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Anticancer analgesic selenium-containing compound and preparation method and application thereof
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A technology of selenium compounds and mixtures, applied in the field of medicine, can solve the problems of poor cancer pain effect and low analgesic intensity, etc.
Active Publication Date: 2015-02-04
SHENZHEN F&S BIO TECH
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[0010] Tetrahydropalmatine and its L-rotundine are non-addictive and suitable for patients who need to take analgesics for a long time, but the analgesic intensity is low and the effect on cancer pain is poor
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Embodiment 1
[0057] The preparation of embodiment 1 rotundine selenite
[0058] Weigh 22.2 grams of selenium dioxide, add 500 milliliters of deionized water to dissolve, add 71.1 grams of garotondine, stir and dissolve at room temperature. The solvent was removed by freeze-drying to obtain rotundine selenite.
[0059] Heavy water (D 2 O) in 1 HNMR: δ(ppm) 7.1580~7.1029(2H,d), 6.9560(1H,S), 6.8987(1H,S), 4.5006~4.3766(2H,dd), 4.1430~4.0978(1H,d), 3.9491~3.9104 (1H,p),3.8973(3H,s),3.8926(3H,s),3.8604(3H,s),3.8390(3H,s),3.7489~3.6513(1H,p),3.5014~3.4354(1H,p ), 3.3118~3.2563 (1H, p), 3.1589~2.9861 (2H, p).
[0060] Heavy water (D 2 O) in 77 SeNMR: δ (ppm) 32.27.
[0061] Element content: C, 52.01; H, 5.57; N, 2.91; O, 23.16; Se, 16.37; theoretical value: C, 52.07; H, 5.62; N, 2.89; O, 23.12;
Embodiment 2
[0062] The preparation of embodiment 2 dirotundine selenite
[0063] Weigh 22.2 grams of selenium dioxide, add 1000 milliliters of deionized water to dissolve, add 142.2 grams of garotondine, stir and dissolve at room temperature. The solvent was removed by freeze-drying to obtain dirotundine selenite.
[0064] Element content: C, 60.13; H, 6.20; N, 3.38; O, 21.02; Se, 9.45; theoretical value: C, 60.07; H, 6.24; N, 3.34; O, 20.96;
Embodiment 3
[0065] The preparation of embodiment 3 selenic acid
[0066] Dissolve 15 grams of selenium dioxide in 10 milliliters of water, add 500 grams of hydrogenperoxide with a content greater than 30%, reflux for 12 hours, then distill under reduced pressure at a pressure of 133.3 to 233.6 Pa to 433K for dehydration, and cool the obtained concentrated solution to 283 to 288K to add Solidselenic acidcrystal, the product is dried below 666.6Pa.
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Abstract
The invention relates to an anticancer analgesicselenium-containing compound and a preparation method and an application thereof. The structure of the selenium-containing compound is as shown in the general formula (I), wherein n=1 or 2, x=2 or 4; and chiral center (*) is R / S-(+ / -) or S-(-) configuration. The selenium-containing compound provided by the invention has anticancer and analgesic functions, has a more excellent analgesic effect than tetrahydropalmatine or rotundine, can be used in cancer pain, even cancer pain in middle and advanced stage, has no addition and can be used to effectively improve life quality of patients.
Description
technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a selenium-containing compound used for anti-cancer and analgesia, a preparation method and application thereof. Background technique [0002] Selenium is an essential trace element for the human body and has extremely important biological functions for health. Unlike other (semi)metals, selenium becomes part of the protein by a co-translational mechanism as part of selenocysteine, the 21st amino acid in human protein synthesis. Twenty-five selenoproteins have been identified in humans so far, yet only a few of their functions are understood. Most selenoproteins are involved in the regulation of antioxidant responses and redox states, especially the glutathioneperoxidase (GPxs) family and the thioredoxinreductase (TrxRs) family. Some selenoproteins also play more specific and essential roles, for example, thyroxine deiodinases (DIOs) are involved in the metabolis...
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