Kochia sieversiana (Pall.) C. A. M., a naturally alkali-resistant halophyte, was chosen as the test organism for our research. The seedlings of K. sieversiana were treated with varying (0-400 mM) salt stress (1:1 molar ratio of NaCl to Na 2 SO 4 ) and alkali stress (1:1 molar ratio of NaHCO 3 to Na 2 CO 3 ). The concentrations of various solutes in fresh shoots, including Na + , K + , Ca 2+ , Mg 2+ , Cl À , SO 4 2À , NO 3 À , H 2 PO 3 À , betaine, proline, soluble sugar (SS), and organic acid (OA), were determined. The water content (WC) of the shoots was calculated and the OA components were analyzed. Finally, the osmotic adjustment and ion balance traits in the shoots of K. sieversiana were explored. The results showed that the WC of K. sieversiana remained higher than 6 [g g À1 Dry weight (DW)] even under the highest salt or alkali stress. At salinity levels >240 mM, proline concentrations increased dramatically, with rising salinity. We proposed that this was not a simple response to osmotic stress. The concentrations of Na + and K + all increased with increasing salinity, which implies that there was no competitive inhibition for absorption of either in K. sieversiana. Based on our results, the osmotic adjustment feature of salt stress was similar to that of alkali stress in the shoots of K. sieversiana. The shared essential features were that the shoots maintained a state of high WC, OA, Na + , K + and other inorganic ions, accumulated largely in the vacuoles, and betaine, accumulated in cytoplasm.On the other hand, the ionic balance mechanisms under both stresses were different. Under salt stress, K. sieversiana accumulated OA and inorganic ions to maintain the intracellular ionic equilibrium, with close to equal contributions of OA and inorganic ions to anion. However, under alkali stress, OA was the dominant factor in maintaining ionic equilibrium. The contribution of OA to anion was as high as 84.2%, and the contribution of inorganic anions to anion was only 15.8%. We found that the physiological responses of K. sieversiana to salt and alkali stresses were unique, and that mechanisms existed in it that were different from other naturally alkaliresistant gramineous plants, such as Aneurolepidium chinense, Puccinellia tenuiflora.
Effects of salt and alkali stresses on growth, osmotic adjustment and ionic balance of Suaeda glauca (Bge.), an alkali-resistant succulent halophyte, were compared. The results showed that alkali stress clearly inhibited the growth of S. glauca. Moreover, the concentrations of Na + and K + both increased with increasing salinity under both stresses, suggesting no competitive inhibition between absorptions of Na + and K + . The mechanism underlying osmotic adjustment during salt stress was similar to alkali stress in shoots. The shared essential features were that organic acids, betaine and inorganic ions (dominated by Na + ) mostly accumulated. On the other hand, the mechanisms governing ionic balance under both stresses were different. Under salt stress, S. glauca accumulated organic acids and inorganic anions to maintain the intracellular ionic equilibrium, but the anion contribution of inorganic ions was greater than that of organic acids. However, the concentrations of inorganic anions under alkali stress were significantly lower than those under salt stress of the same intensity, suggesting that alkali stress might inhibit uptake of anions, such as NO 3 -and H 2 PO 4 -. Under alkali stress, organic acids were the dominant factor in maintaining ionic equilibrium. The contribution of organic acids to anions was 74.1%, while that of inorganic anions was only 25.9%. S. glauca enhanced the synthesis of organic acids, dominated by oxalic acid, to compensate for the shortage of inorganic anions.
The stress conditions of salt-alkalinized soil were simulated to investigate the features and acting factors of saltalkaline mixed stress, using a natural salt-alkaline tolerant grass Aneurolepidium chinense (Trin.) Kitag. According to the features of salt-alkalinized soil in the northeast of China, various salt-alkali conditions with different salinities and pHs were established by mixing NaCl, NaHCO 3 , Na 2 SO 4 , and Na 2 CO 3 , in various proportions. The treatments included a salt concentration range of 50 to 350 mM and pH values from 7.14 to 10.81. Seedlings of A. chinense were stressed under these salt-alkali conditions. Several physiological indices of seedling stress were determined, including survival rate, tillering rate, number of rhizomes, relative growth rate (RGR), proline content, electrolyte leakage rate, and Na + and K + content, in order to analyze the characteristics of the stresses due to the salt-alkali mixes and their main stress factors.The results showed that the survival rate, tillering rate, number of rhizomes, RGR, and K + content of A. chinense decreased with increasing salinity and pH (or alkalinity). Proline and Na + content and electrolyte leakage rate increased with increasing salinity and pH (or alkalinity). The deleterious effects of a high pH value or salinity alone were significantly less than those of high pH in combination with salinity. This result suggested that for a salt-alkaline mixed stress, a reciprocal enhancement between salt stress and alkali stress was a characteristic feature, and it was most evidently reflected in the survival rate. When salinity was below 125 mM or pH was below 8.8, survival rates were all 100%. However, when salinity was above 125 mM and pH was above 8.8, survival rates sharply declined with the increasing of either salinity or pH.The buffer capacity of the treatment solution was taken as a stress factor in order to simplify the stress factor analysis. The results of the statistical analysis showed that for the stress factors of the salt-alkaline mixed stress, [CO 2− 3 ] and [HCO − 3 ] could be fully represented by the buffer capacity, and [Na + ] could be fully represented by salinity, whereas [SO 2− 4 ] was negligible. Therefore, four factors, salinity, buffer capacity, pH and [Cl − ], could reflect all of the stress factors. Perfect linear correlations were observed between all physiological indices and four or three stress factors by a stepwise regression analysis. However, the effects of the four stress factors on the physiological indices were significantly different in magnitude. Buffer capacity and salinity were dominant factors for all physiological indices. Thus, it is reasonable to consider the sum of salinity plus buffer capacity as the strength value of salt-alkaline mixed stress. Furthermore, the relationships between different physiological indices and various stress factors were shown to be different.Abbreviations: RGR -relative growth rate; DW -dry weight; FW -fresh weight.
