Optimization of surgical exposure for harvesting gracilis-semitendinosus tendons.

PURPOSE: This study was conducted to provide anatomical data and surface markers for the safe and efficient exposure of surgical incisions for harvesting gracilis tendons (GT) and semitendinosus tendons (STT) while avoiding technical pitfalls and nerve injury during harvest for ligament reconstruction. METHODS: Seventy-four Chinese cadaveric lower limbs were dissected to expose the infrapatellar branch of the saphenous nerve (IPBSN) and pes anserinus (PA). Measurements of the borders and accessory bands of the PA tendons were taken. The arrangement of PA tendons and distribution of the IPBSN were assessed. RESULTS: The PA was roughly shaped like a quadrangle, with its superior border at the horizontal plane of the tibial tuberosity (TT). The GT and STT bifurcation point was located on the medial border of the PA. From medial side to lateral side, the sartorius tendons (ST), GT, and STT fused gradually and formed the lateral border of the PA at the distal end. The tendon arrangement of the PA was primarily affected by ST, which commonly covered GT and STT completely. Variant tendons were found in 41.9% of specimens. The insertion of the accessory bands was distal but close to the inferior border of the PA. Accessory bands were observed only in STT and ST, and STT accounted for the most. The width of the first accessory band of STT was similar to the width of the STT. Additionally, most of the IPBSNs were proximal to the horizontal plane of the TT. CONCLUSION: For clearly exposing the GT and STT, it is crucial to expose the GT and STT bifurcation point on the medial border of the PA, whether directly or indirectly through the incision.The influence of ST insertion and the variability of tendons within the PA must be paid attention to during the operation. To protect IPBSNs highly, the incision should not be higher than the TT level.

Design, synthesis and mode of action of novel 3-chloro-6-pyrazolyl picolinate derivatives as herbicide candidates.

BACKGROUND: Picolinate/picolinic acid compounds are an important class of synthetic auxin herbicides. To explore the herbicidal activity of 6-pyrazolyl picolinate compounds, a series of 3-chloro-6-pyrazolyl-picolinate derivatives was designed and synthesized. RESULTS: Twenty-five 3-chloro-6-pyrazolyl-picolinate derivatives synthesized were tested for herbicidal activity and the IC50 value of compound c5 to the growth of Arabidopsis thaliana root was 27 times lower than that of the commercial herbicide clopyralid. Compound c5 displayed better post-emergence herbicidal activity and broader (Picloram, Clopyralid, Aminopyralid) herbicidal spectrum at a dosage of 400 g ha-1 in comparison with clopyralid; it also was safe to wheat and maize at this dosage. Arabidopsis thaliana phenotypes and expression of auxin-response genes demonstrated that compound c5 might be a novel auxin-type herbicide. Molecular docking analyses revealed that compound c5 had stronger binding ability to receptor AFB5 (auxin signaling F-box protein 5) than clopyralid. CONCLUSION: These 6-pyrazolyl picolinate compounds could be used as potential lead structures for the discovery of a novel synthetic auxin herbicide. © 2021 Society of Chemical Industry.

A highly selective and sensitive fluorescence probe for a specific binding site on insect ryanodine receptors.

There is a significant need to study the binding of active compounds to the specific sites on insect ryanodine receptors (RyRs) that are the targets of two novel classes of diamide insecticides to which insects are becoming increasingly resistant. Here, we describe a rapid assay to study the action of potential compounds on the flubendiamide (Flu) binding site of insect RyRs that uses a fluorescence polarization assay with the fluorescence probe Flu-R-L that we synthesized. The IC50 of Flu for inhibiting probe binding on insect RyR was 18.82 ng/mL. The binding of 86 novel phthalic diamide derivatives on insect RyRs was studied using this newly established assay, and the compounds that exhibited high-affinity binding in the assay also possessed in vivo insecticidal activity against Plutella xylostella. Thus, Flu-R-L is a highly selective and sensitive fluorescence probe for studying the binding affinity of novel compounds to the Flu binding site of insect RyRs. The assay based on Flu-R-L is a rapid, accurate, and sensitive method for the screening of potentially bioactive molecules that bind specifically to insect RyRs.

