Identification of Cyclic Dipeptides and a New Compound (6-(5-Hydroxy-6-methylheptyl)-5,6-dihydro-2H-pyran-2-one) Produced by Streptomyces fungicidicus against Alternaria solani

As an important microbial resource, Actinomycetes, especially Streptomyces, have important application values in medicine and biotechnology. Streptomyces fungicidicus SYH3 was isolated from soil samples in tomato-growing areas and showed good inhibitory effects on Alternaria solani in tomato. To obtain pure active compounds, SYH3 fermentation broth was subjected to XAD-16 macroporous resin and silica gel column chromatography. Combined with the repeated preparation and separation of preparative high-performance liquid chromatography (HPLC), a total of four monomer compounds were obtained after activity tracking. Compound 4 was identified as a new six-membered lactone ring compound named 6-(5-hydroxy-6-methylheptyl)-5,6-dihydro-2H-pyran-2-one by 1D and 2D nuclear magnetic resonance (NMR) data and mass spectrometry (MS). The other three active compounds belong to the cyclodipeptide, and their half maximal inhibitory concentration (IC₅₀) values against A. solani were 43.4, 42.9, and 30.6 μg/mL, respectively. Compound 4 significantly inhibited the spore germination and induced swollen and deformed local hyphae of A. solani with an IC₅₀ value of 24.9 μg/mL. Compound 4 also had broad-spectrum antifungal activity and had a good antifungal effect on the tested plant-pathogenic fungi. The modes of action of new compound (4) still require further investigation, representing a novel and effective anti-fungal agent for future application.     

Trends and Technological Advancements in the Possible Food Applications of Spirulina and Their Health Benefits: A Review

Spirulina is a kind of blue-green algae (BGA) that is multicellular, filamentous, and prokaryotic. It is also known as a cyanobacterium. It is classified within the phylum known as blue-green algae. Despite the fact that it includes a high concentration of nutrients, such as proteins, vitamins, minerals, and fatty acids—in particular, the necessary omega-3 fatty acids and omega-6 fatty acids—the percentage of total fat and cholesterol that can be found in these algae is substantially lower when compared to other food sources. This is the case even if the percentage of total fat that can be found in these algae is also significantly lower. In addition to this, spirulina has a high concentration of bioactive compounds, such as phenols, phycocyanin pigment, and polysaccharides, which all take part in a number of biological activities, such as antioxidant and anti-inflammatory activity. As a result of this, spirulina has found its way into the formulation of a great number of medicinal foods, functional foods, and nutritional supplements. Therefore, this article makes an effort to shed light on spirulina, its nutritional value as a result of its chemical composition, and its applications to some food product formulations, such as dairy products, snacks, cookies, and pasta, that are necessary at an industrial level in the food industry all over the world. In addition, this article supports the idea of incorporating it into the food sector, both from a nutritional and health perspective, as it offers numerous advantages.     

Antimicrobial Effect and Cytotoxic Evaluation of Mg-Doped Hydroxyapatite Functionalized with Au-Nano Rods

Hydroxyapatite (HA) is the main inorganic mineral that constitutes bone matrix and represents the most used biomaterial for bone regeneration. Over the years, it has been demonstrated that HA exhibits good biocompatibility, osteoconductivity, and osteoinductivity both in vitro and in vivo, and can be prepared by synthetic and natural sources via easy fabrication strategies. However, its low antibacterial property and its fragile nature restricts its usage for bone graft applications. In this study we functionalized a MgHA scaffold with gold nanorods (AuNRs) and evaluated its antibacterial effect against S. aureus and E. coli in both suspension and adhesion and its cytotoxicity over time (1 to 24 days). Results show that the AuNRs nano-functionalization improves the antibacterial activity with 100% bacterial reduction after 24 h. The toxicity study, however, indicates a 4.38-fold cell number decrease at 24 days. Although further optimization on nano-functionalization process are needed for cytotoxicity, these data indicated that Au-NRs nano-functionalization is a very promising method for improving the antibacterial properties of HA.     

