CN101805285B - Nicotinic acid-contained curcumin ester derivative and preparation method and application thereof - Google Patents

Nicotinic acid-contained curcumin ester derivative and preparation method and application thereof Download PDF

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CN101805285B
CN101805285B CN2009100426658A CN200910042665A CN101805285B CN 101805285 B CN101805285 B CN 101805285B CN 2009100426658 A CN2009100426658 A CN 2009100426658A CN 200910042665 A CN200910042665 A CN 200910042665A CN 101805285 B CN101805285 B CN 101805285B
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nicotinic acid
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curcumin ester
ester
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CN101805285A (en
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廖端芳
郑兴
庹勤慧
朱炳阳
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University of South China
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Abstract

The invention relates to a nicotinic acid-contained curcumin ester derivative and a preparation method and application thereof. The curcumin has various physiological activities and pharmacological effects, such as the resistance of inflammation, bacterium, tumor, tracheitis and oxidation, blood pressure reduction, neuroprotection, and the like. The compound and salts thereof can be used for preparing medicaments of resisting inflammation, cancers, bacteria and viruses, lowering blood pressure and blood sugar and adjusting blood fat. The compound has the excellent effects of lowering blood fat, blood sugar and blood pressure and resisting cancers, bacteria and viruses, has less toxicity, easy preparation method, convenient industrial production, can satisfy the need of the medical field and has the advantages of high curative effect, low toxicity, and the like.

Description

Nicotinic acid-contained curcumin ester derivative and method of manufacture thereof and purposes
Technical field
The present invention relates to a kind of medicine, particularly a kind ofly have anti-inflammatory, transfer blood fat, nicotinic acid-contained curcumin ester derivative and the method for manufacture and the purposes of hypoglycemic, anticancer, step-down, antibiotic, antivirus action.
Background technology
Curcumine is a kind of important activity composition that nearly all zingiberaceous plant all contains.Curcumine have anti-inflammatory, antibiotic, antitumor, hypotensive, prevent and treat multiple physiologically active and pharmacological actions such as trachitis, anti-oxidant and neuroprotective.Curcumine has got into the I phase clinical experiment stage in the U.S..But, further discover in curcumine active on the low side, the body in vivo absorb less, tachytrophism and bioavailability be low, these characteristics have greatly limited its application.At present curcumine is carried out structural modification and mainly concentrate on the following aspects: CN101003470A; CN1646473A; WO 2003/088927; Cancer Lett., 2000 (159): 135-140.But the technology of above-mentioned patent, bibliographical information all fails to deal with problems effectively.
Summary of the invention
One of the object of the invention provides a kind of new nicotinic acid-contained curcumin ester derivative, to satisfy the needs of field of medicaments.
The technical scheme that realizes above-mentioned purpose of the present invention is: in order to strengthen the activity of curcumin chemical compounds; The contriver introduces the nicotinic acid group in the curcumin chemical compounds; To obtain a kind of novel nicotinic acid-contained curcumin ester derivative; To improve the biological activity of curcumin chemical compounds, to satisfy the needs of clinical application.
Nicotinic acid-contained curcumin ester derivative of the present invention is the compounds with general structure I.
Wherein: R in the general formula I 1, R 2, R 3, R 4, R 5, R 6, R 7, R 8, R 9, R 10, R 11, R 12, R 13, R 14Can be identical or different: can be hydrogen, halogen, hydroxyl or the alkyl that contains 1-8 carbon atom, alkoxyl group, acyl alkoxyl group or alkynyl, the thiazolinyl that contains 2-6 carbon atom or the naphthenic base that contains 3-9 carbon atom or aralkyl, phenyl, cyanic acid alkyl, 4-nitro alkyl, carboxyl, alkylhalide group, list or polyhydroxy alkyl, alkyl-thio-alkyl, alkyl sulfonyl alkyl, acyloxy alkyl, acyl group alkyl, sulfonic group, but R 1, R 2, R 3, R 4, R 5, R 6, R 7, R 8, R 9, R 10In at least one is R.
