CN106344566A - Application of Ternatusine A in preparation of drugs for treating rectal cancer - Google Patents

Application of Ternatusine A in preparation of drugs for treating rectal cancer Download PDF

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Publication number
CN106344566A
CN106344566A CN201610815132.9A CN201610815132A CN106344566A CN 106344566 A CN106344566 A CN 106344566A CN 201610815132 A CN201610815132 A CN 201610815132A CN 106344566 A CN106344566 A CN 106344566A
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CN
China
Prior art keywords
ternatusine
rectal cancer
drugs
preparation
application
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Pending
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CN201610815132.9A
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Chinese (zh)
Inventor
田丽华
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Zibo Qidingli Patent Information Consulting Co Ltd
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Zibo Qidingli Patent Information Consulting Co Ltd
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Priority to CN201610815132.9A priority Critical patent/CN106344566A/en
Publication of CN106344566A publication Critical patent/CN106344566A/en
Pending legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

The invention discloses application of Ternatusine A in the preparation of drugs for treating rectal cancer and belongs to the technical field of novel applications of drugs. In-vitro MTT antitumor activity evaluation discovers that Ternatusine A also has significant action for human rectal cancer cell lines LOVE1, LOVO, SW620 and SW480; therefore, Ternatusine A is applicable to the preparation of drugs for resisting rectal cancer and has a promising development and application prospect. The application of Ternatusine A related herein in the preparation of drugs for treating rectal cancer is disclosed for the first time, and the inhibitory activity of Ternatusine A for rectal cancer cells is unexpectedly high.

