Salvurmin A and Salvurmin B, Two Ursane Triterpenoids of Salvia urmiensis Induce Apoptosis and Cell Cycle Arrest in Human Lung Carcinoma Cells

Background: Ursane triterpenoids could be considered as novel multi-target therapeutic anti-cancer agents. Salvurmin A and Salvurmin B are novel cytotoxic ursane triterpenoids isolated from the aerial parts of Salvia urmiensis, an endemic plant species of Iran. Methods: In this study, we assessed cytotoxicity of these compounds against two human cancer cell lines and one human normal cell line and investigated its mechanism via apoptosis and cell cycle arrest. Results: Salvurmin A and B showed the most cytotoxic effect on A549 cells compared to other studied cancer cells. IC50 values for Salvurmin A and B against A549 cells were 35.6 ± 1.5 and 19.2 ± 0.8 µM, respectively. Based on annexin V staining, both of these compounds significantly induced apoptosis in A549 cells. Moreover, these two compounds significantly increased cell accumulation in G2/M and decreased the number of cells in G0/G1 phases in A549 cells in a dose-dependent manner. Conclusion: Based on the results Salvurmin B can be considered as potential candidate for further studies against human lung carcinoma

Justicidin B: A Promising Bioactive Lignan

Adverse effects and drug resistance to the current onchopharmacologicals have increased the demand for alternative novel therapeutics. We herein introduce justicidin B, an arylnaphthalen lignan isolated from different plant origins, especially Justicia, Phyllanthus, Haplophyllum and Linum species. This cyclolignan exhibits a wide array of biological properties ranges from piscicidal to antifungal, antiviral and antibacterial activities. Activity against Trypanosoma brucei makes justicidin B a potential antiprotozoal agent for the treatment of neglected tropical diseases. Pharmacological properties like antiplatelet, anti-inflammatory and bone resorption inhibition have been also attributed to justicidin B. This compound is a potent cytotoxic substance on several cell lines, especially chronic myeloid and chronic lymphoid leukemia. Pharmacological values, natural variation, as well as biotechnological production of justicidin B by plant cell, tissue and organ culture are also described in this review. Chemical characteristics and chromatographic methods to identify justicidin B and its biosynthetic pathway have been discussed. Different approaches to the total synthesis of justicidin B are compared. This review would shed light on the role of justicidin B as an intriguing natural compound and provides a chance to optimize conditions for industrial applications

Immunomodulatory Peptides as Vaccine Adjuvants and Antimicrobial Agents

The underdevelopment of adjuvant discovery and diversity, compared to core vaccine technology, is evident. On the other hand, antibiotic resistance is on the list of the top ten threats to global health. Immunomodulatory peptides that target a pathogen and modulate the immune system simultaneously are promising for the development of preventive and therapeutic molecules. Since investigating innate immunity in insects has led to prominent achievements in human immunology, such as toll-like receptor (TLR) discovery, we used the capacity of the immunomodulatory peptides of arthropods with concomitant antimicrobial or antitumor activity. An SVM-based machine learning classifier identified short immunomodulatory sequences encrypted in 643 antimicrobial peptides from 55 foe-to-friend arthropods. The critical features involved in efficacy and safety were calculated. Finally, 76 safe immunomodulators were identified. Then, molecular docking and simulation studies defined the target of the most optimal peptide ligands among all human cell-surface TLRs. SPalf2-453 from a crab is a cell-penetrating immunoadjuvant with antiviral properties. The peptide interacts with the TLR1/2 heterodimer. SBsib-711 from a blackfly is a TLR4/MD2 ligand used as a cancer vaccine immunoadjuvant. In addition, SBsib-711 binds CD47 and PD-L1 on tumor cells, which is applicable in cancer immunotherapy as a checkpoint inhibitor. MRh4-679 from a shrimp is a broad-spectrum or universal immunoadjuvant with a putative Th1/Th2-balanced response. We also implemented a pathway enrichment analysis to define fingerprints or immunological signatures for further in vitro and in vivo immunogenicity and reactogenicity measurements. Conclusively, combinatorial machine learning, molecular docking, and simulation studies, as well as systems biology, open a new opportunity for the discovery and development of multifunctional prophylactic and therapeutic lead peptides

Antioxidant Activity of Six Marine Sponges Collected from the Persian Gulf: Antioxidant activity of marine sponges

Compounds especially from natural sources are capable of protecting against reactive oxygen species (ROS) mediated damage. Therefore, there is a growing interest in novel substances exhibiting antioxidant properties. Several marine environments can provide a rich source of novel biologically active compounds. The aim of this paper is to evaluate in vitro antioxidant properties of six sponge speciescollected from Kish Island in the Persian Gulf. We evaluated the effects of different concentrations of the dichloromethane and methanolic extracts of six sponges on scavenging DPPH and OH free radicals. The activities of these extracts were compared with those of commercial antioxidants such as gallic acid. The maximum level of DPPH radical scavenging (0.234± 0.033 mg/ml) was observed for the methanolic extract of Pseudosaberites clavatus in the reaction mixture. Also, most of sponge extracts exhibited medium to high hydroxyl radical scavenging activity. The results of this study suggest that marine sponges of the Persian Gulf are promising sources of antioxidants

Lipoamino Acid Coated Superparamagnetic Iron Oxide Nanoparticles Concentration and Time Dependently Enhanced Growth of Human Hepatocarcinoma Cell Line (Hep-G2)

Superparamagnetic iron oxide nanoparticles (SPION) have been widely used in medicine for magnetic resonance imaging, hyperthermia, and drug delivery applications. The effect of SPION on animal cells has been a controversial issue on which there are many contradictions. This study focused on preparation of SPION with novel biocompatible coatings, their characterization, and cytotoxicity evaluation. An amino acid (glycine) and two novel lipo-amino acids (2 amino-hexanoic acid and 2 amino-hexadecanoic acid) coated magnetic nanoparticles were characterized by various physicochemical means such as X-ray diffraction (XRD), transmission electron microscopy (TEM), vibrating sample magnetometry (VSM), differential scanning calorimetry (DSC), and infrared spectroscopy (FT-IR). The cytotoxicity profile of the synthesized nanoparticles on Hep-G2 cells as measured by MTT assay showed the nanoparticles are nontoxic and the cell growth is promoted by SPION. Moreover, lipoamino acid coating SPION appear more beneficial than the other ones. By increasing concentration of SPION, growth enhancing impact will attenuate and toxicity will appear. Although the aggregation of SPION can affect the results, the gradual delivery of ferric/ferrous ions into cells is the main cause of this growth promotion effect. Conclusively, this study shows that lipoamino acid coating SPION can be used for various biomedical purposes