The further technical scheme of the present invention is: the preferred compound of the present invention comprises:
4 '-hydroxyl-4 " nicotinic acid curcumin ester (code name 101)
4 '-methoxyl group-4 " nicotinic acid curcumin ester (code name 102)
4 '-oxyethyl group-4 " nicotinic acid curcumin ester (code name 103)
4 '-propoxy--4 " nicotinic acid curcumin ester (code name 104)
4 '-benzyloxy-4 " nicotinic acid curcumin ester (code name 105)
4 '-heptan oxygen base-4 " nicotinic acid curcumin ester (code name 106)
4 '-octyloxy-4 " nicotinic acid curcumin ester (code name 107)
4 '-last of the ten Heavenly stems oxygen base-4 " nicotinic acid curcumin ester (code name 108)
4 " hydroxyl-4 '-nicotinic acid curcumin ester (code name 109)
4 " allyloxy-4 '-nicotinic acid curcumin ester (code name 110)
4 " methoxyl group-4 '-nicotinic acid curcumin ester (code name 111)
4 " oxyethyl group-4 '-nicotinic acid curcumin ester (code name 112)
4 " propoxy--4 '-nicotinic acid curcumin ester (code name 113)
4 " benzyloxy-4 '-nicotinic acid curcumin ester (code name 114)
4 " heptan oxygen base-4 '-nicotinic acid curcumin ester (code name 115)
4 " octyloxy-4 '-nicotinic acid curcumin ester (code name 116)
4 " last of the ten Heavenly stems oxygen base-4 '-nicotinic acid curcumin ester (code name 117)
4 ', 4 " two nicotinic acid curcumin esters (code name 118)
The further again technical scheme of the present invention is: comprise that also the nicotinic acid-contained curcumin ester derivative compounds is at pharmacy acceptable salt and their pharmaceutical prepn.
The present invention's technical scheme further is: comprise that also compound 101, compound 102, compound 103, compound 104, compound 105, compound 106, compound 107, compound 108, compound 109, compound 110, compound 111, compound 112, compound 113, compound 114, compound 115, compound 116, compound 117, compound 118 are at pharmacy acceptable salt and their pharmaceutical prepn.
Two of the object of the invention provides a kind of method of manufacture of nicotinic acid-contained curcumin ester derivative.
The technical scheme that realizes above-mentioned purpose of the present invention is: with the curcumine of method preparation well known in the art and verivate (II, IV, VI) thereof in solvent in 60 ~ 75 ℃ down with the nicotinic acid of method preparation well known in the art and derivatives reaction thereof 4 ~ 10 hours, acquisition title product (III, V, VII); Reaction formula is following:
Figure G2009100426658D00041
The further technical scheme of the present invention is: the compound that will have general structure III, V or VII reacts under 5 ~ 85 ℃ of conditions with acid, promptly obtains the salt of the said compound of the present invention.
The present invention's technical scheme further is: said acid comprises hydrochloric acid, Hydrogen bromide or hydroiodic acid HI, preferred hydrochloric acid.
The further again technical scheme of the present invention is: said solvent is sulfur oxychloride or acetone.
Three of the object of the invention provides a kind of purposes of nicotinic acid-contained curcumin ester derivative.
The technical scheme that realizes above-mentioned purpose of the present invention is: the application of nicotinic acid-contained curcumin ester derivative in the medicine of diseases such as preparation treatment inflammation, hyperlipidemia, hyperglycemia, hypertension, cancer, mushroom or virus infection.
The further technical scheme of the present invention is: the nicotinic acid-contained curcumin ester derivative compounds is at pharmacy acceptable salt and their pharmaceutical prepn, and they are in pharmaceutically purposes.
The further again technical scheme of the present invention is: the purposes of nicotinic acid-contained curcumin ester derivative compounds comprises as antiphlogiston, antimicrobial drug, anticarcinogen, hypotensor, lipid regulating agent, antiviral drug and neuroprotective drug.