A monoclonal antibody-based indirect competitive enzyme-linked immunosorbent assay for flubendiamide detection.

Flubendiamide (FD), the first commercial phthalic acid diamide that targets insect ryanodine receptor (RyRs), has played an important role in pest management. With its extensive worldwide application, a rapid and convenient method to detect its existence in the environment is necessary. In this study, an indirect competitive enzyme-linked immunosorbent assay (icELISA) was developed to analyse FD residue on environmental and food samples. The established icELISA showed a half maximal inhibition concentration (IC50) of 17.25 µg L-1, with a working range of 4.06-103.59 µg L-1 for FD, and showed no cross-reactivity with chlorantraniliprole, cyantraniliprole, and several FD analogues. Average FD recoveries from spinach, tap water, and soil samples were 89.3-112.3%, 93.0-102.1%, and 86.9-97.6%, respectively. Meanwhile, FD detection results of icELISA were compared with those of ultra-high-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). The comparable results verified that icELISA was suitable for rapid detection of FD residue in environmental and agricultural samples.

Design, Synthesis, and Biological Activities of Novel 1,3,5-Trimethylpyrazole-Containing Malonamide Derivatives.

New 1,3,5-trimethylpyrazole-containing malonamide derivatives based on pyflubumide were designed, synthesized, and characterized using ¹H-NMR, 13C-NMR, and high-resolution mass spectra (HRMS). The results of preliminary bioassays showed that the target compounds possessed good activities against Tetranychus cinnabarinus, Plutella xylostella, and Aphis craccivora. Most of the target compounds exhibited moderate to good acaricidal activity against Tetranychus cinnabarinus at a concentration of 400 µg/mL, and some showed moderate activity at a concentration of 200 µg/mL; in particular, compounds 8m and 8p exhibited 70.0% mortality. In addition, some of the target compounds exhibited good insecticidal activities against Plutella xylostella at a concentration of 200 µg/mL, especially compounds 8i and 8o, which achieved 100.0% mortality at a concentration of 100 µg/mL. Interestingly, some of the target compounds exhibited potent anti-aphid activity against Aphis craccivora at a concentration of 200 µg/mL; furthermore, compounds 8p and 8q demonstrated 100.0% anti-aphid activity at a concentration of 50 µg/mL. The preliminary analyses of the structure⁻activity relationships (SAR) indicated that the acaricidal and insecticidal activities varied significantly depending on the type of substituent and substitution pattern, which provides guidance for the further investigation of such structural modifications.

Synthesis of Chrysogeside B from Halotolerant Fungus Penicillium and Its Antimicrobial Activities Evaluation.

Chrysogeside B, a natural cerebroside, was efficiently synthesized from commercial feedstocks. The bioassays showed that compounds 4, 5 and 6 exhibited enhanced biological activities compared Chrysogeside B. Further studies revealed that free hydroxyl groups and glycosidic bond have significant impact on the antimicrobial activities. The synthesis of Chrysogeside B and analogues designed to allow identification of the features of this glycolipid required for recognition by tested bacteria and Hela cells is described.

A one-pot approach to pyridyl isothiocyanates from amines.

A one-pot preparation of pyridyl isothiocyanates (ITCs) from their corresponding amines has been developed. This method involves aqueous iron(III) chloride-mediated desulfurization of a dithiocarbamate salt that is generated in situ by treatment of an amine with carbon disulfide in the present of DABCO or sodium hydride. The choice of base is of decisive importance for the formation of the dithiocarbamate salts. This one-pot process works well for a wide range of pyridyl ITCs. Utilizing this protocol, some highly electron-deficient pyridyl and aryl ITCs are obtained in moderate to good yields.