Starting from methylpheophorbide-a, a homologous series of purpurinimides containing alkyl substituents at two different positions [as 3-(1(1)-O-alkyl) and 13(2)-N-alkyl] were synthesized. These compounds with variable lipophilicity (log P 5.32-16.44) exhibit long wavelength absorption near lambda(max)700 nm (epsilon: 45 000 in dichloromethane) with singlet oxygen ((1)O2) production in the range of 57-60%. The shifts in in vivo absorptions and tumor/skin uptake of these compounds were determined in C3H mice bearing RIF tumors by in vivo reflectance spectroscopy. The results obtained from a set of photosensitizers with similar lipophilicity (log P 10.68-10.88) indicate that besides the overall lipophilicity, the presence and position of the alkyl groups (O-alkyl vs N-alkyl) in a molecule play an important role in tumor uptake, tumor selectivity, and in vivo PDT efficacy. At present, all purpurinimide analogues are being evaluated at various doses, and experiments are underway to establish a quantitative structure-activity relationship on a limited set of compounds. The 1D and 2D NMR and mass spectrometry analyses confirmed the structures of the desired purpurinimides and the byproducts formed during various reaction conditions. The mechanisms of the formation of the unexpected 12-formyl- and 12-(hydroxymethyl)purpurinimides under certain reaction conditions are also discussed.
Traditional approaches to ecosystem restoration have considered afforestation to be an important tool. To alleviate land degradation in China, the Chinese government has therefore invested huge amounts of money in planting trees. However, the results of more than half a century of large-scale afforestation in arid and semi-arid China have shown that when the trees are not adapted to the local environment, the policy does not improve the environment, and may instead increase environmental degradation. When precipitation is lower than potential evaporation, surface soil moisture typically cannot sustain forest vegetation, and shrubs or steppe species replace the forest to form a sustainable natural ecosystem that exists in a stable equilibrium with the available water supply. The climate of much of northwestern China appears to be unsuitable for afforestation owing to the extremely low rainfall. Although some smallscale or short-term afforestation efforts have succeeded in this region, many of the resulting forests have died or degraded over longer periods, so policymakers must understand that these small-scale or short-term results do not support an inflexible policy of large-scale afforestation throughout arid and semi-arid northwestern China. Rather than focusing solely on afforestation, it would be more effective to attempt to recreate natural ecosystems that are better adapted to local environments and that thus provide a better chance of sustainable, long-term rehabilitation.
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