Compound of the present invention has been carried out following pharmacological evaluation:
The anti-inflammatory aspect:
The anti-inflammatory aspect is included in body and isolated experiment.Adopt high fat rat model in the body experiment; Detect compound 101 with general formula I structure, compound 109, compound 118 to (the C-reactive protein of c reactive protein in the serum with the ELISA method; CRP), interleukin (interleukin, IL-6), the influence that discharges of inflammatory factor such as IL-10.Oral 25mg/Kg/ days (sneaking in the feed), 4 weeks of successive administration, significantly lipopenicillinase the time, can obviously reduce the content of change of serum C RP, IL-6, IL-10, its usefulness and lovastatin are similar.Isolated experiment adopts high fat animal or the isolating CD4+T cell of intact animal spleen; Stimulate inflammatory reaction with CD3 antibody; IL-4 in the T cell culture medium of still hatching with ELISA method detection compound, the release conditions of IL-10 is observed the release of these compound inflammation-inhibiting factors equally.
Transfer lipid aspects: adopt ApoE knock-out mice Atherosclerosis Model, with the full-automatic biochemical analyzing equipment enzyme process of HITACHI7060 ( Zhang C, et al. J Lipid Res.2006; 47 (9): 2055-63) measured the accent blood fat and the study of anti-atherogenic effect of compound 101 with general formula I structure, compound 109, compound 118.Oral 25mg/Kg/ days (sneaking in the feed), 8 weeks of successive administration, can significantly reduce blood plasma LDL-C, TC level, TG also there is certain reduction effect; Simultaneously, the effect of the HDL-C that raises in addition, its usefulness and lovastatin are suitable; And obviously suppressing atheromatous plaque forms.
Anticancer aspect comprises in the body and experiment in vitro.Wherein the CDCC of compound 101, compound 109, compound 118, its IC have detected with mtt assay and srb assay in experiment in vitro system 50Value is 0.05 ~ 25.0nM.Experiment is performed such in the body: give the compound of lotus Lewis lung knurl mouse peritoneal injection general formula I, and continuous 9 days, can significantly suppress the growth of Lewis lung knurl, inhibiting rate is 91.3%.If abdominal injection 0.5-25mg/kg compound 101, compound 109, compound 118 can suppress the S-180 knurl growth of ICR-Jc1 mouse hypodermic inoculation.
Antibiosis: compound 101, compound 109, compound 118 with general formula I structure have significant anti-microbial effect.
Hypoglycemic aspect: oral 0.1-40mg/Kg compound 101, compound 109, compound 118, detect blood sugar concentration and find that compound 101, compound 109, compound 118 have remarkable hypoglycemic activity after 7 days.
Hypotensive aspect: oral 1.0-25mg/Kg compound 101, compound 109, compound 118, detect blood pressure and find that compound 101, compound 109, compound 118 have remarkable hypotensive activity after 14 days.
Anti-virus aspect: compound 101, compound 109, compound 118 can significantly suppress the growth and breeding of HIV-1 virus.
Acute toxicity test: give mice lavage compound 101, compound 109, compound 118 with 1 heavy dose; Observe index and toxic reaction degree such as small white mouse behavioral activity continuously; And when experiment finishes, put to death small white mouse and analyse, to obtain compound 101, compound 109, compound 118 toxicity data.Observed 14 days continuously, it is unusual that small white mouse does not have evident act, death also occurs, and maximum dose level 1000mg/kg and following dosage thereof that experiment is set all do not have overt toxicity to small white mouse.
Prove that through pharmacological evaluation compound of the present invention has in various degree anti-inflammatory, transfers blood fat, anticancer, step-down, hypoglycemic, antibiotic, antivirus action, and toxicity is lower.
Therefore, compound of the present invention and salt thereof can be used for preparing anti-inflammatory, transfer blood fat, anticancer, step-down, hypoglycemic, antibiotic, antiviral drug.
