山药化学成分的研究

从胡椒科植物山蒟中分得两个新木脂素类成分(Ia)和(Ⅱ),以及巴豆环氧素(Crorepoxide)(Ⅲ)和β-谷甾醇(Ⅳ)。经光谱分析及化学鉴定,(Ia)、(Ⅱ)为新结构,分别命名为山蒟素 B(hancinone)、山蒟素 C(hancinone C)。     

荜拔中的新酰胺成分

从荜拔地上部分乙醇提取物中分得５个化合物,经波谱分析确定其结构分别为：（α,β,α,β）－１,３－双（３,４－二甲基苯基）－２,４－双［１－（２－羰基－５,６－二氢吡啶）－甲酰基］－环丁烷（１）。     

华南胡椒化学成分的研究

从胡椒科植物华南胡椒（Ｐｉｐｅｒ ａｕｓｔｒｏｓｉｎｅｎｓｅ Ｃ．ＤＣ．）中分离出七个成分,经光谱分析和理化常数测定,分别鉴定为Ｎ－ｉｓｏｂｕｔｙｌ－３（３＇,４＇－ｍｅｔｈｙｌｅｎｅｄｉｏｘｙ－５＇－ｍｅｔｈｏｘｙｐｈｅｎｙｌ）－２Ｅ－ｔｒｉｍｏｎｏｉｅｎａｍｉｄｅ（Ｉ）、Ｎ－ｉｓｏｂｕｔｙｌ－７（３＇,４＇－ｍｅｔｙｌｅｎｅｄｉｏｘｙｐｈｅｎｙｌ）－２Ｅ,４Ｅ－ｈｅｐｔａｄｉｅｎａｍｉｄｅ（Ⅱ     

Piper longum Constituents Induce PANC-1 Human Pancreatic Cancer Cell Death under Nutrition Starvation

Pancreatic cancer is a highly aggressive form of cancer with a poor prognosis, partly due to ‘austerity’, a phenomenon of tolerance to nutrient deprivation and survival in its hypovascular tumor microenvironment. Anti-austerity agents which preferentially diminish the survival of cancer cells under nutrition starvation is regarded as new generation anti-cancer agents. This study investigated the potential of Piper longum constituents as anti-austerity agents. The ethanolic extract of Piper longum was found to have preferential cytotoxicity towards PANC-1 human pancreatic cancer cells in a nutrient-deprived medium (NDM). Further investigation led to the identification of pipernonaline ( 3 ) as the lead compound with the strongest anti-austerity activity, inducing cell death and inhibiting migration in a normal nutrient medium, as well as strongly inhibiting the Akt/mTOR/autophagy pathway. Therefore, pipernonaline ( 3 ) holds promise as a novel antiausterity agent for the treatment of pancreatic cancer.     

Chemical Profile and Biological Activities of Fungal Strains Isolated from Piper nigrum Roots: Experimental and Computational Approaches

The current report describes the chemical investigation and biological activity of extracts produced by three fungal strains Fusarium oxysporum, Penicillium simplicissimum, and Fusarium proliferatum isolated from the roots of Piper nigrum L. growing in Vietnam. These fungi were namely determined by morphological and DNA analyses. GC/MS identification revealed that the EtOAc extracts of these fungi were associated with the presence of saturated and unsaturated fatty acids. These EtOAc extracts showed cytotoxicity towards cancer cell lines HepG2, inhibited various microbacterial organisms, especially fungus Aspergillus niger and yeast Candida albicans (the MIC values of 50–100 μg/mL). In α-glucosidase inhibitory assay, they induced the IC₅₀ values of 1.00-2.53 μg/mL were better than positive control acarbose (169.80 μg/mL). The EtOAc extract of F. oxysporum also showed strong anti-inflammatory activity against NO production and PGE-2 level. Four major compounds linoleic acid (37.346 %), oleic acid (27.520 %), palmitic acid (25.547 %), and stearic acid (7.030 %) from the EtOAc extract of F. oxysporum were selective in molecular docking study, by which linoleic and oleic acids showed higher binding affinity towards α-glucosidase than palmitic and stearic acids. In subsequent docking assay with inducible nitric oxide synthase (iNOS), palmitic acid, oleic acid and linoleic acid could be moderate inhibitors.     

Safety of ethanolic kava extract: Results of a study of chronic toxicity in rats

BACKGROUNDS: Recently, potential liver toxicity was discussed with the intake of kava extract preparations (Piper methysticum) as anxiolytic drugs. The aim of this study was to test chronic toxicity in rats by oral application of an ethanolic kava full extract. METHODS: Wistar rats of both sexes were fed 7.3 or 73 mg/kg body weight of ethanolic kava extract for 3 and 6 months. The animals were examined for changes in body weight, hematological and liver parameters, and macroscopical and microscopical histological changes in the major organs. RESULTS: No signs of toxicity could be found. CONCLUSIONS: The results are in accordance with the medical experience regarding the use of kava preparations and the long tradition of kava drinking in the South Pacific island states. Specifically, the results do not back the suspicion of potential liver toxicity.     

