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Title:
COMPOSITIONS DERIVED FROM GALENIA AFRICANA AND METHODS OF USE FOR CANCER TREATMENT
Document Type and Number:
WIPO Patent Application WO/2018/116146
Kind Code:
A1
Abstract:
The present invention discloses a cancer treatment method which includes the step of treating a patient having cancer with an extract from Galenia Africana L. plant. The extract may include pinocembrin and/or 2',4' dihydroxychalcone and/or 7- hydroxyflavanone. The cancer may be breast cancer or melanoma. The composition may be solubilized with MPG and/or Suganate.

Inventors:
BARRY MICHAEL-JOHN JOSEPH (NZ)
Application Number:
PCT/IB2017/058097
Publication Date:
June 28, 2018
Filing Date:
December 19, 2017
Export Citation:
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Assignee:
BIOPHARM NZ LTD (NZ)
GERNTHOLTZ OTTO CARL (ZA)
International Classes:
A61K36/36; A61K31/12; A61K31/353; A61P35/00
Other References:
TICHA LA ET AL.: "Phytochemical and Antimicrobial Screening of Flavanones and Chalcones from Galenia africana and Dicerothamnus rhinocerotis", NAT PROD COMMUN, vol. 10, no. 7, 2015, pages 1185 - 1190, XP055510011
MATIVANDLELA SP ET AL.: "Antimycobacterial flavonoids from the leaf extract of Galenia africana", J NAT PROD., vol. 72, no. 12, 2009, pages 2169 - 2171, XP055510011
GHANI NA ET AL.: "Chemical Constituents and Cytotoxic Activity of Polyalthia cauliflora var. cauliflora", RESEARCH JOURNAL OF MEDICINAL PLANT, vol. 6, no. 1, 2012, pages 74 - 82, XP055510039
SURESH KUMAR MA ET AL.: "Pinocembrin Triggers Bax-dependent Mitochondrial Apoptosis in Colon Cancer Cells", MOLECULAR CARCINOGENESIS, vol. 46, no. 3, 2007, pages 231 - 241, XP002760349
LOU C ET AL.: "2 ,4 -Dihydroxychalcone-induced apoptosis of human gastric cancer MGC- 803 cells via down-regulation of survivin mRNA", TOXICOLOGY IN VITRO, vol. 24, no. 5, 2010, pages 1333 - 1337, XP027080408
YANG S ET AL.: "Antimetastatic potentials of flavones on oral cancer cell via an inhibition of matrix-degrading proteases", ARCHIVES OF ORAL BIOLOGY, vol. 53, no. 3, 2008, pages 287 - 294, XP022450646
ZAKI MA ET AL.: "Bioactive Formylated Flavonoids from Eugenia rigida: Isolation, Synthesis, and X-ray Crystallography", JOURNAL OF NATURAL PRODUCTS, vol. 79, September 2016 (2016-09-01), pages 2341 - 2349, XP055510055
TAN KW ET AL.: "Identification of novel dietary phytochemicals inhibiting the efflux transporter breast cancer resistance protein (BCRP/ABCG2)", FOOD CHEMISTRY, vol. 138, no. 4, 2013, pages 2267 - 2274, XP028996511
CHEN Z ET AL.: "Antiproliferative and apoptotic effects of pinocembrin in human prostate cancer cells", BANGLADESH J PHARMACOLOGY, vol. 8, no. 3, 2013, pages 255 - 262, XP055510063
RASUL A ET AL.: "Pinocembrin: A Novel Natural Compound with Versatile Pharmacological and Biological Activities", BIOMED RESEARCH INTERNATIONAL, vol. 2013, 2013, pages 1 - 9, XP055510074
CHEN K ET AL.: "Pinocembrin suppresses TGF-beta1-induced epithelial mesenchymal transition and metastasis of human Y-79 retinoblastoma cells through inactivating alphavbeta3 integrin/FAK/p38a signaling pathway", CELL & BIOSCIENCE, vol. 4, no. 41, 2014, pages 1 - 13, XP021193547
AWASTHI, M. ET AL.: "Molecular docking and 3D-QSAR-based virtual screening of flavonoids as potential aromatase inhibitors against estrogen-dependent breast cancer", JOURNAL OF BIOMOLECULAR STRUCTURE AND DYNAMICS, vol. 33, no. 4, 2015, pages 804 - 819, XP055510098
BENGUEDOUAR, L. ET AL.: "Ethanolic Extract of Algerian Propolis and Galangin Decreased Murine Melanoma Tumour Progression", ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY, vol. 16, no. 9, 2016, pages 1172 - 1183, XP055510105
See also references of EP 3558333A4
Attorney, Agent or Firm:
GERNTHOLTZ, Otto Carl (ZA)
Download PDF:
Claims:
PATENT CLAIMS

1 . A cancer treatment method which includes the step of treating a patient having cancer with an extract from Galenia Africana L. plant.