Compound of the present invention can compsn administered in the patient of needs treatment; Said compsn comprises compound of the present invention and the salt and the pharmaceutically acceptable carrier of treating significant quantity; Said carrier comprises thinner (like water), weighting agent (like starch), wetting agent (like glycerine), tackiness agent (like derivatived cellulose) etc.; And be prepared into tablet, capsule, pill, granule, syrup, emulsion, suspension liquid and solution with method well known in the art; By conventional administration, preferential oral administration, dosage is 0.001 ~ 25mg/kg body weight.
Compound of the present invention has good reducing blood-fat, hypoglycemic, anticancer, step-down, antibiotic, antivirus action, and toxicity is less, and the preparation method is easy, is convenient to suitability for industrialized production, can satisfy the needs of field of medicaments.Compound of the present invention has curative effect height, low toxin.
Below in conjunction with embodiment detailed content of the present invention is further described.
Embodiment
Embodiment 1
4 '-hydroxyl-4 " nicotinic acid curcumin ester (code name 101), 4 "-hydroxyl-4 '-nicotinic acid curcumin ester (code name 109) and 4 ', 4 " and two nicotinic acid curcumin esters (code name 118) preparation:
The 0.01mol curcumine was reacted 10 hours with 0.03mol nicotinic acid down in 75 ℃ in the 10ml sulfur oxychloride; Pour in the ice-water bath; With ethyl acetate extraction 3 times, anhydrous sodium sulfate drying is used ETHYLE ACETATE: sherwood oil=1: 3 column chromatography then; Acquisition title product 4 '-hydroxyl-4 " nicotinic acid curcumin ester (code name 101), 4 "-hydroxyl-4 '-nicotinic acid curcumin ester (code name 109) and 4 ', 4 " two nicotinic acid curcumin esters (code name 118).Related data is following:
4 '-hydroxyl-4 " nicotinic acid curcumin ester (code name 101): MS (EI, 70ev) m/z:473; Anal.Calcd.for C 27H 23NO 7: C, 68.49, H, 4.90, N 2.96; Found C, 68.22, H, 4.80, N 2.95.
4 " hydroxyl-4 '-nicotinic acid curcumin ester (code name 109): MS (EI, 70ev) m/z:473; Anal.Calcd.for C 27H 23NO 7: C, 68.49, H, 4.90, N 2.96; Found C, 68.27, H, 4.67, N 2.96.
4 ', 4 " two nicotinic acid curcumin esters (code name 118): MS (EI, 70ev) m/z:578; Anal.Calcd.for C 33H 26N 2O 8: C, 68.51, H, 4.53, N 4.84; Found C, 68.41, H, 4.52, N 4.85.
Embodiment 2
4 '-methoxyl group-4 " preparation of nicotinic acid curcumin ester (code name 102):
" nicotinic acid curcumin ester (code name 101) is dissolved in the 25ml acetone, adds 10 gram catalyzer K with 0.03mol methyl iodide and 0.01mol 4 '-hydroxyl-4 2CO 3, 60 ℃ down reaction 4 hours title product 4 '-methoxyl group-4 " nicotinic acid curcumin ester.Related data is following:
MS(EI，70ev)m/z：487；Anal.Calcd.for?C 28H 25NO 7：C，68.98，H，5.17，N?2.87；Found?C，68.93，H，5.19，N?2.86。
Embodiment 3
4 '-oxyethyl group-4 " nicotinic acid curcumin ester (code name 103), 4 '-propoxy--4 "-nicotinic acid curcumin ester (code name 104), 4 '-benzyloxy-4 " nicotinic acid curcumin ester (code name 105), 4 '-heptan oxygen base-4 "-nicotinic acid curcumin ester (code name 106), 4 '-preparation of octyloxy-4 " nicotinic acid curcumin ester (code name 107), 4 '-last of the ten Heavenly stems oxygen base-4 "-nicotinic acid curcumin ester (code name 108):
With the 0.03mol haloalkane replace methyl iodide according to the operation of embodiment 2 can obtain compound 4 '-oxyethyl group-4 " nicotinic acid curcumin ester (code name 103), 4 '-propoxy--4 "-nicotinic acid curcumin ester (code name 104), 4 '-benzyloxy-4 " nicotinic acid curcumin ester (code name 105), 4 '-heptan oxygen base-4 "-nicotinic acid curcumin ester (code name 106), 4 '-octyloxy-4 " nicotinic acid curcumin ester (code name 107), 4 '-last of the ten Heavenly stems oxygen base-4 "-nicotinic acid curcumin ester (code name 108).Related data is following:
4 '-oxyethyl group-4 " nicotinic acid curcumin ester (code name 103): MS (EI, 70ev) m/z:501; Anal.Calcd.for C 29H 27NO 7: C, 69.45, H, 5.43, N 2.79; Found C, 69.46, H, 5.42, N 2.59.
