Safe natural pharmaceutical composition for treating cancer
OwnerYaguang Liuinventor
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Abstract
The present invention related to the natural drug of Homoharringtonine (HHT) combined with other ingredients which include Matrine (MAT), Apigenin (APN), Yejuhua lactone (YLE), Lipopolysaccharide of Kelp (LIK), Puerarin (PUN) and Indirubin (IND) for diverting human cancer cells to closely normal cells, inducing apoptosis of cancer cells and inhibiting cancer cells. Specifically, this invention provides a new method for producing HHT and other ingredients
Claims72
A safe natural drug comprises Homoharringtonine (HHT) or HHT combined with other ingredients, which include Matrine (MAT), Apigenin (APN), Yejuhua lactone (YLE), Lipopolysaccharide of Kelp (LIK), Puerarin (PUN) and Indirubin (IND), for diverting human cancer cells to resemble normal cells, inducing apoptosis of cancer cells and inhibiting cancer growth
25 A safe natural drug of claim 1, wherein the amount sufficient to inhibit cancer cells proliferation, is 1-5 mg/m2 by infusion through venous or injection of HHT and added about 25˜250 mg of APN orally
28 A safe natural drug of claim 1, wherein the amount sufficient to inhibit cancer cells proliferation, is 1-5 mg/m2 by infusion through venous or injection of HHT and added about 25˜250 mg of PUN orally
32 A safe natural drug of claim 1, wherein the amount sufficient to inhibit transplanted tumor is 1-5 mg/m2 by infusion through venous or injection of HHT and added about 25-250 mg of YLE orally
43 A safe natural drug of claim 1, wherein the amount sufficient to inhibit tumor incidence in vivo is about 1-5 mg/m2 by infusion through venous or injection of HHT and added about 25˜250 mg of APN orally
45 A safe natural drug of claim 1, wherein the amount sufficient to inhibit tumor incidence in vivo is about 1-5 mg/m2 by infusion through venous or injection of HHT and added about 25˜250 mg of LIN orally
46 A safe natural drug of claim 1, wherein the amount sufficient to inhibit tumor incidence in vivo is about 1-5 mg/m2 by infusion through venous or injection of HHT and added about 25˜250 mg of PUN orally
50 A safe natural drug of claim 1, wherein the amount sufficient to inhibit carcinogen-DNA binding is about 1-5 mg/m2 by infusion through venous or injection of HHT and added about 25˜250 mg of YLE orally.
52 A safe natural drug of claim 1, wherein the amount sufficient to inhibit carcinogen-DNA binding is about 1-5 mg/m2 by infusion through venous or injection of HHT and added about 25˜250 mg of PUN orally
56 A safe natural drug of claim 1, wherein the amount sufficient to inhibit peroxidation is about 1-5 mg/m2 by infusion through venous or injection of HHT and added about 25˜250 mg of YLE orally.
57 A safe natural drug of claim 1, wherein the amount sufficient to inhibit peroxidation is about 1-5 mg/m2 by infusion through venous or injection of HHT and added about 25˜250 mg of LIK orally.
59 A safe natural drug of claim 1, wherein the amount sufficient to inhibit peroxidation is about 1-5 mg/m2 by infusion through venous or injection of HHT and added about 25˜250 mg of IND orally
60 A process for producing natural pharmaceutical composition in accordance with claim 1 wherein said producing Matrine (MAT) comprising:
- (a) extracting the dried powder of root of Sophora flavescens Alt with methanol;
- (b) filtering the extract,
- (c) concentrating the filtrate and residue was obtained,
- (d) residue was dissolved in HCI and adjusted pH to 3 5;
- (e) NaOH was added to HCI solution and adjusted pH to 13;
- (f) solution of pH 13 was extracted by CH2Cl2,
- (g) CH2Cl2 was recovered under reduced pressure and residue was dissolved in CHCl3;
- (h) adding diethyl ether to CHCl3 and then mixture was filtered,
- (i) filtrate was concentrated and syrup was obtained;
- (j) the syrup was chromatographic column packed with alumina again;
- (k) column as eluted with oil ether-acetone,
- (l) elution was concentrated and residue obtained,
- (m) acetone was added to residue and crystallized;
- (o) crystals were recrystallized in acetone;
- and
- (p) crystals were dried under vacuum;
61 A process for producing natural pharmaceutical composition in accordance with claim 1 wherein said producing Apiin (APN) comprising
- (a) extracting the dried powder of Apium graveolens L with cold ethanol,
- (b) extract was filtrated,
- (c) filtrate (1) was concentrated under reduced pressure and filtrated,