Synthesis of Moracin C and Its Derivatives with a 2-arylbenzofuran Motif and Evaluation of Their PCSK9 Inhibitory Effects in HepG2 Cells

Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a key factor in several cardiovascular diseases, as it is responsible for the elevation of circulating low-density lipoprotein cholesterol (LDL-C) levels in blood plasma by direct interaction with the LDL receptor. The development of orally available drugs to inhibit this PCSK9-LDLR interaction is a highly desirable objective. Here, we report the synthesis of naturally occurring moracin compounds and their derivatives with a 2-arylbenzofuran motif to inhibit PCSK9 expression. In addition, we discuss a short approach involving the three-step synthesis of moracin C and a divergent method to obtain various analogs from one starting material. Among the tested derivatives, compound 7 (97.1%) was identified as a more potent inhibitor of PCSK9 expression in HepG2 cells than berberine (60.9%). These results provide a better understanding of the structure–activity relationships of moracin derivatives for the inhibition of PCSK9 expression in human hepatocytes.     

Tracking the Electrocatalytic Activity of a Single Palladium Nanoparticle for the Hydrogen Evolution Reaction

The nanoparticle-based electrocatalysts’ performance is directly related to their working conditions. In general, a number of nanoparticles are uncontrollably fixed on a millimetre-sized electrode for electrochemical measurements. However, it is hard to reveal the maximum electrocatalytic activity owing to the aggregation and detachment of nanoparticles on the electrode surface. To solve this problem, here, we take the hydrogen evolution reaction (HER) catalyzed by palladium nanoparticles (Pd NPs) as a model system to track the electrocatalytic activity of single Pd NPs by stochastic collision electrochemistry and ensemble electrochemistry, respectively. Compared with the nanoparticle fixed working condition, Pd NPs in the nanoparticle diffused working condition results in a 2–5 orders magnitude enhancement of electrocatalytic activity for HER at various bias potential. Stochastic collision electrochemistry with high temporal resolution gives further insights into the accurate study of NPs’ electrocatalytic performance, enabling to dramatically enhance electrocatalytic efficiency.     

Milk-Derived Carbon Quantum Dots: Study of Biological and Chemical Properties Provides Evidence of Toxicity

Carbon dots (CDs) are carbon-based zero-dimensional nanomaterials that can be prepared from a number of organic precursors. In this research, they are prepared using fat-free UHT cow milk through the hydrothermal method. FTIR analysis shows C=O and C-H bond presence, as well as nitrogen-based bond like C-N, C=N and –NH₂ presence in CDs, while the absorption spectra show the absorption band at 280 ± 3 nm. Next, the Biuret test was performed, with the results showing no presence of unreacted proteins in CDs. It can be said that all proteins are converted in CDs. Photo luminance spectra shows the emission of CDs is 420 nm and a toxicity study of CDs was performed. The Presto Blue method was used to test the toxicity of CDs for murine hippocampal cells. CDs at a concentration of 4 mg/mL were hazardous independent of synthesis time, while the toxicity was higher for lower synthesis times of 1 and 2 h. When the concentration is reduced in 1 and 2 h synthesized CDs, the cytotoxic effect also decreases significantly, ensuring a survival rate of 60–80%. However, when the synthesis time of CDs is increased, the cytotoxic effect decreases to a lesser extent. The CDs with the highest synthesis time of 8 h do not show a cytotoxic effect above 60%. The cytotoxicity study shows that CDs may have a concentration and time–dependent cytotoxic effect, reducing the number of viable cells by 40%.     

