• Natural Product Sciences
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• v.4 no.1
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• pp.23-25
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• 1998

Two samples of the fruits of Piper longum have been chemically investigated. From one sample a new alkamide, pergumidiene and from other sample two rare alkamides, brachystamide B and piperderdine have been isolated. The known compounds, piperine, piperlonguminine, pellitorine, (+)-sesamine and 3-(3', 4', 5'-trimethoxyphenyl)-propionic acid were the common constituents of both the samples.

• Bulletin of the Korean Chemical Society
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• v.31 no.4
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• pp.921-924
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• 2010

Blocking of IL-6 has been postulated to be an effective therapy in the pathogenesis of several inflammatory diseases. The current study was performed to examine the potential effects of alkamides isolated from P. longum and P. nigrum on IL-6 induced Stat3 activation and identify the structure-activity relationship of these alkamides in human hepatoma cells. Among 10 alkamides isolated from P. longum and P. nigrum, compounds 6, 7 and 9 were identified as strong inhibitors of IL-6 action, which inhibit IL-6 induced Stat3-dependent luciferase activities. These inhibitory activities were positively influenced by the presence of piperidine moiety.

• Microbiology and Biotechnology Letters
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• v.51 no.4
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• pp.432-440
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• 2023

Irrational and injudicious use of antibiotics, easy availability of them as over-the-counter drugs in economically developing countries, and unavailability of regulatory policies governing antimicrobial use in agriculture, animals, and humans, has led to the development of multi-drug resistance (MDR) bacteria. The use of medicinal plants can be considered as an alternative, with a consequent impact on microbial resistance. We tested extracts of Piper longum fruits as new natural products as agents for reversing the resistance to antibiotics. Six crude extracts of P. longum fruits were utilized against a clinical isolate of multidrug-resistant Staphylococcus aureus.The antibiotic susceptibility testing disc method was used in the antibiotic resistance reversal analysis. Apart from cefoxitin and erythromycin, all other antibiotics used (lincosamides [clindamycin], quinolones [levofloxacin and ciprofloxacin], and aminoglycosides [amikacin and gentamicin]) were enhanced by P. longum extracts. The extracts that showed the greatest synergy with the antibiotics were EAPL (ethyl acetate [extract of] P. longum), n-BPL (n-butanol [extract of] P. longum), and MPL (methanolic [extract of] P. longum The results of this study suggest that P. longum extracts have the ability to increase the effectiveness of different classes of antibiotics and reverse their resistance. However, future studies are needed to elucidate the molecular mechanisms behind the synergy between antibiotic and phytocompound(s) and identify the active biomolecules of P. longum responsible for the synergy in S. aureus.

• 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.

• Natural Product Sciences
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• v.13 no.2
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• pp.97-100
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• 2007

The present study includes macro and microscopical details, powder study, physico-chemical study and HPTLC fingerprinting of the Piper longum fruits. Microscopic studies revealed the presence of stone cells, starch grains and thin walled fragments of parenchymatous cells. Physico-chemical studies showed alcohol and ether soluble extract 24.53 and 6.7, sugar 0.35, starch 21.33 and tannin 0.83% respectively. Successive soxhlet extract showed maximum percentage of hexane soluble fraction i.e. 22.52. The HPTLC profile has also been performed against the reference marker pipeline, which was identified at R$_f$ 0.42. In the present paper a detailed pharmacognostical evaluation of fruit has been undertaken.

• 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.

• Journal of Life Science
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• v.19 no.5
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• pp.671-675
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• 2009

Prostate cancer has been a critical health problem due to an increase of prostate cancer-related deaths worldwide. Also, a frequent treatment option for prostate cancer is androgen ablation, but this treatment has a limited scope, especially for hormone-refractory cancer. There is an urgent need for the identification of alternative therapeutic strategies for prostate cancer. Previously, over one hundred species of dried-plant methanol extracts were tested for inhibitory effects on proliferation. One of them, Piper longum Linn. was selected based on its potent anti-proliferation effect. The dried root of P. longum Linn. was extracted with 100% methanol for 2-3 days and its extract was fractionated using chloroform. The chloroform layer was then subjected to column chromatography on silica gel, reverse phase-18 (RP-18) and Sephadex LH-20, in turn. Finally, the pure compound was obtained and identified as pipernonaline by NMR spectroscopic and physico-chemical analysis. In this study, anti-proliferation and cell cycle arrest effects of pipernonaline on human prostate cancer PC-3 cells were investigated using the MTT and PI staining, respectively. Our findings suggest that pipernonaline represents a dose-dependent growth inhibition pattern on PC-3 cells and, moreover, its growth inhibition is associated with sub-G1 and G0/G1 cell cycle accumulation in PC-3 cells. Also, these results provide an anticancer candidate for human prostate cancer.

• 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.

• Advances in Traditional Medicine
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• v.4 no.2
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• pp.95-99
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• 2004

The ethanolic extract of some medicinal plants having anti-asthmatic activity such as Solanum xanthocarpum, Curcuma longa, Glycyrrhiza glabra, Piper longum, A. vasica, A. lebbeck, and Tinospora cordifolia was evaluated for antihistaminic and anti-cataleptic activity. The aqueous solution of ethanolic extract of S. xanthocarpum and G. glabra potentiated histamine-induced tracheal chain contractions. Whereas, C. longa, P. longum, and T. cordifolia, and A. lebbeck were without any significant effect on histamine. Only A. vasica inhibited histamine-induced tracheal chain contraction. G. glabra per se produced contraction of the tracheal chain, which was blocked by pretreatment with atropine. Single dose of S. xanthocarpum potentiated clonidine-induced catalepsy but on repeated doses (once in a day for 3 days) inhibited catalepsy. Pretreatment with ethanolic extract of C. longa, P. longum, T. cordifolia inhibited catalepsy whereas G. glabra and A. lebbeck significantly potentiated clonidine-induced catalepsy. None of the extracts inhibited haloperidol-induced catalepsy. Thus the extracts having antihistaminic activity or mast cell stabilizing activity inhibited clonidineinduced catalepsy.

• International Journal of Oral Biology
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• v.44 no.3
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• pp.89-95
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• 2019

Piperlongumine (PL) is a natural product found in long pepper (Piper longum). The pharmacological effects of PL are well known, and it has been used for pain, hepatoprotection, and asthma in Oriental medicine. No studies have examined the effects of PL on bone tissue or bone-related diseases, including osteoporosis. The current study investigated for the first time the inhibitory effects of PL on osteoclast differentiation, bone resorption, and osteoclastogenesis-related factors in RAW264.7 macrophages stimulated by the receptor activator for nuclear factor-${\kappa}B$ ligand (RANKL). Cytotoxicity was examined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, and osteoclast differentiation and bone resorption were confirmed by tartrate-resistant acid phosphatase (TRAP) staining and pit formation analysis. Osteoclast differentiation factors were confirmed by western blotting. PL exhibited toxicity in RAW264.7 macrophages, inhibiting osteoclast formation and bone resorption, in addition to inhibiting the expression of osteoclastogenesis-related factors, such as tumor necrosis factor receptor-associated factor 6 (TRAF6), c-Fos, and NFATc1, in RANKL-stimulated RAW264.7 macrophages. These findings suggest that PL is suitable for the treatment of osteoporosis, and it serves as a potential therapeutic agent for various bone diseases.