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PubMed2005

Piperine from the fruits of Piper longum with inhibitory effect on monoamine oxidase and antidepressant-like activity.

A bioassay-guided isolation of the ethanol extract from the fruits of Piper longum yielded a known piperidine alkaloid, piperine, as a monoamine oxidase (MAO) inhibitor. Piperine showed an inhibitory effect against MAO-A (IC50 value: 20.9 microM) and MAO-B (IC50 value: 7.0 microM). Kinetic analyses by a Lineweaver-Burk plot clearly indicated that piperine competitively inhibited MAO-A and MAO-B with Ki values of 19.0+/-0.9 microM and 3.19+/-0.5 microM, respectively. The inhibition by piperine was found to be reversible by dialysis of the incubation mixture. In addition, the immobility times in the tail suspension test were significantly reduced by piperine, similar to that of the reference antidepressant fluoxetine, without accompanying changes in ambulation when assessed in an open-field. These results suggest that piperine possesses potent antidepressant-like properties that are mediated in part through the inhibition of MAO activity, and therefore represent a promising pharmacotherapeutic candidate as an antidepressant agent.

Alkaloids↗
PubMed2006

Chemical constituents of the roots of Piper sarmentosum.

Sixteen compounds were isolated from the fresh roots of Piper sarmentosum. Seven of these have been previously isolated from the fruits and leaves of this plant: the aromatic alkene (1), 1-allyl-2-methoxy-4,5-methylenedioxybenzene (4), beta-sitosterol, pyrrole amide (6), sarmentine (10), sarmentosine (13) and pellitorine (14). (+)-Sesamin (2), horsfieldin (3), two pyrrolidine amides 11 and 12, guineensine (15) and brachystamide B (16) are new for P. sarmentosum. Sarmentamide A, B, and C (7-9) are new natural products. Compounds 1--4 and 6--16 were tested for antiplasmodial, antimycobacterial and antifungal activities.

Animals↗
PubMed2005

Radioprotective property of the ethanolic extract of Piper betel Leaf.

The radioprotective activity of Piper betel ethanolic extract (PE) has been studied using rat liver mitochondria and pBR 322 plasmid DNA as two model in vitro systems. The extract effectively prevented gamma-ray induced lipid peroxidation as assessed by measuring thiobarbituric acid reactive substrates, lipid hydroperoxide and conjugated diene. Likewise, it prevented radiation-induced DNA strand breaks in a concentration dependent manner. The radioprotective activity of PE could be attributed to its hydroxyl and superoxide radicals scavenging property along with its lymphoproliferative activity. The radical scavenging capacity of PE was primarily due to its constituent phenolics, which were isolated and identified as chevibetol and allyl pyrocatechol.

Animals↗
PubMedDate not supplied

Antiproliferative effects of two amides, piperine and piplartine, from Piper species.

The present work evaluated the cytotoxicity of piplartine {5,6-dihydro-1-[1-oxo-3-(3,4,5-trimethoxyphenyl)-trans-2-propenyl]-2(1H)pyridinone} and piperine {1-[5-(1,3)-benzodioxol-5-yl)-1-oxo-2,4-pentadienyl]piperidine}, components obtained from Piper species. The substances were tested for their cytotoxicity on the brine shrimp lethality assay, sea urchin eggs development, 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay using tumor cell lines and lytic activity on mouse erythrocytes. Piperine showed higher toxicity in brine shrimp (DL50 = 2.8 +/- 0.3 microg/ml) than piplartine (DL50 = 32.3 +/- 3.4 microg/ml). Both piplartine and piperine inhibited the sea urchin eggs development during all phases examined, first and third cleavage and blastulae, but in this assay piplartine was more potent than piperine. In the MTT assay, piplartine was the most active with IC50 values in the range of 0.7 to 1.7 microg/ml. None of the tested substances induced hemolysis of mouse erythrocytes, suggesting that the cytotoxicity of piplartine and piperine was not related to membrane damage.

