Medicinal Chemistry

In this study, charming luminescent nanostructures have been obtained from two components between amino acids functionalized naphthalene derivative (IN) and bases (Adenine (A), Thymine (T), Guanine (G) and Uracil (U)) units via co-assembly. These fluorescent nanotubes, walnut-like structures, nanofibers and sponge-like structures have been investigated by means of Ultraviolet Spectra (UV), Fluorescence Spectra and Scanning Electron Microscopy (SEM). The results illustrated that these nanostructures were of strong fluorescence and the drive forces were the intermolecular hydrogen bonding and π-π stacking interactions.

A series of novel naphthalimide dithiocarbamate 4a-f, 5a-f were efficiently synthesized via introduce dithiocarbamate and dithioate side chain onto the naphthalic anhydride core. The structures of the synthesized analogs were elucidated by spectroscopic methods, including IR,1H and 13C NMR, and (ESIHRMS) techniques. The anti-cancer activities of the generated naphthalimide derivatives 4c, 4d, 4e, 4f, and 5d were evaluated against 21 tumour cell lines; inculding 10 tumor subpanels using MTT assay. Analogue 4c offer antitumor activity with an IC50 of 10.54 μM against SKBR3 breast cancer cells. Compound 4d showed varying degrees of antitumor activities towards several tumour cell lines ranging from 21.1 to 71.7 μM. In addition to the antitumor activities; the synthesized compounds were evaluated for their In vitro anti-inflammatory activity. Compounds 4c and 4d revealed potent anti-inflammatory properties in comparison with the reference drug celecoxib. Molecular docking studies provided complementary theoretical support for experimental biological data.

We reveal a fluorescence enhancement mechanism of an aggregation-induced emission (AIE)-DNA probe for target DNA detection. The enhancement is caused by the restriction of intramolecular rotation (RIR) effect that arises from steric hindrance between the AIE dye moiety in a hybridized probe and the dangling end (free-ssDNA) or peripheral dsDNA. Thus, these AIE-DNA probes can selectively detect two or more DNA repeat sequences, such as telomeric repeats.

Background: Despite the significant advances in chemotherapy, the prognosis of unresectable gastric cancer is still very poor and the role of immunotherapy remains to be clarified. We examined whether lentinan, a biological response modifier, could enhance the chemotherapeutic effects.

Materials and methods: A retrospective cohort study was conducted to evaluate the survival benefits of lentinan among the patients with gastric cancer receiving chemotherapy. To investigate the mechanisms underlying the clinical effects of lentinan, its cytotoxic activity was accessed by cell proliferation assay. The expression of molecules relevant to immune checkpoints were analyzed by real-time PCR using human gastric cancer cell lines; MKN1, MKN45, and NUGC3.

Results: The addition of lentinan prolonged the survival of patients with gastric cancer receiving S-1 based chemotherapy. Lentinan reduced the constitutive expression of PD-L1 in all cell lines mainly by suppressing the MAPK pathway.

Conclusion: Lentinan at clinical concentrations stimulates tumor-specific adaptive immunity through PD-L1 downregulation, which may enhance chemotherapy-induced tumor clearance and patient survival.

Ethnopharmacological relevance: An ethnobotanical survey was conducted to collect information of medicinal plants on Arthritis relating to anti-inflammatory and Analgesia effect by Chaoshan-Shantou People living in Guangdong.

Aim of the study: This investigation was to document valuable knowledge represented as Chaoshan herbal medicine.

Materials and methods: Information was obtained from interviews and by reviewing studies of Chaoshan and Cantonese reported in the literature.

Results: Our data covered 86 species belonging to 82 genera in 52 families. In the search of the PubMed database, there are 28 herbs that have been studied, which have the most anti-inflammatory effects of the herb, followed by analgesia.

Conclusions: Due to the rapid disappearance of urbanization and industrialization of traditional culture and natural resources, indicating that the recorded information may be lost forever. Therefore, there is an urgent need to record the value of Chaoshan medicinal knowledge and encourage the transfer to the next generation.

Circadian rhythms regulate a wide range of biological processes and play a fundamental role in mammalian behavior, physiology, and metabolism. The hierarchically organized circadian timing system in mammals, with a master pacemaker in the suprachiasmatic nucleus (SCN) of the hypothalamus and subsidiary oscillators in extra-SCN brain regions and peripheral tissues, mediates periodicities in physiological processes. It has been well recognized that disruption or misalignment of the intrinsic rhythms leads to diverse pathological states. Since mammalian circadian clock genes were first identified in the 1990’s, genetic and biochemical approaches have uncovered the molecular bases of the cell-autonomous and self-sustainable rhythms that are generated by two interlocking feedback loops of clock proteins. With our understanding of key features underlying the overt circadian rhythm and physiological outputs, it has emerged that pharmacological control of the circadian clock may provide a novel therapeutic strategy to treat a variety of circadian rhythm-related human diseases such as neuropsychiatric, metabolic, cardiovascular, and immune/inflammatory diseases, and even cancer. Pharmaceutical approaches to circadian clock may involve either development of drugs to treat such circadian-related disorders or combinational uses with existing therapeutic strategies to improve their therapeutic efficacy via the intrinsic clock-dependent mechanisms. In this review, we will focus on recent progress in discovery of small molecule chemical compounds that can pharmacologically modulate molecular circadian clock and their potential to be developed into therapeutic drugs.

The results of present study support the view that Hemidesmus indicus and its isolated bioactive compound (2H4MB) showing potential antibacterial and antifungal activities that could be utilized to control infectious diseases caused by the test pathogens and Candida albicans in the human system. Analysis of essential oil from root of the plant obtained by using Clevenger apparatus by hydro distillation was undertaken through GC-MS. 2-Hydroxy- 4-methoxybenzaldehyde (2H4MB) was the major chemical entity (99.41%) amongst 10 identified compounds. The in vitro antibacterial activity of 3 different extracts (Hexane, Methanol and Aqueous) and Bioactive compound 2-Hydroxy-4-methoxybenzaldehyde (2H4MB) as well as MIC values of isolated compound (2H4MB) were performed. The most active extract was found to be the hexane extract showing the maximum zone of inhibition of 22 mm against Staphylococcus aureus. The isolated bioactive compound (2H4MB) showed the highest diameter of zone of inhibition of 23 mm against Staphylococcus aureus. The Minimum Inhibitory Concentration values of the Bioactive compound 2H4MB on test pathogens varies from 80 μg/ml to 250 μg/ml, Minimum Bactericidal Concentration values varies from 150 μg/ml to 250 μg/ml. The MFC values and MIC values of 2H-4-MB on Candida albicans were 200 μg/ml and 150 μg/ml respectively. The active extract was also tested for cytotoxicity using freshly obtained sheep erythrocytes and it was revealed zero cytotoxicity.