4 '-propoxy--4 " nicotinic acid curcumin ester (code name 104): MS (EI, 70ev) m/z:515; Anal.Calcd.for C 30H 29NO 7: C, 69.89, H, 5.67, N 2.72; Found C, 69.73, H, 5.66, N 2.68.
4 '-benzyloxy-4 " nicotinic acid curcumin ester (code name 105): MS (EI, 70ev) m/z:465; Anal.Calcd.for C 34H 30NO 7: C, 72.33, H, 5.36, N 2.48; Found C, 72.31, H, 5.39, N 2.50.
4 '-heptan oxygen base-4 " nicotinic acid curcumin ester (code name 106): MS (EI, 70ev) m/z:571; Anal.Calcd.for C 34H 37NO 7: C, 71.44, H, 6.52, N 2.45; Found C, 71.42, H, 6.51, N 2.47.
4 '-octyloxy-4 " nicotinic acid curcumin ester (code name 107): MS (EI, 70ev) m/z:585; Anal.Calcd.for C 35H 39NO 7: C, 71.78, H, 6.71, N 2.39; Found C, 71.77, H, 6.73, N 2.36.
4 '-last of the ten Heavenly stems oxygen base-4 " nicotinic acid curcumin ester (code name 108): MS (EI, 70ev) m/z:613; Anal.Calcd.for C 37H 43NO 7: C, 72.41, H, 7.06, N 2.28; Found C, 72.39, H, 7.07, N 2.29.
Embodiment 4
4 " allyloxy-4 '-preparation of nicotinic acid curcumin ester (code name 110):
With 0.03mol allyl bromide 98 and 0.01mol 4 " hydroxyl-4 '-nicotinic acid curcumin ester (code name 109) is dissolved in the 25ml acetone, adds 10 gram catalyzer K 2CO 3, reaction got title product 4 in 4 hours under 60 ℃ " and allyloxy-4 '-nicotinic acid curcumin ester (code name 110).Related data is following:
MS(EI，70ev)m/z：513；Anal.Calcd.for?C 30H 27NO 7：C，70.16，H，5.30，N?2.73；Found?C，70.15，H，5.29，N2.75。
Embodiment 5
4 " methoxyl groups-4 '-nicotinic acid curcumin ester (code name 111), 4 "-oxyethyl group-4 '-nicotinic acid curcumin ester (code name 112), 4 " propoxy--4 '-nicotinic acid curcumin ester (code name 113), 4 "-benzyloxy-4 '-nicotinic acid curcumin ester (code name 114), 4 " heptan oxygen base-4 '-nicotinic acid curcumin ester (code name 115), 4 "-octyloxy-4 '-nicotinic acid curcumin ester (code name 116), 4 " last of the ten Heavenly stems oxygen base-4 '-preparation of nicotinic acid curcumin ester (code name 117):
Replace allyl bromide 98 can obtain compound 4 with the 0.03mol haloalkane according to embodiment 4 operations " methoxyl group-4 '-nicotinic acid curcumin ester (code name 111); 4 "-oxyethyl group-4 '-nicotinic acid curcumin ester (code name 112); 4 " propoxy--4 '-nicotinic acid curcumin ester (code name 113); 4 "-benzyloxy-4 '-nicotinic acid curcumin ester (code name 114); 4 " heptan oxygen base-4 '-nicotinic acid curcumin ester (code name 115); 4 "-octyloxy-4 '-nicotinic acid curcumin ester (code name 116); 4 " last of the ten Heavenly stems oxygen base-4 '-nicotinic acid curcumin ester (code name 117).Related data is following:
4 " methoxyl group-4 '-nicotinic acid curcumin ester (code name 111): MS (EI, 70ev) m/z:487; Anal.Calcd.for C 28H 25NO 7: C, 68.98, H, 5.17, N 2.87; Found C, 68.92, H, 5.29, N 2.89.
