Synthesis and Biological Activities of 11- and 12-Substituted Benzophenanthridinone Derivatives as DNA Topoisomerase IB and Tyrosyl-DNA Phosphodiesterase 1 Inhibitors.

Herein, a series of 11- or 12-substituted benzophenanthridinone derivatives was designed and synthesized for the discovery of dual topoisomerase IB (TOP1) and tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitors. Enzyme-based assays indicated that two compounds 12 and 38 showed high TOP1 inhibitory potency (+++), and four compounds 35, 37, 39 and 43 showed good TDP1 inhibition with IC values ranging from 10 to 18 μM. 38 could induce cellular TOP1cc formation, resulting in the highest cytotoxicity against HCT-116 cells (0.

[Cadmium Enrichment and Bioavailability of Quaternary Profiles in Nansha District, Guangzhou, China].

Comprehending the distribution pattern and enrichment rule of the heavy metal cadmium (Cd) in soil and grasping its activity and influencing factors is crucial for guaranteeing the soil environment safety of agricultural and construction land and improving the overall quality of the soil environment. The concentration of heavy metal Cd in the quaternary profile of Nansha was measured, and the pollution level was evaluated using the geographical accumulation index () and potential ecological risk index (). Then, we determined the correlation between the total amount of Cd and the physicochemical properties of the soil using factor analysis (FA-MLR).

Discovery, enantioselective synthesis of myrtucommulone E analogues as tyrosyl-DNA phosphodiesterase 2 inhibitors and their biological activities.

As a recently discovered DNA repair enzyme, tyrosyl-DNA phosphodiesterase 2 (TDP2) can specifically repair topoisomerase 2 (TOP2)-mediated DNA damage, resulting in cancer cell resistance to TOP2 inhibitors. Its inhibitors can enhance the anticancer efficacy of TOP2 inhibitors. In this work, we report the discovery of natural product myrtucommulone E as selective TDP2 inhibitor and its first enantioselective total synthesis through a pivotal CPA-catalyzed Michael addition reaction.

Synthesis of 11-aminoalkoxy substituted benzophenanthridine derivatives as tyrosyl-DNA phosphodiesterase 1 inhibitors and their anticancer activity.

Tyrosyl-DNA phosphodiesterase 1 (TDP1) is an enzyme that repairs DNA lesions caused by the trapping of DNA topoisomerase IB (TOP1)-DNA break-associated crosslinks. TDP1 inhibitors have synergistic effect with TOP1 inhibitors in cancer cells and can overcome cancer cell resistance to TOP1 inhibitors. Here, we report the synthesis of 11-aminoalkoxy substituted benzophenanthridine derivatives as selective TDP1 inhibitors and show that six compounds 14, 16, 18, 20, 25 and 27 exhibit high TDP1 inhibition potency.

Pyranodipyran Derivatives with Tyrosyl DNA Phosphodiesterase 1 Inhibitory Activities and Fluorescent Properties from sp. EGF 15-0-3.

Four new benzodipyran racemates, namely (±)-aspergiletals A-D (-), representing a rare pyrano[4,3-]chromene scaffold were isolated together with eurotiumide G () and eurotiumide F () from the soft-coral-derived fungus sp. EGF 15-0-3. All the corresponding optically pure enantiomers were successfully separated by a chiral HPLC column.

[Bioavailability and Ecological Risk Assessment of Cadmium in the Sea-Land Interaction Sediments of the Pearl River Delta].

Cadmium (Cd) pollution poses a threat to human health, and research on Cd bioavailability as well as its ecological risk assessment can help prevent and mitigate Cd hazards. The enrichment characteristics and variability of Cd were investigated in sea-land interaction soil fractions and the associated environmental and ecological risks were evaluated using the accumulation index (), potential ecological hazard index (), and risk assessment coding (RAC). The results showed that:① The Cd content of miscellaneous fill material was typically lower than 0.

[Content and Distribution of Cadmium in Soil and Fluvial Sediments in the Sea-Land Interaction Zone].

Cadmium pollution poses a threat to human health. The examination of spatial distribution of Cd in soils can be used to assess the risks posed to humans and the environment. The enrichment characteristics and variation rules of heavy metal cadmium in the soil were revealed by analyzing the concentration and fractions of Cd in the soil at different depths in the sea-land interaction zone.

[Detection of Gene Abnormalities in 43 Cases of Chronic Lymphocytic Leukemia by Fluorescence in Situ Hybridization].

Objective: To explore the value of fluorescence in situ hybridization (FISH) in diagnosis and prognosis evaluation of chronic lymphocytic leukemia (CLL).

Methods: R banding technique was used for karyotype analysis in 43 cases of CLL, and fluorescence in situ hybridization（FISH） technique was used for analysis of 5 genes in 43 cases of CLL, including D13S25, RB1,ATM, P53 and CEP 12 .

Results: The detection rate of chromosome abnormality was 9.

Investigating the association between oral hygiene and head and neck cancer.

Objectives: This analysis examined the association between oral hygiene and head and neck cancer (HNC) and whether this association differed by the consumption of alcohol, betel quid, or cigarette and by the genetic polymorphisms of inflammation-related genes.

Materials And Methods: Interviews regarding dental care and oral health were conducted with 317 HNC cases and 296 controls. Genotyping was performed for 6 single nucleotide polymorphisms in IL6, IL10 and PTGS2.

Allergies and risk of head and neck cancer: an original study plus meta-analysis.

Background: Although the relationship between allergy and cancer has been investigated extensively, the role of allergy in head and neck cancer (HNC) appears less consistent. It is not clear whether allergies can independently influence the risk of HNC in the presence of known strong environmental risk factors, including consumption of alcohol, betel quid, and cigarette.

Methods: THE CURRENT PAPER REPORTS RESULTS FROM: 1) an original hospital-based case-control study, which included 252 incident cases of HNC and 236 controls frequency-matched to cases on sex and age; and 2) a meta-analysis combining the results of the current case-control study and 13 previously published studies (9 cohort studies with 727,569 subjects and 550 HNC outcomes and 5 case-control studies with 4,017 HNC cases and 10,928 controls).

[Cytogenetic study on 53 patients with multiple myeloma].

To explore the conventional cytogenetic (CC) characteristics and the partial molecular cytogenetic characteristics of multiple myeloma (MM), R banding technique was used for karyotype analysis in 53 cases of MM, and fluorescence in situ hybridization(FISH) technique was used for molecular cytogenetic analysis in 20 cases out of them. The results showed that the rate of chromosome abnormality was 32.1% in 53 cases.

[Application of fluorescence in situ hybridization technique in diagnosis of variant Ph chromosome translocation and Ph-negative chronic myelocytic leukemia].

Objective: To explore the value of fluorescence in situ hybridization (FISH) technique in diagnosis of variant Ph chromosome translocation (VT) and Ph chromosome-negative chronic myelocytic leukemia (CML).

Methods: Nine CML patients with VT and 2 Ph chromosome-negative CML patients confirmed by R banding were assayed with dual color-dual fusion BCR/ABL probe by FISH.

Results: The 9 patients with VT involved chromosomes 1, 3, 5, 12, 13, 15, 17 and 21 besides chromosomes 9 and 22, and some of them showed recurrent aberrations; FISH results were positive and the signal feature was 2R2G1Y.