BackgroundArtemisinin is the current drug of choice for treatment of malaria and a number of other diseases. It is obtained from the annual herb, Artemisia annua and some microbial sources by genetic engineering. There is a great concern that the artemisinin production at current rate will not meet the increasing demand by the pharmaceutical industry, so looking for additional sources is imperative.MethodsIn current study, artemisinin concentration was analysed and compared in the flowers, leaves, roots and stems of Artemisia annua and 14 other Artemisia species including two varieties each for Artemisia roxburghiana and Artemisia dracunculus using high performance liquid chromatography (HPLC).ResultsThe highest artemisinin concentration was detected in the leaves (0.44 ± 0.03%) and flowers (0.42 ± 0.03%) of A. annua, followed by the flowers (0.34 ± .02%) of A. bushriences and leaves (0.27 ± 0%) of A. dracunculus var dracunculus. The average concentration of artemisinin varied in the order of flowers > leaves > stems > roots.ConclusionThis study identifies twelve novel plant sources of artemisinin, which may be helpful for pharmaceutical production of artemisinin. This is the first report of quantitative comparison of artemisinin among a large number of Artemisia species.
The use of soluble cocrystal for delivering drugs with low solubility, although a potentially effective approach, often suffers the problem of rapid disproportionation during dissolution, which negates the solubility advantages offered by the cocrystal. This necessitates their robust stabilization in order for successful use in a tablet dosage form. The cocrystal between carbamezepine and succinic acid (CBZ-SUC) exhibits a higher aqueous solubility than its dihydrate, which is the stable form of CBZ in water. Using this model system, we demonstrate an efficient and material-sparing tablet formulation screening approach enabled by intrinsic dissolution rate measurements. Three tablet formulations capable of stabilizing the cocrystal both under accelerated condition of 40 °C and 75% RH and during dissolution were developed using three different polymers, Soluplus® (F1), Kollidon VA/64 (F2) and Hydroxypropyl methyl cellulose acetate succinate (F3). When compared to a marketed product, Epitol® 200 mg tablets (F0), drug release after 60 min from formulations F1 (∼82%), F2 (∼95%) and F3 (∼95%) was all higher than that from Epitol® (79%) in a modified simulated intestinal fluid. Studies in albino rabbits show correspondingly better bioavailability of F1-F3 than Epitol.
In the present study, we examined the potential role of paclobutrazol in delaying leaf senescence, in causing changes in the activities of antioxidants, and in the maintenance of photosynthetic activity during the senescence process, and, therefore, on the grain yield of maize under semiarid field conditions. Maize seeds were pretreated with 0 (CK), 200 (PS1), 300 (PS2), and 400 (PS3) mg paclobutrazol L−1. Our results indicated that elevated levels of reactive oxygen species (ROS) and higher accumulation of malondialdehyde (MDA) contents were positively associated with accelerated leaf senescence during the grain-filling periods. The leaf senescence resulted in the disintegration of the photosynthetic pigments and reduced the net photosynthetic rate after silking. However, the resultant ROS burst (O2− and H2O2) was lessened and the leaf senescence and chlorophyll degradation were evidently inhibited in leaves of paclobutrazol-treated maize plants, which was strongly linked with upregulated activities of antioxidant enzymes in treated plants. The enhanced chlorophyll contents and availability of a greater photosynthetic active green leaf area during the grain filling period facilitated the maintenance of higher photosynthetic rate, and light-harvesting efficiency of photosynthesis associated with photosystem II (PSII) resulted in higher kernel number ear−1 and thousand kernel weights, and thus increased the final grain yield. The average maize grain yield was increased by 18.8% to 55.6% in paclobutrazol treatments, compared to untreated control. Among the various paclobutrazol treatments, PS2 (300 mg L−1) treatment showed the most promising effects on enhancing the activities of antioxidative enzymes, delaying leaf senescence and improving the yield of maize. Thus, understanding this effect of paclobutrazol on delaying leaf senescence introduces new possibilities for facilitating yield improvement of maize under semiarid conditions.
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