[Study on diagnosis and treatment of lumbar disc herniation and related factors based on dynamic electromyography].

OBJECTIVE: To analyze dynamic electromyography characteristics and related factors of lumbar back muscle activity in patients with lumbar disc herniation, and to clarify the clinical significance of dynamic electromyography in the diagnosis and treatment of patients with lumbar disc herniation(LDH). METHODS: From September 2014 to March 2021, 40 patients with lumbar disc herniation(LDH group) were detected by surface electromyography telemeter. There were 14 males and 26 females, aged from 20 to 61 years old, with an average of(40.68±10.56) years old, the course of illness was from 1 to 120 months, with an average of (17.75±27.56) months. In addition, 12 normal people were recruited as the control group. There were 2 males and 10 females. The age ranged from 24 to 53 years old, with an average of(36.50±10.30) years old. All subjects were subjected to dynamic electromyographic tests of the subthoracic erector spinae, lumbar erector spinae, and multifidus muscles during static standing and trunk flexion and extension. Compare the EMG activity data (average EMG amplitude, median frequency, original EMG graph) of the tested muscles between patients with lumbar disc herniation and normal people, and analyze the correlation between the general data of patients with lumbar disc herniation and the tested muscle EMG data. RESULTS: When standing still, the average electromyographic amplitude of the erector spinal muscle of the right and left thoracic segments of the subjects in the LDH group increased compared with the control group, and the difference was significant(P<0.05). In the trunk flexion and extension, the average electromyographic amplitude of the right and left proximal thoracic erector spinae, the right left lumbar erector spinae, and the right left multifidus muscle of the subjects in the LDH group are all larger than the control group, and the difference was significant(P<0.05). In the trunk flexion and extension, the median frequencies of the right left proximal thoracic erector spinae、the right left lumbar erector spinae, and the right left multifidus muscle of the subjects in the LDH group were all larger than the normal control group, and the difference was significant (P<0.05). During trunk flexion and extension, the original electromyographic patterns of subjects in the LDH group were significantly different from those in the control group. During the maintenance of the maximum trunk flexion of the subjects in the LDH group, there was a high level of electromyographic activity of the lower back muscles, and the electromyographic static signals that should appear regularly in the original signal could not be distinguished. When the trunk was flexed and extended, had gender, age, weight and height of subjects in the LDH group were not significantly correlated with the average EMG amplitude and median frequency of bilateral proximal thoracic, lumbar erector spinae and bilateral multifidus muscles respectively(P>0.05). CONCLUSION: Patients with lumbar disc herniation have characteristic surface EMG changes in the back muscles that are different from those of normal people. These features can more objectively reflect the patient's muscle condition and can be an effective indicator for the diagnosis and treatment effect evaluation of patients with lumbar disc herniation. It can be seen that surface electromyography is not only a detection method, it can be considered in the routine diagnosis and treatment plan of LDH to guide clinical work.

The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.

Chronic myeloid leukemia (CML) is a malignant disease of the hematopoietic system with crucial pathogenic protein named BCR-ABL, which endangers the life of patients severely. As a milestone of targeted drug, Imatinib has achieved great success in the treatment of CML. Nevertheless, inevitable drug resistance of Imatinib has occurred frequently in clinical due to the several mutations in the BCR-ABL kinase. Subsequently, the second-generation of tyrosine kinase inhibitors (TKIs) against BCR-ABL was developed to address the mutants of Imatinib resistance, except T315I. To date, the third-generation of TKIs targeting T315I has been developed for improving the selectivity and safety. Notably, the first allosteric inhibitor has been in market which could overcome the mutations in ATP binding site effectively. Meanwhile, some advanced technology, such as proteolysis-targeting chimeras (PROTAC) based on different E3 ligand, are highly expected to overcome the drug resistance by selectively degrading the targeted proteins. In this review, we summarized the current research progress of inhibitors and degraders targeting BCR-ABL for the treatment of CML.

The synthesis of anticancer sulfonated indolo[2,1-a]isoquinoline and benzimidazo[2,1-a]isoquinolin-6(5H)-ones derivatives via a free radical cascade pathway.

A facile CuBr2 induced radical relay addition/cyclization of activated alkenes with substituted-thiosulfonates has been achieved, leading to a broad range of sulfonated indolo[2,1-a]isoquinolines and benzimidazo[2,1-a]isoquinolin-6(5H)-ones in moderate to good yields. In particular, some compounds exhibit bioactivity against cancer cell lines. This protocol shows advantages of low-cost, base-free, simple operation, and broad functional group tolerance.

[The potential effects of linalool on enantioselective skin permeation of norgestrel].

The purpose of this study is to investigate the enantioselectivity of norgestrel (NG) transdermal permeation and the potential influence of linalool and lipids on the enantioselectivity. In vitro skin permeation studies of NG across the excised rat skins were performed with Valia-Chien diffusion cells, and the permeation samples were analyzed by enantioselective HPLC. The possible enantioselective permeation of NG across intact rat back skin and lipids extracted rat back skin and the influence of linalool were evaluated. The skin permeation rate of dl-NG was two times higher than that of l-NG when donor solutions (EtOH/H2O 2 : 8, v/v) containing l-NG or dl-NG. It may be mainly attributed to the solubility discrepancy between enantiomer and racemate. The enantioselective permeation of dl-NG across intact rat skin was observed when the donor solutions containing dl-linalool. The permeation flux of l-NG was 22% higher than that of d-NG. But interestingly, the enantioselective permeation of dl-NG disappeared under the same experimental condition except that the lipid extracted rat skin was used. Attenuated total reflection-fourier transform infrared spectroscopy analysis of stratum corneum showed that the wave number for asymmetric CH2 stretching vibrations of lipids treated with dl-linalool was greater than that of the control. The results indicated that the enantioselective permeation of NG may be contributed by the interaction between dl-linalool and lipids. More than half of lipids were composed of ceramides. The stereospecific interaction maybe existed among chiral enhancer (linalool), lipids (ceramides) and/or chiral drugs (NG).

Progress in synthesis and antitumor activities of estradiol-linked platinum complex.

Platinum complexes such as cisplatin and caboplatin are widely used in cancer chemotherapy. However, their clinical applications are substantially limited by unexpected toxic side effects. In this review, we discuss the current progress on the design and synthesis of estradiol-linked platinum complexes as the targeted antitumor drugs. Many of them display a high antitumor activity against the growth of breast cancer cell lines in vitro. The estradiol-linked platinum complexes could be used as target therapeutics for breast cancer.