Alkaloids↗
PubMed2006

In vivo growth-inhibition of Sarcoma 180 by piplartine and piperine, two alkaloid amides from Piper.

Piplartine {5,6-dihydro-1-[1-oxo-3-(3,4,5-trimethoxyphenyl)-2-propenyl]-2(1H)pyridinone} and piperine {1-5-(1,3)-benzodioxol-5-yl)-1-oxo-2,4-pentadienyl]piperidine} are alkaloid amides isolated from Piper. Both have been reported to show cytotoxic activity towards several tumor cell lines. In the present study, the in vivo antitumor activity of these compounds was evaluated in 60 female Swiss mice (N = 10 per group) transplanted with Sarcoma 180. Histopathological and morphological analyses of the tumor and the organs, including liver, spleen, and kidney, were performed in order to evaluate the toxicological aspects of the treatment with these amides. Administration of piplartine or piperine (50 or 100 mg kg(-1) day(-1) intraperitoneally for 7 days starting 1 day after inoculation) inhibited solid tumor development in mice transplanted with Sarcoma 180 cells. The inhibition rates were 28.7 and 52.3% for piplartine and 55.1 and 56.8% for piperine, after 7 days of treatment, at the lower and higher doses, respectively. The antitumor activity of piplartine was related to inhibition of the tumor proliferation rate, as observed by reduction of Ki67 staining, a nuclear antigen associated with G1, S, G2, and M cell cycle phases, in tumors from treated animals. However, piperine did not inhibit cell proliferation as observed in Ki67 immunohistochemical analysis. Histopathological analysis of liver and kidney showed that both organs were reversibly affected by piplartine and piperine treatment, but in a different way. Piperine was more toxic to the liver, leading to ballooning degeneration of hepatocytes, accompanied by microvesicular steatosis in some areas, than piplartine which, in turn, was more toxic to the kidney, leading to discrete hydropic changes of the proximal tubular and glomerular epithelium and tubular hemorrhage in treated animals.

Alkaloids↗
PubMed2003

New constituents of Piper guineense fruit and leaf.

Fourteen compounds were isolated from the fruits and leaves of Piper guineense Schum and Thonn (Piperaceae). Two of those were regarded to be new natural compounds, N-pyrrolidyl-2,4-octadecadienamide and N-piperidyl-2,4-octadecadienamide.

Fruit↗
PubMed2003

Analgesic activity of Piper longum Linn. root.

Piper longum root, commonly called Kandantippili, is traditionally used to treat rheumatism, insomnia, palsy and epilepsy. But a scientific study on its central actions is not available. This study screens P. longum root for opioid type analgesia using rat tail-flick method and for NSAID type analgesia using acetic-acid writhing method. Pentazocine (ip) and ibuprofen (oral) are used as respective drug controls. An aqueous suspension of P. longum root powder is given orally to mice and rat in doses of 200, 400 and 800 mg/kg. The delay in reaction time for thermal stimulus in rats and the number of writhings to chemical stimulus in mice are determined in each group. The results are analysed statistically. The 400 and 800 mg/kg doses of P. longum show significant NSAID type of analgesia (P < 0.001). Both Ibuprofen (40 mg/kg) and P. longum (800 mg/kg) show 50% protection against writhing. The delay in reaction time to thermal stimulus was less than 6% for different doses of P. longum as against 100% for pentazocine. This indicates that P. longum root has weak opioid but potent NSAID type of analgesic activity.

Analgesics↗
PubMed2003

Association of cucumovirus and potyvirus with betelvine (Piper betle L.) as evidenced by ELISA and RT-PCR.

An attempt was made to detect various viruses of Piper betle grown at Mahoba and Banthara in India. DAC-ELISA and RT-PCR tests were performed in leaf sap samples of betelvine for detection of a cucumovirus (Cucumber mosaic virus) and potyvirus (Bean yellow mosaic virus) using specific antibodies and universal primers of respective viruses. DAC-ELISA could detect only CMV. However, RT-PCR detected both cucumovirus and potyvirus infection in betelvine samples. Association of CMV with betelvine was observed for the first time in the present study.

