and Nutrition
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• v.45 no.11
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• pp.1589-1594
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• 2016

Piperine [(E,E)-5-(3,4-methtylenedioxyphenyl)-2,4-pentadienolypiperidide] is a principal of Piperaceae, including Piper nigrum L. and Piper longum Linn., which has been used as a spice and traditional medicine. In this study, we investigated whether or not piperine has anti-cancer effects on AGS human gastric cancer cells. The results demonstrated that piperine not only inhibited proliferation using MTT assay but also induced apoptotic bodies using DAPI assay in a dose-dependent manner in response to piperine. Expression levels of p53, Bax (pro-apoptotic), cleaved caspase-9, and cleaved-PARP increased, whereas expression levels of Bcl-2, XIAP (anti-apoptotic), and Akt decreased in a dose-dependent manner compared with the control by western blotting analysis. To identify the connection between phospo-Akt and Bcl-2 family in response to piperine, LY249002 (Akt inhibitor) was treated with piperine ($150{\mu}M$). The results were shown that expression of phospo-Akt was reduced whereas expression of Bax and cleaved-PARP increased in a dose-dependent manner. These results indicate that piperine induced apoptosis in AGS cells and may serve as a chemopreventive or therapeutic agent for human gastric cancer.