Pre-emergence application of (thio)urea analogues compromises the development of the weed species Bidens pilosa, Urochloa brizantha, and Urochloa decumbens.

Invasive species (weeds) contribute to great losses in crop productivity, and one of the strategies for controlling their distribution in the field involves the use of herbicides. However, the development of new formulations for the control of weeds is challenged by environmental issues, increases in the resistance of weeds to herbicides, and poor selectivity of herbicides towards invasive species. Here, by using pre-emergence experiments, we assessed the phytotoxicity of two (thio)urea analogues (2A10 and 2B2) against the weed species Bidens pilosa (a dicot), Urochloa brizantha and Urochloa decumbens (monocots). Similar to diuron (400 µM), which is a commercial urea analogue herbicide, the urea analogue 2A10 (>200 µM) was lethal to B. pilosa. Although 2A10 failed to disrupt the germination of U. brizantha seeds, this compound (≥600 µM) inhibited the accumulation of chlorophyll a and b and carotenoids and resulted in the development of seedlings that presented relatively short roots and small, chlorotic leaves. Moreover, the thiourea analogue 2B2 (≥600 µM) reduced the germination percentage of U. decumbens seeds and delayed their germination, and at a concentration of 800 µM, this analogue impaired root growth and blocked the formation of lateral roots. The presence of an oxygen atom in the urea moiety of the 2A10 structure is critical for its marked activity against B. pilosa seeds, as 2B2 bears a sulphur atom instead and marginally inhibits seed germination. Neither 2A10 nor 2B2 was toxic to the non-weed species Lactuca sativa (lettuce; a dicot), and the latter even exerted beneficial effects by stimulating leaf expansion. Therefore, the evaluated (thio)urea analogues are promising for the design and development of new phytotoxic compounds for the pre-emergent control of the spread of B. pilosa (2A10) or the post-emergence control of U. brizantha (2A10) and U. decumbens (2B2).

Nitric oxide precursors prevent Al-triggered auxin flow inhibition in Triticum aestivum roots.

Aluminum (Al) is an element widely distributed in soils, even though Al3+ is one of the most detrimental cations to plant growth. The effect of nitric oxide (NO) precursors on indole-3-acetic acid (IAA) flow towards roots upon Al treatment is herein reported using two Triticum aestivum (wheat) cultivars with recognized differential Al tolerance. Roots of Al-tolerant seedlings with no treatment (control) accumulated higher amounts of NO than Al-sensitive ones. The treatment with Al further stimulated NO production in root cells while root exposure to NO3 -, L-arginine (Arg) or the NO donor S-nitrosoglutathione (GSNO) decreased both Al and lipid peroxide accumulation in both cultivars. Regardless of the cultivar, NO3 -, Arg or GSNO prevented the blockage of IAA flow towards roots. Overall, the treatment of wheat roots with NO precursors prior to Al treatment effectively guarantees normal IAA flow towards roots, a condition that favors the organ's growth and development.

Free radical scavenging and antiproliferative properties of Biginelli adducts.

A series of Biginelli adducts bearing different substituents at C-4 position were synthesized by using p-sulfonic acid calix[4]arene as a catalyst. The in vitro potential to scavenge reactive nitrogen/oxygen species (RNS and ROS) and the ability to inhibit cancer cells growth were then investigated. Four adducts were found to be potent scavengers of 2,2-diphenyl-1-picrylhydrazyl (RNS) and/or superoxide anion (ROS) radicals. The antiproliferative activity against cancer cells was disclosed for the first time for 16 monastrol analogs. The capacity of all compounds to inhibit cancer cells growth was dependent on the histological origin of cells, except for BA24, which was highly active against all cell lines. BA20 and BA33 were as potent as the reference drug doxorubicin against adriamycin-resistant ovarian and prostate cancer cells, respectively. These results highlight some monastrol analogs as lead compounds for the design of new free radical scavengers and anticancer agents.