Antibodies, Viral↗
PubMed2004

[Pharmacological studies on extracts from Piper boehmeriaefolium var. tonkinense].

OBJECTIVE: To study sedative, analgesic, antidepressant and anti-inflammatory effects of the extracts from Piper boehmeriaefolium var. tonkinense. METHOD: EtOAc soluble constituents and EtOH soluble constituents were administered 50, 100 mg x kg(-1) to mice respectively. The sedative effects were determined by autonomic action test. The analgesic effects were observed by the twisting test induced by acetic acid. The antidepressant effects were investigated by the forced swimming test. The anti-inflammatory effects were studied by auricle swelling induced by xylene. RESULT: EtOAc extracts could significantly lower autonomic action times, reduce squirming induced by acetic acid accumulated immobility time in forced swimming and auricle swelling values by xylene. But EtOH extracts could only decrease autonomic action times and accumulated immobility time. CONCLUSION: The active ingredients with sedation, analgesia, antidepressant and anti-inflammation in P. boehmeriaefolium var. tonkinense exist mainly in the EtOAc extracts.

Acetates↗
PubMed2005

Protective effects of Piper nigrum and Vinca rosea in alloxan induced diabetic rats.

In the present study aqueous extract of Piper nigrum seeds and Vinca rosea flowers were administered orally to alloxan induced diabetic rats once a day for 4 weeks. These treatments lead to significant lowering of blood sugar level and reduction in serum lipids. The levels of antioxidant enzymes, catalase and glutathione peroxidase decreased in alloxan induced diabetic rats however these levels returned to normal in insulin, P. nigrum and V. rosea treated rats. There was no significant difference in superoxide dismutase activity in all groups compared to controls. Lipid peroxidation levels were significantly higher in diabetic rats and it was slightly increased in insulin, P. nigrum and V. rosea treated rats as compared to control rat. These results suggest that oxidative stress plays a key role in diabetes, and treatment with P. nigrum and V. rosea are useful in controlling not only the glucose and lipid levels but these components may also be helpful in strengthening the antioxidants potential.

Animals↗
PubMed2004

[Reproductive structures of Piper amalago var. medium Linnaeus (Piperaceae)].

Flowers, fruits, seeds and subterranean organ of Piper amalago var. medium Linnaeus were analyzed structurally. Flowers are hermaphrodite lacking perianth, with two stamens and a tricarpelate gynoecea. Tetrasporangiate anthers shows epidermis, endothecium, one or two middle layers and secretory tapetum. Ovary has a simple structure, with ventral meristem. There is one orthotropous, bitegmic and crassinucellate ovule. Fruits are drupes. Seeds are endotegmic with copious perisperm. Putamen is composed of a sclerified inner mesocarp and endocarp. Individuals of the species can be interlinked by radicular subterranean organ, that can spread vegetatively.

Flowers↗
PubMed2005

[Antidepressant amides from Piper laetispicum C. DC].

AIM: To investigate the antidepressant constituents of Piper laetispicum C. DC. METHODS: The compounds were enriched by column chromatography on silica gel. Structural determination of the pure compounds was based on extensive analyses of modern spectroscopic methods including MS, HR-MS, UV, IR, 1D- and 2D-NMR spectra. The mouse forced swimming test was used for chasing antidepressant activity. RESULTS: Three amides were isolated and identified as N-isobutyl-(3,4-methylendioxyphenyl)-2E, 4E, 9E-undecatrienoamide (I), N-isobutyl-9-phenyl-2E, 4E-nonadienamide (II) and N-isobutyl-7-phenyl-2E, 4E-heptadienamide (III). CONCLUSION: N-Isobutyl-(3,4-methylendioxyphenyl)-2E, 4E, 9E-undecatrienoamide (I) is a new compound named as laetispicine. N-Isobutyl-9-phenyl-2E, 4E-nonadienamide (II) and N-isobutyl-7-phenyl-2E, 4E-heptadienamide (III) were isolated for the first time as natural substance.