MsrA Efflux Pump Inhibitory Activity of Piper cubeba L.f. and its Phytoconstituents against Staphylococcus aureus RN4220

MsrA, an efflux pump belonging to ATP‐binding cassette (ABC) transporter family that conferred resistance to macrolides, was detected in Staphylococcus aureus strains. Herein, we report the isolation of phytoconstituents from Piper cubeba fruit methanol extract and investigated their efflux pump inhibitory potential against S. aureus MsrA pump. Four isolated compounds, viz. pellitorine, sesamin, piperic acid and tetrahydropiperine studied in combination with erythromycin in S. aureus RN4220, exhibited 2–8‐fold reduction in minimum inhibitory concentration (MIC) of erythromycin. Pellitorine and sesamin decreased MIC of erythromycin by 8‐fold. The real‐time fluorometry‐based efflux and accumulation studies of ethidium bromide (EtBr) on S. aureus RN4220 in the presence of these compounds showed reduced efflux and enhanced uptake, thus indicating inhibition of the efflux pump. Pellitorine showed significant post‐antibiotic effect of erythromycin. The results revealed that the primary mechanism of action of these compounds involves steady ATP production impairment.     

Morphological and immunohistochemical study of the midgut and fat body of Spodoptera frugiperda (J.E. Smith) (Lepidoptera: noctuidae) treated with essential oils of the genus Piper

ABSTRACT

Essential oils are a promising alternative to insecticides. We investigated the LD₅₀ of oils extracted from Piper corcovadensis, P. marginatum, and P. arboreum after 48 h topical contact with Spodoptera frugiperda larvae using morphometry, histochemistry and immunohistochemistry of the midgut and fat body. Chromatography revealed that E-caryophyllene was the principal compound common to the Piper species. The essential oils of P. corcovadensis, P. marginatum and P. arboreum caused deleterious changes in the midgut of S. frugiperda larvae. P. corcovadensis oil produced the lowest LD₅₀ and significant histopathological alterations including elongation of the columnar cells, formation of cytoplasmic protrusions, reduction in carbohydrate, increased apoptotic index and decreased cell proliferation. P. arboreum oil caused histopathological alterations similar to P. corcovadensis, but caused the highest rate of cell proliferation and increased regenerative cells, which indicated rapid regeneration of the epithelium. Our findings demonstrated the insecticidal potential of P. corcovadensis for control of S. frugiperda owing to the significant damage it inflicted on S. frugiperda midgut.     

Control of storage rot of cassava tuber caused by Rhizopus oryzae using some plant extracts

Abstract

The potency of Piper nigrum seed and leaf, Aframomum meleguata seed and Ageratum conyzoides leaf extracts in the control of cassava tuber rot caused by Rhizopus oryzae was investigated. Water, ethanol and petroleum ether were used as extracting solvents. These extracts were fungitoxic both in vitro and in vivo against the test pathogen. P. nigrum seed extracts were the best followed by those of A. meleguata seed, A. conyzoides leaf and then P. nigrum leaf. The extracts were more effective in controlling rot development in unwounded than wounded tubers especially when they were applied before inoculation with the test pathogen. Ethanol extracts gave the highest growth inhibition in vivo followed by water and the petroleum ether extract whereas water extracts showed marked superiority over the extracting solvents in checking rot development in cassava tuber. Water and ethanol extracts of P. nigrum seed and leaf, A. meleguata seed and A. conyzoides leaf could be used as pesticide of plant origin in the control of R. oryzae causing cassava tuber rot in storage.     

Bioactivity of Piper guineense Schum. & Thonn seed and Moringa oleifera Lam. leaf powder against Trogoderma granarium Everts (Coleoptera: Dermestidae)

Laboratory studies were carried out to investigate bioactivity of Piper guineense seeds and Moringa oleifera leaf powders applied singly or in a mixture against larvae and adult Trogoderma granarium Everts in airtight containers. Three levels (0.0 g, 0.5 g, and 1.0 g/20 g groundnut seeds) of the plant powders were used and pirimiphos-methyl was applied at 0.01 g/20 g seeds (recommended dose). Another control consisting of untreated seeds with aerated lids was included in the bioassay. Both larvae and adults were not killed in control with aerated lids throughout the experimental period and larvae were also tolerant to airtight storage conditions. Adults were more susceptible to plant powders than larvae and adult mortality recorded in P. guineense at 1.0 g, 0.5 g and M. oleifera at 1.0 g/20 g seeds were not significantly different from the mortality observed with the recommended dose of Pirimiphos methyl at five days after treatment (DAT). Larval mortality observed in a mixture of both plants (1:1; w/w) caused significantly higher mortality (77.5%) than other treatments at 5 DAT. All treatments (P. guineense and M. oleifera applied singly or in a mixture) were repellant to larvae T. granarium with 60% repellency recorded in the mixture of plants, 50% repellency in P. guineense and 30% repellency in M. oleifera slurry. The water absorption capacity of treated seeds was not affected by treatment with plant powders and ranged from 31.98% to 37.59%.