Description

Application in preparation treatment rectum cancer drug for the ternatusine a
Technical field
The present invention relates to the new application of compound ternatusine a, more particularly, to ternatusine a are in preparation treatment Application in rectum cancer drug.
Background technology
Cancer is one of disease maximum to human life and health harm, has substantial amounts of people to die from cancer every year.Anticancer The research and development of medicine are always the focus of study of pharmacy.74% is had to be natural product or derivatives thereof in antitumor drug, such as Ramulus et folium taxi cuspidatae Alcohol and its derivant are exactly the current clinically reasonable antitumor drug of application effect.Therefore, find from natural product and resist Chemical compound for treating cancer or lead compound have great importance.
Compound ternatusine a according to the present invention be one deliver within 2013 (zhilai zhan, et al., ternatusine a,a new pyrrole derivative with an epoxyoxepino ring from Ranunculus ternatus.organic letters, 2013,15 (8): 1,970 1973.) noval chemical compound, this compound Have brand-new framework types, current purposes merely relates to antibacterial, antioxidation and anti AIDS virus, (zhilai zhan, et al.,ternatusine a,a new pyrrole derivative with an epoxyoxepino ring from Ranunculus ternatus.organic letters, 2013,15 (8): 1,970 1973.), for according to the present invention Purposes in preparation treatment rectum cancer drug for the ternatusine a belongs to first public.
Content of the invention
It is an object of the invention to not finding in studying according to existing ternatusine a that it has anti-rectal cancer activity The present situation of report, there is provided application in preparation medicine for treating rectal cancer for the ternatusine a.
Shown in described compound ternatusine a structure such as formula ():
The present invention is found by external mtt antitumor activity evaluation, and ternatusine a is to people's rectum cancer cell strain The growth of love1, lovo, sw620 and sw480 also has significant inhibitory action, suppresses the ic50 value point of this 4 plants of cell growths Not Wei 1.89 ± 0.43 μm, 2.76 ± 0.18m, 1.72 ± 0.38 μm and 2.59 ± 0.31 μm.Therefore, ternatusine a energy For preparing medicine for treating rectal cancer, there is good development prospect.
Purposes in preparation treatment rectum cancer drug for the ternatusine a according to the present invention is belonged to public first Open, because framework types belong to brand-new framework types, and it is unexpectedly strong for the inhibitory activity of rectum cancer cell, There is not the possibility being provided any enlightenment by other compounds, possess prominent substantive distinguishing features, be simultaneously used for the anti-of rectal cancer Control obviously to have and significantly improve.
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to concrete reality Apply any restriction of example, but be defined in the claims.
Specific embodiment
The preparation method of compound ternatusine a involved in the present invention referring to document (zhilai zhan, et al., ternatusine a,a new pyrrole derivative with an epoxyoxepino ring from ranunculus ternatus.organic letters,2013,15(8):1970–1973.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to concrete reality Apply any restriction of example, but be defined in the claims.
Embodiment 1: the preparation of compound ternatusine a tablet involved in the present invention:
Take 5 g of compound ternatusine a to add 195 grams of dextrin, mix, conventional tablet presses make 1000.
Embodiment 2: the preparation of compound ternatusine a capsule involved in the present invention:
Take 5 g of compound ternatusine a to add 195 grams of starch, mix, encapsulated make 1000.
To further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Experimental example: the growth inhibition effect to people's rectum cancer cell strain for the compound ternatusine a is evaluated using mtt method
1. method: be in the cell of growth logarithmic (log) phase: people rectum cancer cell strain love1, lovo, sw620 and sw480 (purchase Buy from Chinese Academy of Sciences's cell bank) with 1.5 × 104Concentration kind is in 96 orifice plates.Original training is sucked after cell culture 24h is adherent Foster base.Test is divided into blank control group, drug treating group.Blank group changes 1640 culture medium containing 10% hyclone;Medicine Treatment group is changed and is 100 μm containing concentration, 50 μm, 10 μm, 1 μm, 0.1 μm, 0.01 μm and 0.001 μm of ternatusine a's Culture medium.After culture 48h, add the mtt of concentration 5mg/ml, continue to be put in co2Incubator cultivates 4h, then along on culture fluid Portion sucks 100 μ l supernatants, adds 100 μ l dmso, and 10min is placed in dark place, is measured using microplate reader (sunrise Products) Light absorption value (wavelength 570nm), and cell survival is calculated according to light absorption value, each process sets 6 repeating holes.Cell survival rate (%)=δ od drug treating/δ od blank × 100.
2. result: ternatusine a has to the growth of people rectum cancer cell strain p love1, lovo, sw620 and sw480 There is significant inhibitory action.This compound suppresses the ic50 of people rectum cancer cell strain love1, lovo, sw620 and sw480 growth Value be respectively 1.89 ± 0.43 μm, 2.76 ± 0.18m, 1.72 ± 0.38 μm and 2.59 ± 0.31 μm.
Shown by above-described embodiment, the ternatusine a of the present invention to people rectum cancer cell strain love1, lovo, The growth of sw620 and sw480 has good inhibiting effect.Thus prove, the ternatusine a of the present invention has anti-rectum Cancer activity, can be used for preparing medicine for treating rectal cancer.

Claims (1)

  1. Application in treatment rectum cancer drug for the 1.ternatusine a, described compound ternatusine a structure such as formula Shown in ():
CN201610815132.9A 2016-09-11 2016-09-11 Application of Ternatusine A in preparation of drugs for treating rectal cancer Pending CN106344566A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201610815132.9A CN106344566A (en) 2016-09-11 2016-09-11 Application of Ternatusine A in preparation of drugs for treating rectal cancer

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201610815132.9A CN106344566A (en) 2016-09-11 2016-09-11 Application of Ternatusine A in preparation of drugs for treating rectal cancer

Publications (1)

Publication Number Publication Date
CN106344566A true CN106344566A (en) 2017-01-25

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CN201610815132.9A Pending CN106344566A (en) 2016-09-11 2016-09-11 Application of Ternatusine A in preparation of drugs for treating rectal cancer

Country Status (1)

Country Link
CN (1) CN106344566A (en)

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WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20170125

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