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Compound separated from gamboge resin and derivative thereof and pharmaceutical composition comprising compound and derivative

A compound, technology from Garcinia cambogia, applied in the field of novel compounds and their derivatives

Active Publication Date: 2015-01-07
TAIWAN SUNPAN BIOTECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0019] It can be seen that the above-mentioned existing gamboge resin obviously still has inconvenience and defects in methods, products and use, and needs to be further improved urgently
In order to solve the above-mentioned problems, the relevant manufacturers have tried their best to find a solution, but no suitable design has been developed for a long time, and there is no suitable method for general methods and products to solve the above-mentioned problems. This is obvious. It is a problem that relevant industry players are eager to solve

Method used

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  • Compound separated from gamboge resin and derivative thereof and pharmaceutical composition comprising compound and derivative
  • Compound separated from gamboge resin and derivative thereof and pharmaceutical composition comprising compound and derivative
  • Compound separated from gamboge resin and derivative thereof and pharmaceutical composition comprising compound and derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0244] Example 1. Analytical grade (analytical) reversed phase high performance liquid chromatography (reversed phase high performance liquid chromatography, RP-HPLC) analysis of the acetone extraction product TSB-14 of garcinia resin

[0245] This experiment mainly analyzes the acetone extraction product TSB-14 of gamboge resin obtained in Example 1 of a Taiwan patent case TW I282280 (corresponding to US7,138,428 B2 and CN 100413868 C) of the applicant. Grade RP-HPLC, in order to further confirm that the acetone extraction product TSB-14 of garcinia resin contains those components.

[0246] The acetone extraction product TSB-14 of the garcinia cambogia resin of 1.0 mg was dissolved in 1 mL of acetone, and carried out analytical grade RP-HPLC according to the method described in the "general operating procedure" above, and obtained as figure 1 Analytical RP-HPLC elution profile shown.

[0247] From figure 1 It can be seen that the acetone extraction product TSB-14 of garci...

Embodiment 2

[0248] Example 2. Preparation of Purified Compounds Derived from Acetone Extracted Products of Garcinia Resin

[0249] The semi-preparative grade RP-HPLC of the acetone extraction product TSB-14 of A, garcinia resin:

[0250] The acetone extraction product TSB-14 of 3 g of garcinia resin was dissolved in 30 mL of acetone / acetonitrile (v / v=1:9), and the semi-preparative RP- HPLC, wherein the mobile phase is 0.05% TFA aqueous solution / 65% acetonitrile=35:65. The resulting semi-prep RP-HPLC elution profile is shown in figure 2 middle. Will figure 2 with the above embodiment 1 figure 1 After a comparison, it can be clearly seen that the peaks 1 to 35 are in the figure 2 s position. The applicant divides these 35 peaks into 3 sections (sections) (that is, section 1 to section 3), wherein section 1 contains peaks 1 to 12, and the residence time is from the 0th to the 42nd minute; Section 2 contains peaks 13 to 24 with residence times from 42 to 135 minutes; and section 3 ...

Embodiment 3

[0273] Example 3. Characterization of Compounds Purified from Fraction 1 to Fraction 3

[0274] The 35 products derived from the separation part 1 to the separation part 3 obtained in the above Example 2 were analyzed according to the method described in the above "general operating procedure" for physical and chemical properties, including melting point, 1H-NMR, 13C -NMR, homonuclear correlation spectroscopy (1H-1H COZY), heteronuclear multiple-quantum coherence (HMQC), heteronuclear multiple-bond coherence (HMBC), nuclear Overhauser Effect spectroscopy (nuclearOverhauser effect spectroscopy, NOESY), EIMS, HREIMS, FABMS and HRFABMS. The experimental data obtained are summarized as follows:

[0275] 1. Product Gh-47:

[0276] The measured properties of the product Gh-47 are as follows:

[0277] Yellow flaky crystal, melting point: 204-209°C.

[0278] EIMS m / z (relative intensity): 560[M]+(100), 545(47), 532(22), 517(36), 405(44), 389(11), 363(24), 349( 17), 307(12), 287(2...

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Abstract

The present invention relates to a compound isolated from gamboge resin and its derivatives, as well as pharmaceutical compositions containing these compounds and derivatives, and discloses a novel compound with the following chemical formula (I): wherein each substituent Definitions are as defined in the specification and claims. Also disclosed are the uses of these compounds, an acetone extraction product of Garcinia cambogia resin, and fractions obtained from the acetone extraction product, for the preparation of pharmaceutical compositions.

Description

technical field [0001] The present invention relates to one, concerning 5 isolated fractions from an acetone-extracted product of gamboge resin, and 18 novel novel Compounds and derivatives thereof, especially related to one of the isolated parts and the novel compounds proved to have tumor / cancer cell growth inhibiting activity. The acetone extract and the fractions have also been shown to have analgesic and anti-inflammatory activities. Also pertaining to the acetone extraction product, the fractions and the novel compounds and their derivatives. Background technique [0002] Gamboge resin is a gum-resin secreted by the plant of Garcinia sp. in the family Guttiferae. It has been used as a vegetable dye and pigment since ancient times. The source is also folk medicine (folk-medicine) in some regions such as India and Thailand. [0003] Gamboge (Latin scientific name: Garcinia morell Desv; Chinese pinyin is TENGHUANG; English name gamboge) is an evergreen tree that grows...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/20A61K31/352A61P35/00A61P29/00A61P35/02
Inventor 李森彬
Owner TAIWAN SUNPAN BIOTECH DEV