Antidepressive Agents↗
PubMed2005

Alteration of pharmacokinetics of oxytetracycline following oral administration of Piper longum in hens.

The pharmacokinetic profile of orally administered oxytetracycline (10 mg/kg body weight) was studied 7 days post oral treatment of Piper longum (15 mg equivalent/kg) in White Leghorn hens (2-2.8 kg). On the day 8, oxytetracycline (OTC) was administered orally and blood samples were collected from the wing vein in heparinised vials for plasma separation at 0 (pre-treatment), 15, 30, 60, 120, 240, 360, 480 and 600 minutes post OTC administration. Plasma OTC concentrations were determined by microbial assay technique using Bacillus cereus var. mycoides (ATCC 11778) as test organism. The plasma levels of OTC against time were adequately described by one compartment open model. The pharmacokinetic data revealed that P.longum treated animals had significantly higher area under curve (AUC), area under the first moment of plasma drug concentration-time curve (AUMC) and mean residential time (MRT). Prior treatment of P.longum significantly reduced elimination rate constant(beta)and increased elimination half life (t(1/2beta)). The total body clearance (Cl(B)) reduced by 21%whereas total duration of pharmacological effect (t(d)) increased by 29%. The treatment with P. longum reduced loading and maintenance dose by 33.3 and 39%, respectively.

Administration, Oral↗
PubMed2005

Mosquito larvicidal activity of aqueous extracts of long pepper (Piper retrofractum vahl) from Thailand.

Aqueous extracts of nine medicinal plants were bioassayed against larvae of Culex quinquefasciatus Say and Aedes aegypt (L.). Among these plants, the long pepper, Piper retrofractum Vahl (Piperaceae), showed the highest level of activity against mosquito larvae. To gain more information on larvicidal activity of P. retrofractum, fresh fruits of this plant were extracted in water and the extracts made into powder and bioassayed against 3rd and 4th instar larvae of Cx. quinquefasciatus and Ae. aegypti in the laboratory. Extracts of unripe (001/3) and ripe (002/3 and 001/4) fruits showed different levels of activity against Cx. quinquefasciatus larvae. Extracts 001/3 and 002/3 were equi-toxic to a Bacillus sphaericus resistant and susceptible strains, both from Thailand. The ripe fruit extract 002/3 was somewhat more active against Ae. aegypti than Cx. quinquefasciatus. Another ripe fruit extract (001/4) was much more toxic to both mosquito species. Diluted solutions of the solid extract (002/3) in distilled water lost their larvicidal activity upon aging. Loss of activity at 25 degrees C was greater than that stored at 4 degrees C, and greater in water than in acetone solution.

Aedes↗
PubMed2006

[Potential allelopathic effects of Piper nigrum, Mangifera indica and Clausena lansium].

With Piper nigrum, Mangifera indica and Clausena lansium as the donators, this paper studied their potential allelopathic effects on the germination and growth of Zea mays, Glycine max, Cucurbita moschata, Arachis hypogaea, Raphanus sativus, Echinochloa crusgalli, Digitaria sanguinalis and Stylosanthes guianensis. The results showed that the aqueous extracts of these donators could inhibit the germination and growth of Z. mays, G. max, C. moschata, E. crus-galli and D. sanguinalis at high concentration, but stimulate them at low concentration. In rhizosphere soil of P. nigrum and M. indica, the germination and growth of Z. mays L was stimulated, while A. hypogaea was inhibited. The aqueous extracts of the donators were extracted by ethyl acetate and n-butanol, respectively, and the inhibitory activity of both aqueous and n-butanol fractions from P. nigrum and M. indica on Z. mays, R. sativus and S. guianensis was stronger than that of ethyl acetate fraction, indicating that P. nigrum and M. indica contained the allelochemicals with high polarity.

Clausena↗
PubMed1998

The revised Piper Fatigue Scale: psychometric evaluation in women with breast cancer.