2. A method as claimed in claim 1 , in which the extract includes pinocembrin and/or 2', 4' dihydroxychalcone and/or 7-hydroxyflavanone.

3. A method as claimed in claim 1 or claim 2, in which the cancer is breast cancer.

4. A method as claimed in claim 1 or claim 2, in which the cancer is melanoma.

5. A cancer treatment composition which includes an extract from Galenia Africana L. plant.

6. A composition as claimed in claim 5, in which the extract includes pinocembrin and/or 2', 4' dihydroxychalcone and/or 7-hydroxyflavanone.

7. A composition as claimed in claim 5 or claim 6, in which the cancer is breast cancer.

8. A composition as claimed in claim 5 or claim 6, in which the cancer is melanoma.

9. A composition as claimed in any one of claims 5 to 8, which is solubilized.

10. A composition as claimed in claim 9, in which the composition is solubilized with MPG and/or Suganate.

1 1 . A cancer treatment method substantially as hereinbefore described.

12. A cancer treatment composition substantially as hereinbefore described.

Description:
COMPOSITIONS DERIVED FROM GALENIA AFRICANA AND METHODS

OF USE FOR CANCER TREATMENT

FIELD OF INVENTION

The present invention relates to a cancer treatment method and composition.

More particularly, the present invention relates to a cancer treatment method and composition for treating breast cancer and melanoma.

BACKGROUND TO INVENTION

Kraalbos (KB) extracts from Galenia Afhcana L. plant are known to be rich in pinocembrin, 2', 4' dihydroxychalcone, 7-hydroxyflavanone and 2', 4' dihydroxydihydrochalcone compounds. These molecules have previously been shown to exhibit varying degrees of cytotoxity on cancer cells.

It is an object of the invention to suggest a novel cancer treatment method and composition which includes an extract of Galenia Afhcana.

SUMMARY OF INVENTION

According to the invention, a cancer treatment method includes the steps of treating a patient having cancer with an extract from Galenia Afhcana L. plant.

Also according to the invention, a cancer treatment composition includes an extract from Galenia Afhcana L. plant The extract may include pinocembrin and/or 2', 4' dihydroxychalcone and/or 7- hydroxyflavanone.

The cancer may be breast cancer.

The cancer may be melanoma.

The composition may be solubilized.

The composition may be solubilized with MPG and/or Suganate. DETAILED DESCRIPTION OF INVENTION

The invention will now be described by way of example.

According to the invention, a cancer treatment method includes the steps of treating a patient having cancer with an extract from Galenia Africana L. plant.

Also according to the invention, a cancer treatment composition includes an extract from Galenia Africana L. plant

The extract may include pinocembrin and/or 2', 4' dihydroxychalcone and/or 7- hydroxyflavanone.

The cancer may be breast cancer.

The cancer may be melanoma.

The composition may be solubilized. The composition may be solubilized with MPG and/or Suganate. Experiment 1

The objective of the experiment was to test the role of Galenia Africana (GA) extracts on the proliferation of MCF-7 human breast cancer cells. Cells were treated with B1 , B2, B3, D1 , D1 B2 or D1 B3. D1 exhibited the most cytotoxicity (IC50 of 26.53 ug/ml), followed by B2 (IC50 of 32.28 ug/ml). Based on the chemical composition of these extracts, it is clear that those that contain high levels of 2', 4' dihydroxychalcone have the most effect. Indeed, a combination of D1 and B3 at 50:50 ratio had minimal effect as compared to a combination of D1 and B2 at 70:30 ratio.

The results are shown below:

Experiment 2

The objective of the experiment was to test the role of Galenia Africana extracts on the proliferation of MCF-7 human breast cancer cells.

The results are shown below:

MCF-7 human breast cancer cells treated with GA extracts (MTT Assay 1 )

The following figure depicts ME1402 human melanoma cells treated with GA extracts after 48 hrs of incubation. Mean cell survival calculated as percentage of the mean vehicle control.

The following figure depicts MCF12A human breast cells treated with KB extracts after 48 hrs of incubation. Mean cell survival calculated as percentage of the mean vehicle control.