• Title/Summary/Keyword: piperine

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Syntheses and Central Nervous Depressant Activities of Piperine Derivatives (V) (피페린 유도체의 합성 및 중추 억제작용에 관한 연구(V) -Methylenedioxyphenylalkenoic Acid Amide 유도체-)

  • 도경삼;임중기;우경식;이은방
    • YAKHAK HOEJI
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    • v.30 no.4
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    • pp.163-168
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    • 1986
  • Thirteen compounds were synthesized by condensing the N-heterocyclic amines (piperidine, pyrrolidine, morpholine) and secondary aliphatic amines (dimethylamine, diethylamine) with 3,4-methylenedioxyphenylalkenoic acid chlorides for developing CNS depressants. Among them, N, N-diethyl-3,4-methylenedioxycinnamamide (IX) and N, N-dimethyl-5-(3,4-methylenedioxyphenyl)-2, 4-pentadienoic acid amicle (XII) exhibited strong activity in antagonism against pentylenetetrazole-induced convulsion, strychnine-induced convulsion and maximal electroshock seizure. N, N-Dimethyl-3, 4-methylenedioxycinnamide (VIII) showed more potent activity in antagonism against strychnine-induced convulsion and maximal electroshock seizure and in the prolongation of hexobarbital sleeping time.

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Syntheses and Central Nervous Depressant Activities of Piperine Derivatives (II) Piperic Acid Amides (Piperine유도체의 합성 및 중추억제작용에 관한 연구(II) Piperic Acid Amide 유도체)

  • 은재순;임중기;김완주;우원식;이은방
    • YAKHAK HOEJI
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    • v.27 no.4
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    • pp.283-287
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    • 1983
  • In order to search more active and less toxic central nervous depressants, piperic acid amides were synthesized by condensation of piperonal with crotonic acid amides. The bioassay results revealed that, among the compounds synthesized, the piperonic acid methylamide and ethylamide exhibited potent protective activity against strychnine-induced convulsion.

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Piperoctadecalindine, a New Piperidine Alkaloid from Piper retrofractum Fruits

  • Ahn Jong Woong;Lee Chong Ock;Kim Eun Joo;Zee Ok Pyo;Kim Hyung Jin
    • Bulletin of the Korean Chemical Society
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    • v.13 no.4
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    • pp.388-391
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    • 1992
  • A chemical investigation of the fruits of Piper retrofractum (Piperaceae) has led to the isolation and characterization of a novel piperidine alkaloid, piperoctadecalidine together with three known alkaloids piperine, pipernonaline and guineensine. The structure of the new compound was detemined to be (2E,4E,14Z)-N-(2,4,14-Octadecatrienoyl) piperidine by spectral and synthetic methods.

Fermentative Production of White Pepper Using Indigenous Bacterial Isolates

  • Thankamani Vaidyanatha Lyer;Giridhar Raghavan Nair
    • Biotechnology and Bioprocess Engineering:BBE
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    • v.9 no.6
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    • pp.435-439
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    • 2004
  • Three Bacillus strains were isolated from soil samples. Morphological and physiologi­cal characterization indicated that the isolated strains were B. mycoides, B. licheniformis and B. brevis. White pepper was produced from black pepper by the fermentative method using the isolates in shake flaks as well as in a large-scale fermenter. Volatile oil and piperine contents of the product were $3.2\%$ (v/w) and $4\%$ (v/w) respectively. The moisture content was $15\%$. The mi­crobial contamination was less than 10 per 100 g. The product also exhibited excellent storage stability.

Pharmacodynamic and pharmacokinetic interactions between herbs andwestern drugs

  • Lee, Ju-Young
    • Advances in Traditional Medicine
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    • v.8 no.3
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    • pp.207-214
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    • 2008
  • In recent years, the combined use of Herbal medicines and Western drugs has been increasing. Though certain problems may occur when both types of medicines are taken together, they havenot been adequately analyzed. It was reported that anticoagulation was enhanced in addition tobleeding when patients took long-term warfarin therapy in combination with Salvia miltiorrhiza(danshen), and laxative herbs accelerate intestinal transit and interfere with the absorption. Herbal constituents, curcumin, ginsenosides, piperine, catechins and silymarin were found to beinhibitors of P-glycoprotein. St John's wort induces the intestinal expression of P-glycoprotein. Anthraquinone, quercetin and coumarins were found to be a potent inhibitor of P-450. Glycyrrhizin or liquorice extracts, Garlic and St John's wort are a potent inducer of CYP3A4. This review provides a critical overview of interactions between herbal medicines and other drugs. Hence, it is necessary to study the pharmacodynamic and pharmacokinetic interactions of many herbal medicines between western drugs.