- (c) filtrate (2) was cooled and precipitate was obtained,
- (e) precipitate was washed by diethyl ether and acetone;
- (f) precipitate was dissolved in hot water;
- (g) Pb (OAC)2 was added to hot water and precipitate was formed;
- (h) the mixture was filtered;
- (i) NaOH was added to filtrate and precipitate was formed,
- (j) precipitate was washed with water and suspended on EtOH;
- (k) H2S was gassed to suspension of EtOH and filtered;
- (l) filtrate was concentrated under reduced pressure and crystals were formed;
- (m) crystals were refined by recrystallization in cold ethanol;
- and
- (n) crystals were dried under vacuum
62 A process for producing natural pharmaceutical composition in accordance with claim 1 wherein said producing Indirubin (IND) comprising:
- (a) dried powder of Baphicanthus cusia (Ness) Bremek, or Isatis tinctoria L, or Isatis indigotica Fort, or Polygonum tinctorium Ait was extracted with hot water,
- (b) extract was filtered and filtercake extracted with methanol,
- (c) methanol was recovered under reduced pressure and residue obtained,
- (d) the residue was extracted with chloroform,
- (e) the chloroform was recovered and residue was chromatographed on silica gel;
- (f) silica gel eluted by chloroform,
- (g) chloroform was concentrated and crystals were obtained,
- (h) crystals were refined by recrystallization in chloroform, and
- (i) crystals were dried under vacuum.
A method of extracting homoharringtonine (HHT) from cultured plant tissue and natural plant material that contains HHT, comprising the steps of:
- Contacting the plant material for a selected period of time with a solvent whereby at least some of said HHT is soluble and transported into said solvent thereby forming a crude extract;
- Adjusting said pH of crude extract for specifically separating said crude HHT,
- Desorbing said crude HHT sequentially from said adsorbent from said adsorbent by flowing a series of eluant mixtures making up a step gradient elution over said column and collecting each of individual eluant mixtures of said step gradient elution flowing through said column wherein each of said individual eluant mixture contains pure HHT compound.
71 A process for producing KHT by semi-synthesis comprising:
- (a) extracting a ground cultured plant tissue or plant selected from the group consisting of Cephalotaxus fortunei Hook, C sinensis Li, C hainanensis, C wilsoniana and other Cephalotaxus species with 90% ethanol at room temperature for 24 hours;
- (b) the ethanol was recovered under reduced pressure;
- (c) tartaric acid was added to concentrated ethanol solution,
- (d) ammonia water was added to acidic solution and adjusted pH to 9;
- (e) pH 9 solution was filtered and yielded filtrate,
- (f) filtrate was extracted with CHCl3;
- (g) CHCl3 was recovered and residue was obtained;
- (h) residue was chromatographed packed with alumna and eluted by CHCl3-MeOH;
- (i) elute was concentrated under reduced pressure and residue was dried under vacuum;
- and
- (j) the dried residue is Cephalotaxus (CEP), which used for semi-synthesis of HHT.
The method of claim 71, wherein said semi-synthesis of HHT comprising:
- (a) benzene-α-acetone-Na was put into benzene;
- (b) mixture was stirred then was dissolved in pyridine at stirred at 0° C.;
- (c) oxalic chloride was added to solution of pyridine,
- (d) solution warmed to room temperature and stand overnight;
- (e) the solution was added to CH2Cl2 and cooled to 0° C.;
- (f) CEP and pyridine were added to cold CH2Cl2 solution,
- (g) Mixture (2) was washed with 10% Na2CO3 and saturated NaCl solution;
- (h) Solvents were evaporated and solid α-ketoester-harringtonine obtained;
- (i) CH3CHBrCOOEt and activated zin dust were added to α-ketoester-harringtonine and mixture (3) was obtained,
- (j) CHCH3 and H2O and solid Na2CO3 were added to the mixture (3),
- (k) CHCl3 was evaporated under reduced pressure and residue was obtained;
- (l) the residue was chromatography picked with alumina;
- (m) column eluted with chloroform and followed by chloroform-methanol;
- (n) solvents were recovered under reduced pressure and solid was obtained;
- (o) solid was dissolved in ethanol,
- (p) ethanol was recovered under reduced pressure and crystals were obtained;
- (q) crystals were recrystallized in diethyl ether;
- (r) crystals were dried under vacuum, and
- (s) the product is HHT.
Dependencies are inferred from the claim text.