PURPOSE/OBJECTIVES: To confirm the multidimensionality of the Piper Fatigue Scale (PFS) and to reduce the total number of PFS items without compromising reliability and validity estimates. DESIGN: Methodologic, part of a larger, cross-sectional, mailed survey design study. SETTING: Urban and suburban area in the northeast United States. SAMPLE: As part of the larger study, 2,250 surveys were distributed to women survivors of breast cancer who were on a mailing list for the educational organization Living Beyond Breast Cancer, 715 surveys (32%) were returned. Of these, 382 women met this methodologic study's criteria for having completed each of the 40 items on the PFS. The average respondent was 50 years old, postmenopausal, and treated with combination cancer therapy. METHODS: Principal axes factor analysis with oblique rotation. MAIN RESEARCH VARIABLES: Fatigue factors/subscales. FINDINGS: Five factors/subscales were identified initially. Because the fifth factor contained only two items (ability to bathe/wash and ability to dress), these items and the associated factor/subscale were dropped from the final solution. An additional nine items, not loading on any factor (> 0.40), also were dropped. The remaining items and factors/subscales were reviewed to ensure that the criteria were met: a pattern of inter-item correlations between 0.30-0.70; a minimum number of five or more items/subscale; standardized alpha for the subscales and total scale of at least 0.89; and absence of gender-specific items. CONCLUSIONS: The revised version of the PFS consists of 22 items and four subscales: behavioral/severity (6 items), affective meaning (5 items), sensory (5 items) and cognitive/mood (6 items). Standardized alpha for the entire scale (n = 22 items) is 0.97, indicating that some redundancy still may exist among the items. Additional revisions await further testing. IMPLICATIONS FOR NURSING PRACTICE: As fatigue is acknowledged to be the most frequent symptom experienced by patients with cancer, accurate measurement and assessment is essential to advance not only the science of fatigue but, most importantly, to evaluate the efficacy of intervention strategies on patient and family outcomes.

Breast Neoplasms↗
PubMed2000

The presence of cholinomimetic and calcium channel antagonist constituents in Piper betle Linn.

The crude aqueous extract of Piper betle leaves (Pb.Cr) was studied for the possible presence of cholinomimetic and calcium channel antagonist constituents. Pb.Cr at doses of 1-10 mg/mL caused a moderate spasmogenic effect in isolated guinea-pig ileum and this activity was concentrated in the aqueous fraction, which was found to be about 5 times more potent. Pretreatment of the tissue with atropine (1 microM) but not hexamethonium (100 microM) completely abolished the contractile effect of the aqueous fraction indicating a cholinergic (muscarinic) mechanism. In isolated rabbit jejunum preparations Pb.Cr did not produce a significant increase in the spontaneous contractions, but instead produced a dose-dependent (0.03-3.0 mg/mL) inhibition of spontaneous activity. Activity-directed fractionation revealed that the spasmolytic action was concentrated in the ethyl acetate fraction. When tested against K(+)-induced contractions, both Pb.Cr and its ethyl acetate fraction (Pb.EtAc) caused a dose-dependent inhibition, suggesting calcium channel blockade (CCB). The potent CCB effect of the crude extract and its ethyl acetate fraction was confirmed when pretreatment of the tissue with Pb.Cr or Pb.EtAc shifted the Ca(++) dose-response curves to the right in a dose-dependent manner. These data indicate that the plant contains cholinomimetic and possible calcium channel antagonist constituents, which are concentrated in the aqueous and ethyl acetate fractions respectively. It is suggested that some of the traditional uses of this plant may be explained on the basis of these activities.

Animals↗
PubMed2001

Sesamin a potent antifeedant principle from Piper mullesua.

Sesamin, a major lignan of Piper mullesua of Manipur origin, exhibited significant antifeedant activity and moderate growth inhibition towards 4th instar larvae of Spilarctia obliqua. No larval toxicity of sesamin could be established in topical bioassay experiments. Its effective dose for 50% feeding deterrence (ED(50)) and growth inhibition (GI(50)) were found to be 3856 and 6212 ppm, respectively.

Animals↗