Inhibitory Effect of a Drug Metabolizing Enzyme CYP3A4 on Spices (향신료의 약물대사효소 CYP3A4 저해효과)

  • Cha, Bae-Cheon
    • Korean Journal of Pharmacognosy
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    • v.34 no.1 s.132
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    • pp.86-90
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    • 2003
  • For the determination of inhibiting cytochrome P450(CYP)3A4 activity, an improvement HPLC method was established by using a new internal standard and solvent system. Moreover, CYP3A4 amount for a optimum reaction of enzyme was determined by a comparative study with a variety concentration of enzyme. Using a established method, inhibitory effect of CYP3A4 that is drug metabolizing enzyme Investigated on EtOAc extracts of 5-class spices. As a result of experiment, EtOAc extract of white pepper (Piper nigrum L.) showed strong inhibitory activity. On a continuous experiment, the fraction 2, 4 and 5 of while pepper extract showed remarkable inhibitory activity. Pipeline, a main constituent of pepper was not included in these fraction. It is suggested that major compounds for the inhibitory activity of white pepper may be other ingredient that is not piperine.

Inhibition of Aflatoxin $B_1$ Biosynthesis by Piperlongumine Isolated from Piper longum L.

  • Lee, Sung-Eun;Mahoney, Noreen-E.;Campbell Bruce-C.
    • 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.

Active Phytochemicals of Indian Spices Target Leading Proteins Involved in Breast Cancer: An in Silico Study

  • Ashok Kumar Krishnakumar;Jayanthi Malaiyandi;Pavatharani Muralidharan;Arvind Rehalia;Anami Ahuja;Vidhya Duraisamy;Usha Agrawal;Anjani Kumar Singh;Himanshu Narayan, Singh;Vishnu Swarup
    • Journal of the Korean Chemical Society
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    • v.68 no.3
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    • pp.151-159
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    • 2024
  • Indian spices are well known for their numerous health benefits, flavour, taste, and colour. Recent Advancements in chemical technology have led to better extraction and identification of bioactive molecules (phytochemicals) from spices. The therapeutic effects of spices against diabetes, cardiac problems, and various cancers has been well established. The present in silico study aims to investigate the binding affinity of 29 phytochemicals from 11 Indian spices with two prominent proteins, BCL3 and CXCL10 involved in invasiveness and bone metastasis of breast cancer. The three-dimensional structures of 29 phytochemicals were extracted from PubChem database. Protein Data Bank was used to retrieve the 3D structures of BCL3 and CXCL10 proteins. The drug-likeness and other properties of compounds were analysed by ADME and Lipinski rule of five (RO5). All computational simulations were carried out using Autodock 4.0 on Windows platform. The proteins were set to be rigid and compounds were kept free to rotate. In-silico study demonstrated a strong complex formation (positive binding constants and negative binding energy ΔG) between all phytochemicals and target proteins. However, piperine and sesamolin demonstrated high binding constants with BCL3 (50.681 × 103 mol-1, 137.76 × 103 mol-1) and CXCL10 (98.71 × 103 mol-1, 861.7 × 103 mol-1), respectively. The potential of these two phytochemicals as a drug candidate was highlighted by their binding energy of -6.5 kcal mol-1, -7.1 kcal mol-1 with BCL3 and -6.9 kcal mol-1, -8.2 kcal mol-1 with CXCL10, respectively coupled with their favourable drug likeliness and pharmacokinetics properties. These findings underscore the potential of piperine and sesamolin as drug candidates for inhibiting invasiveness and regulating breast cancer metastasis. However, further validation through in vitro and in vivo studies is necessary to confirm the in silico results and evaluate their clinical potential.