METHODS: Different combinations of nitrogen sources, salts and pre-culture combinations were applied in the fermentation media and lovastatin yield was analysed chromatographically.
RESULT: The exclusion of MnSO4 ·5H2O, CuSO4·5H2O and FeCl3·6H2O were shown to significantly improve lovastatin production (282%), while KH2PO4, MgSO4·7H2O, and NaCl and ZnSO4·7H2O were indispensable for good lovastatin production. Simple nitrogen source (ammonia) was unfavourable for morphology, growth and lovastatin production. In contrast, yeast extract (complex nitrogen source) produced the highest lovastatin yield (25.52 mg/L), while powdered soybean favoured the production of co-metabolites ((+)-geodin and sulochrin). Intermediate lactose: yeast extract (5:4) ratio produced the optimal lovastatin yield (12.33 mg/L) during pre-culture, while high (5:2) or low (5:6) lactose to yeast extract ratio produced significantly lower lovastatin yield (7.98 mg/L and 9.12 mg/L, respectively). High spore concentration, up to 107 spores/L was shown to be beneficial for lovastatin, but not for co-metabolite production, while higher spore age was shown to be beneficial for all of its metabolites.
CONCLUSION: The findings from these investigations could be used for future cultivation of A. terreus in the production of desired metabolites.
OBJECTIVE: The objective of this study is to evaluate the anti-cancer potential of the novel class of quinazoline tethered acetamide derivatives against six different cancer cell lines.
METHOD: A novel series of various substituted quinazolinone acetamides were synthesized through a feasible scheme. The synthetic scheme involves the conversion of benzoxazinone (from anthranilic acid and benzoyl chloride) intermediate to 3-amino quinazoline-4-one which is further converted to the final amide by tethering with the propionyl chloride employing Schotten-Baumann Reaction conditions. All the synthesized derivatives characterized by IR, 1HNMR and MASS spectral methods and anti-cancer activity evaluated by employing MTT assay for six cancer cell lines and one normal human cell line.
RESULTS: All the synthesized compounds were screened for anti-cancer activity against six cancer cell lines, including A 549 (lung), DU 145 (prostate), HT 29 (colon), MCF-7 (breast), SiHA (cervical), B16F10 (mouse skin melanoma) and one normal human fibroblast cell lines. All the compounds displayed a decent cytotoxicity profile when compared with the standard drug, doxorubicin. Among the synthesized compounds (5a to 5n) tested, two compounds, 5f and 5g have demonstrated excellent cytotoxicity against SiHA and MCF-7 cancer cell lines.
CONCLUSION: Comparatively, most of the compounds displayed decent cytotoxicity potential relative to the standard drug, doxorubicin. Further investigations are needed to establish the detailed mechanism of action of the developed novel quinazolinone acetamides.
Methods: A prospective observational study including 223 patients receiving the branded medicine Exjade® and 101 patients receiving the copy Osveral® was carried out. Data were assessed for a 1-year period and included clinical symptoms, serum ferritin (SF), serum creatinine (SC), and alanine aminotransferase (ALT). Data were analyzed with SPSS version 22 software (SPSS, Chicago, IL, USA).
Results: The median age of the sample was 8 years. There was no significant difference in gender distribution between the two groups (p = 0.625). Nausea was the most frequently reported adverse effect followed by diarrhea and abdominal pain in both groups. Patients receiving Exjade® had a higher relative reduction of SF at the end of the study compared with the Osveral® group (19.9% versus 9.93%, p = 0.028). SC was found to be significantly higher in the Osveral® group than in the Exjade® group throughout the study period. The mean platelet count was higher in the Exjade® group. ALT was significantly higher among patients receiving Osveral® over the last three months of the study.
Conclusions: Exjade® showed a better ability to reduce SF, with less liver toxicity, and better hemostasis profile. No congenital anomalies associated with short-term use of both drugs during pregnancy were observed or reported.