4 " oxyethyl group-4 '-nicotinic acid curcumin ester (code name 112): MS (EI, 70ev) m/z:501; Anal.Calcd.for C 29H 27NO 7: C, 69.45, H, 5.43, N 2.79; Found C, 69.47, H, 5.52, N 2.63.
4 " propoxy--4 '-nicotinic acid curcumin ester (code name 113): MS (EI, 70ev) m/z:515; Anal.Calcd.for C 30H 29NO 7: C, 69.89, H, 5.67, N 2.72; Found C, 69.85, H, 5.64, N 2.71.
4 " benzyloxy-4 '-nicotinic acid curcumin ester (code name 114): MS (EI, 70ev) m/z:465; Anal.Calcd.for C 34H 30NO 7: C, 72.33, H, 5.36, N 2.48; Found C, 72.40, H, 5.42, N 2.47.
4 " heptan oxygen base-4 '-nicotinic acid curcumin ester (code name 115): MS (EI, 70ev) m/z:571; Anal.Calcd.for C 34H 37NO 7: C, 71.44, H, 6.52, N 2.45; Found C, 71.39, H, 6.48, N 2.52.
4 " octyloxy-4 '-nicotinic acid curcumin ester (code name 116): MS (EI, 70ev) m/z:585; Anal.Calcd.for C 35H 39NO 7: C, 71.78, H, 6.71, N 2.39; Found C, 71.74, H, 6.70, N 2.35.
4 " last of the ten Heavenly stems oxygen base-4 '-nicotinic acid curcumin ester (code name 117): MS (EI, 70ev) m/z:613; Anal.Calcd.for C 37H 43NO 7: C, 72.41, H, 7.06, N 2.28; Found C, 72.43, H, 7.13, N 2.27.
Embodiment 6
Adopt the anti-inflammatory action of ELISA method detection compound 101, compound 109 and compound 118.As an example, some results that obtained see the following form 1:
Table 1: compound 101, compound 109 influence (n=10) with compound 118 to high fat rat blood serum inflammatory factor excretory
Grouping IL-6 (pg/ml)
IL-10(pg/ml)
Normal group 77.62 ± 19.91
126.33±13.10
High fat group 288.33 ± 17.10
333.69±28.10
Compound 101 156.28 ± 27.78*
278.69±14.67*
Compound 109 209.73 ± 43.56*
225.34±19.98*
Compound 118 226.73 ± 36.74*
199.56±38.52*
Lovastatin 192.23 ± 19.56*
231.91±24.55*
* the high fat group of p＜0.05vs
Embodiment 7
The full-automatic biochemical analyzing equipment enzyme process of employing HITACHI7060 ( Zhang C, et al. J Lipid Res.2006; 47 (9): 2055-63) measured the reducing blood lipid of part of compounds of the present invention.As an example, some results that obtained see table 2.
Table 2 compound 101, compound 109, compound 110 and compound 118 are to the influence of atherosclerosis mouse (ApoE-/-) blood fat
Figure G2009100426658D00121
The TC=total cholesterol; The TG=triacylglycerol; The LDL-C=low density lipoprotein cholesterol;
DL-C=low hdl SUV; *, p＜0.05; *, p＜0.01vs model group
Embodiment 8
With reference to the method (Mosman, T.J.Immunol Methods.1983,65,55) of Mosman, through the MTT colorimetric method for determining CDCC of part of compounds of the present invention, the result sees table 3.
