Chemical Constituents And Pharmacological Activities Of Piper Flaviflorum C.DC.

With the high speed development of society, people always suffer from varieties ofpressures, which directly lead to a kind of psychological disorder called depression.Depression is not only a common feeling obstacle psychological ailment on earth, but alsoone of the most vulnerable disabled diseases. Therefore, it’s necessary to search for moreeffective and lower toxicity compounds from natural resources for clinical uses than before.Piper flaviflorum is a climbing liana, which belongs to the Piper genus of piperaceae. Itsproperty is hot and its flavor is spicy, which gets into wind and fire tower (Dai traditionalmedicinal theory). It can eliminate cold and relief pain, exhibit notably decontaminationeffect. Alkaloids, which possess antidepressant and anti-inflammatory activities, belong toa big kind of chemical category of the Piper genus. Meanwhile, the research on thechemical constituents and pharmacological activities of P. flaviflorum is extremelydeficient. Therefore, systematic research on the isolation of chemical components of thisplant and pharmacological properties seems to be vital, which not only enrich the clinicalapplication of medical plants of the Piper genus, but also rationally explore and utilizenovel nature products with high-activity and unique pharmacological mechanism, andmore broadly supply a stable fundamental exploration of medical plants of minority race inChina.This study mainly focused on chemical constituents and pharmacological activities ofP. flaviflorum:1Study on chemical constituents of P. flaviflorum1.1Isolation and identification of chemical constituentsFrom the ethanol extract of the aerial part of P. flaviflorum, we’ve got five fractionsviz. petroleum ether fraction, dichloromethane fraction, ethyl acetate fraction, n-butanolfraction and water fraction. Applying different sorts of methods like chromatographycolumn, ODS, preparative medium-pressure column, preparative thin layerchromatography and semi-preparative high performance liquid column, thedichloromethane fraction afforded30kinds of compounds, which were elucidated24compounds. In a similar way, the ether acetate fraction afforded28kinds of chemicalcomponents, which were elucidated22compounds. The n-butanol fraction gave sixcompounds which were elucidated two compounds. In all,42chemical constituents has been elucidated eventually, in which of three compounds are novel compounds (includingtwo alkaloids and one phenolic glucoside) and one compound is a new nature compound(phenylpropanoid glycoside).23compounds were isolated firstly from the Piper genus and40compounds were isolated firstly from P. flaviflorum. The chemical structure typesmainly contain alkaloids, flavones, flavonoid glycoside, phenylpropanoids and theirglycosides, purine and its nucleoside, imidazole and funan, phenolic acids and theirglycosides, sterol, phytol and so on.1.2Preparation, quantitation and qualitative analysis of total alkaloidsThe total alkaloids were prepared from the ethanol extracts of P. flaviflorum.Determination of quantitation of alkaloids was subjected to acid dye colorimetric method,and it contained alkaloids up to56.4%in which piperine accounted for52.8%. Theexistence of piperine was confirmed by HPLC-DAD and at the same time the other elevenalkaloids were proved to exist in total alkaloids by HPLC-ESI-MS except for piperolactamA, piperolactam B and cepahranone B.2Main pharmacological activity investigationAntidepressant activity in vivo was tested among the total fraction, total alkaloids andpiperine by performing classical ICR mice force swim test (FST). The effect wasobserved by wasting time on duration of immobility wth different doses. Results haveshowed the high doses of total alkaloids and piperine possessed the same antidepressantactivity which led to the conclusion that piperine was the main active chemicalconstituent of P. flaviflorum. At the same time, the monoamine neurotransmitter contents(5-HT, DA, NE) were determined by ELISA assay, and the results showed that theantidepressant activity of P. flaviflorum was due to elevate the5-HT content in micebrains.3General Pharmacological activity screening3.1Anti-inflammatory activityThrough stimulating RAW264.7cells by LPS, the experiment was tested on twonovel alkaloids named flaviflorum A and flaviflorum B and we observed the effect on NOdecreasing in vitro. They were evaluated anti-inflammatory activity and showednon-activity contrast with positive control (indometacin). The total fraction of P.flaviflorum and piperine have been tested on ear edema induced by xylene in mice, the high and low dosage of total fraction showed the anti-inflammatory activity, but piperinewas negative.3.2Anti-tumor activityA novel compound, named flavifloside A, and a new natural compound, named6’-O-(3,4-dimethoxycinnamoyl)-arbutin, with two known compounds named seguinoside Eand seguinoside K have been tested antitumor activities in vitro by performing on fourkinds of tumor cells, named A-549, HCT116, MDA-MB-231and CCRF-CEM. The otherthree showed inactive to tumor cells while the new compound flavifloside A showedantitumor activity to CCRF-CEM cell line with IC50at15.26μg/mL.