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1.
J Skin Cancer ; 2020: 9061532, 2020.
Article in English | MEDLINE | ID: mdl-32411476

ABSTRACT

BACKGROUND: Skin cancer is a growing health concern worldwide. It is the most common malignancy in South Africa and places a large burden on the public healthcare sector. There is a paucity of published scientific data on skin cancer in South Africa. OBJECTIVES: To report the findings of biopsies performed in patients with suspected skin cancer attending the Tygerberg Academic Hospital (TAH) Dermatology outpatient department (OPD) in the Western Cape Province of South Africa. Methodology: A retrospective chart review identified all patients who underwent a biopsy for a suspected skin cancer diagnosis between September 2015 and August 2016 at the TAH dermatology OPD. RESULTS: A total number of 696 biopsies from 390 participants were identified, of which 460 were histologically confirmed as malignant lesions. The proportion of clinically suspected skin cancers that were histologically confirmed as cancer was 68%. The most commonly occurring malignancies were basal cell carcinoma (BCC) (54.8%), squamous cell carcinoma (SCC) (18.9%), squamous cell carcinoma in-situ (SCCI) (8.0%), Kaposi's sarcoma (KS) (6.7%), malignant melanoma (MM) (6.1%), and keratoacanthoma (KA) (4.6%). The number needed to treat (NTT) for all cancers diagnosed and for MM was 1.5 and 4 respectively. BCC (89.3%) and KS (67.7%) was the most common skin cancer in the white and black population respectively. The ratio of BCC to SCC was 2.03. CONCLUSION: This study provides valuable scientific data on the accuracy of skin cancer diagnosis, distribution and patient demographics in the Western Cape Province of South Africa, on which further research can be based. The study highlights the burden of skin cancer on this specific population group and calls for standardised reporting methods and increased surveillance of skin cancers.

2.
J Pharm Pharmacol ; 63(2): 278-86, 2011 Feb.
Article in English | MEDLINE | ID: mdl-21235593

ABSTRACT

OBJECTIVES: The aim of this study was to synthesize a series of ethylene glycol ether derivatives of the antimalarial drug artemisinin, determine their values for selected physicochemical properties and evaluate their antimalarial activity in vitro against Plasmodium falciparum strains. METHODS: The ethers were synthesized in a one-step process by coupling ethylene glycol moieties of various chain lengths to carbon C-10 of artemisinin. The aqueous solubility and log D values were determined in phosphate buffered saline (pH 7.4). The derivatives were screened for antimalarial activity alongside artemether and chloroquine against chloroquine-sensitive (D10) and moderately chloroquine-resistant (Dd2) strains of P. falciparum. KEY FINDINGS: The aqueous solubility within each series increased as the ethylene glycol chain lengthened. The IC50 values revealed that all the derivatives were active against both D10 and Dd2 strains. All were less potent than artemether irrespective of the strain. However, they proved to be more potent than chloroquine against the resistant strain. Compound 8, featuring three ethylene oxide units, was the most active of all the synthesized ethers. CONCLUSIONS: The conjugation of dihydroartemisinin to ethylene glycol units of various chain lengths through etheral linkage led to water-soluble derivatives. The strategy did not result in an increase of antimalarial activity compared with artemether. It is nevertheless a promising approach to further investigate and synthesize water-soluble derivatives of artemisinin that may be more active than artemether by increasing the ethylene glycol chain length.


Subject(s)
Antimalarials/chemical synthesis , Antimalarials/pharmacology , Artemisinins/chemical synthesis , Artemisinins/pharmacology , Ethylene Glycols/chemical synthesis , Ethylene Glycols/pharmacology , Plasmodium falciparum/drug effects , Antimalarials/chemistry , Artemether , Artemisinins/chemistry , Chloroquine/pharmacology , Ethers/chemical synthesis , Ethers/chemistry , Ethers/pharmacology , Ethylene Glycols/chemistry , Solubility
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