Table 3
Active compound The anti-cancer of the stomach of IC50nM The anti-prostate cancer of IC50nM The IC50nM anti-cervical cancer The anti-lung cancer of IC50nM The IC50nM anti-breast cancer
Code name
101 0.22 1.63 8.86 5.03 22.12
109 0.05 16.3 1 20.1 6 1.04 8.42
118 5.52 3.33 3.42 1.05 2.87
Embodiment 9
Reference literature (Zhang Juntian chief editor, modern pharmacology experimental technique.) research various dose part of compounds of the present invention is to the effect of bacterium, fungi.Its result sees table 4.
Table 4
Active compound Staphylococcus MIC μ g/ml Streptococcus m IC μ g/ml Intestinal bacteria MIC μ g/ml Candida albicans MIC μ g/ml Cryptococcus neoformans MIC μ g/ml
Compound 101 5.21 2.78 0.0026 0.0030 0.18
Compound 109 0.12 0.011 7.22 16.33 2.54
Compound 110 1.32 11.02 2.25 5.01 0.0074
Compound 118 0.10 7.10 1.46 3.17 0.028
Embodiment 10
Reference literature (Joon-Su Shin, et al.Bioorg.Med.Chem.Lett.1999, the hypoglycemic activity of method research part of compounds of the present invention 9:869).Its result sees table 5.
Table 5
Active compound Dosage mg/Kg Blood sugar reduces (%)
Compound 101 0.2 82.3
Compound 109 0.4 60.2
Compound 110 0.8 84.1
Compound 118 40 99.6
Embodiment 11
The tablet that contains the compound of general formula (I) can be by method preparation well known in the art.
The compound 125mg of general formula (I)
Magnesium Stearate 4mg
Talcum powder 6mg
Lactose 45mg
Starch 50mg
Embodiment 12
The capsule that contains the compound of general formula (I) can be by method preparation well known in the art.
The compound 120mg of general formula (I)
Magnesium Stearate 20mg
Talcum powder 20mg
Lactose 45mg
Starch 20mg
Vinylpyrrolidone polymer 10mg

Claims (3)

1. nicotinic acid-contained curcumin ester derivative is characterized in that this verivate is:
4 '-hydroxyl-4 " nicotinic acid curcumin ester (code name 101)
4 '-methoxyl group-4 " nicotinic acid curcumin ester (code name 102)
4 '-oxyethyl group-4 " nicotinic acid curcumin ester (code name 103)
4 '-propoxy--4 " nicotinic acid curcumin ester (code name 104)
4 '-benzyloxy-4 " nicotinic acid curcumin ester (code name 105)
4 '-heptan oxygen base-4 " nicotinic acid curcumin ester (code name 106)
4 '-octyloxy-4 " nicotinic acid curcumin ester (code name 107)
4 '-last of the ten Heavenly stems oxygen base-4 " nicotinic acid curcumin ester (code name 108)
4 " hydroxyl-4 '-nicotinic acid curcumin ester (code name 109)
4 " allyloxy-4 '-nicotinic acid curcumin ester (code name 110)
4 " methoxyl group-4 '-nicotinic acid curcumin ester (code name 111)
4 " oxyethyl group-4 '-nicotinic acid curcumin ester (code name 112)
4 " propoxy--4 '-nicotinic acid curcumin ester (code name 113)
4 " benzyloxy-4 '-nicotinic acid curcumin ester (code name 114)
4 " heptan oxygen base-4 '-nicotinic acid curcumin ester (code name 115)
4 " octyloxy-4 '-nicotinic acid curcumin ester (code name 116)
4 " last of the ten Heavenly stems oxygen base-4 '-nicotinic acid curcumin ester (code name 117)
4 ', 4 " two nicotinic acid curcumin esters (code name 118).
2. the purposes of a nicotinic acid-contained curcumin ester derivative as claimed in claim 1 is characterized in that the application in the medicine of preparation treatment inflammation, hyperlipidemia, hyperglycemia, hypertension, cancer, mushroom disease.
3. the purposes of nicotinic acid-contained curcumin ester derivative according to claim 2 is characterized in that being used to prepare antiphlogiston, antimicrobial drug, anticarcinogen, hypotensor, lipid regulating agent.
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