The cationic porphyrin 5,10,15,20-tetra-(N-methyl-4-pyridyl)porphyrin (TMPyP4) binds to quadruplex DNA and is thereby an inhibitor of human telomerase (Wheelhouse et al. J. Am. Chem. Soc. 1998, 120, 3261-3262). Herein the synthesis and telomerase-inhibiting activity of a wide range of analogues of TMPyP4 are reported, from which rules for a structure-activity relationship (SAR) have been discerned: (1) stacking interactions are critical for telomerase inhibition, (2) positively charged substituents are important but may be interchanged and combined with hydrogen-bonding groups, and (3) substitution is tolerated only on the meso positions of the porphyrin ring, and the bulk of the substituents should be matched to the width of the grooves in which they putatively lie. This SAR is consistent with a model presented for the complexation of TMPyP4 with human telomeric quadruplex DNA.
A new series of 2-(4-aminophenyl)benzothiazoles substituted in the phenyl ring and benzothiazole moiety has been synthesized by simple, high-yielding routes. The parent molecule 5a shows potent inhibitory activity in vitro in the nanomolar range against a panel of human breast cancer cell lines, but is inactive (IC50 > 30 microM) against other cell types: activity against the sensitive breast lines MCF-7 and MDA 468 is characterized by a biphasic dose-response relationship. Structure-activity relationships derived using these cell types has revealed that activity follows the heterocyclic sequence benzothiazole > benzoxazole >> benzimidazole and that 2-(4-aminophenyl)benzothiazoles bearing a 3'-methyl- 9a, 3'-bromo- 9c, 3'-iodo- 9f, and 3'-chloro-substituent 9i are especially potent and their activity extends to ovarian, lung, and renal cell lines. Four compounds have been evaluated in vivo against human mammary carcinoma models in nude mice. Compound 9a showed the most potent growth inhibition against the ER+ (MCF-7 and BO) and ER- (MT-1 and MT-3) tumors. Our efforts to identify a pharmacological mechanism of action for these intriguing compounds have not, as yet, been successful.
We compared the effects of salt-stresses (SS, 1 : 1 molar ratio of NaCl to Na 2 SO 4 ) and alkali-stresses (AS, 1 : 1 molar ratio of NaHCO 3 to Na 2 CO 3 ) on the growth, photosynthesis, solute accumulation, and ion balance of barley seedlings, to elucidate the mechanism of AS (high-pH) damage to plants and the physiological adaptive mechanism of plants to AS. The effects of SS on the water content, root system activity, membrane permeability, and the content of photosynthetic pigments were much less than those of AS. However, AS damaged root function, photosynthetic pigments, and the membrane system, led to the severe reductions in water content, root system activity, content of photosynthetic pigments, and net photosynthetic rate, and a sharp increase in electrolyte leakage rate. Moreover, with salinity higher than 60 mM, Na + content increased slowly under SS and sharply under AS. This indicates that high-pH caused by AS might interfere with control of Na + uptake in roots and increase intracellular Na + to a toxic level, which may be the main cause of some damage emerging under higher AS. Under SS, barley accumulated organic acids, Cl − , SO 4 2− , and NO 3 − to balance the massive influx of cations, the contribution of inorganic ions to ion balance was greater than that of organic acids. However, AS might inhibit absorptions of NO 3 -and Cl -, enhance organic acid synthesis, and SO 4 2− absorption to maintain intracellular ion balance and stable pH.
The seedlings of wheat were treated by salt-stress (SS, molar ratio of NaCl : Na 2 SO 4 = 1 : 1) and alkali-stress (AS, molar ratio of NaHCO 3 : Na 2 CO 3 = 1 : 1). Relative growth rate (RGR), leaf area, and water content decreased with increasing salinity, and the extents of the reduction under AS were greater than those under SS. The contents of photosynthetic pigments did not decrease under SS, but increased at low salinity. On the contrary, the contents of photosynthetic pigments decreased sharply under AS with increasing salinity. Under SS, the changes of net photosynthetic rate (P N ), stomatal conductance (g s ), and transpiration rate (E) were similar and all varied in a single-peak curve with increasing salinity, and they were lower than those of control only at salinity over 150 mM. Under AS, P N , g s , and E decreased sharply with rising salinity. The decrease of g s might cause the obvious decreases of E and intercellular CO 2 concentration, and the increase of water use efficiency under both stresses. The Na + content and Na + /K + ratio in shoot increased and the K + content in shoot decreased under both stresses, and the changing extents under AS were greater than those under SS. Thus SS and AS are two distinctive stresses with different characters; the destructive effects of AS on the growth and photosynthesis of wheat are more severe than those under SS. High pH is the key feature of the AS that is different from SS. The buffer capacity is essentially the measure of high pH action on plant. The deposition of mineral elements and the intracellular unbalance of Na + and K + caused by the high pH at AS might be the reason of the decrease of P N and g s and of the destruction of photosynthetic pigments.
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