Hypsizygus marmoreus as a Source of Indole Compounds and Other Bioactive Substances with Health-Promoting Activities

Hypsizygus marmoreus is an edible medicinal mushroom species with a high dietary value. In this study, the fruiting bodies of commercial and self-cultivated crops and mycelium from in vitro H. marmoreus cultures (both white and brown varieties) were evaluated. This study aimed to analyze the presence of indole compounds and other biologically active substances and determine the effect that the addition of zinc and magnesium ions to the culture medium has on the content of the tested compounds in mycelial cultures. The content of indole compounds and other organic compounds was determined using high-performance liquid chromatography, the content of bioelements was determined using flame atomic absorption spectrometry, the glucan content was determined spectrophotometrically, and the antioxidant activity of extracts was estimated using DPPH, FRAP, and ABTS methods. The results showed that H. marmoreus mycelium from in vitro cultures is a good source of indole compounds, bioelements, glucans, and lovastatin. Mycelia from in vitro cultures showed the most diverse composition of indole compounds (L-tryptophan, 5-hydroxy-L-tryptophan, tryptamine, 5-methyltryptamine, and melatonin). Additionally, in vitro cultures of H. marmoreus enriched with Zn and Mg salts increased the contents of Na, Ca, Zn, 5-methyltryptamine, melatonin, protocatechuic acid, sterols, and total glucans. Only in the case of the white variety of mycelial enriched cultures, ergothioneine and Mg levels also increased. To summarize, the content of the active compounds differed depending on the H. marmoreus variety and the tested material.     

Effect of Common Cooking and Drying Methods on Phytochemical and Antioxidant Properties of Corchorus olitorius Identified Using Liquid Chromatography-Mass Spectrometry (LC-MS)

In this study, Corchorus olitorius leaves were subjected to different thermal treatments (blanching, boiling, drying, frying, and steaming) and analyzed, total phenolic content (TPC), total flavonoid content (TFC), and antioxidant activity. Furthermore, Fourier transform infrared spectroscopy (FTIR) was used to identify functional groups, while metabolites were identified with LC-MC. The TPC and antioxidant activity of C. olitorius were significantly (p < 0.05) increased by cooking and drying. The steam-cooked sample had the highest TPC (18.89 mg GAE/g) and TFC (78.42 mg QE/g). With ABTS, FRAP, and DPPH assays, the steam-cooked sample exhibited the highest antioxidant activity of 119.58, 167.31, and 122.23 µM TE/g, respectively. LC-MS identified forty-two (42) metabolites in C. olitorius that included phenolic acid derivatives, flavonoid derivatives, and amino acid derivatives. Overall, steaming appears to be the best cooking method, with respect to the retention of phytochemical compounds and antioxidant activity.     

一个新的铜(Ⅱ)配合物的合成、结构与抗微生物活性研究

利用苯妥英,二(3-氨基丙基)胺与醋酸铜反应合成了一种新的铜三元配合物[Cu(pht)2(bapa)](CH3OH)[Hpht:苯妥英(5,5-Diphenylhydantion);bapa:二(3-氨基丙基)胺(bis(3-aminopropyl)amine)].通过元素分析、红外光谱和X射线单晶衍射确定了其组成和结构.配合物属于三斜晶系,空间群为Pī.晶胞参数:a=0.84190(10)nm,b=1.37540(15)nm,c=1.5622(2)nm,α=86.038(3)°,β=82.542(2)°,γ=83.904(2)°;V=1.7807(4)nm3,Mr=729.32,Z=2,F(000)=766,Dc=1.360 g/cm3,μ=0.666 mm-1,R1=0.0692,wR2=0.1430.配合物中铜离子配位数为5,处于变形三角双锥配位环境中.测试了配合物、配体和铜盐的抑菌活性,结果表明,它们对4种细菌均有一定的活性.     

Uncommon Terpenoids from Salvia Species: Chemistry,Biosynthesis and Biological Activities

The search for new bioactive compounds from plant sources has been and continues to be one of the most important fields of research in drug discovery. However, Natural Products research has continuously evolved, and more and more has gained a multidisciplinary character. Despite new developments of methodologies and concepts, one intriguing aspect still persists, i.e., different species belonging to the same genus can produce different secondary metabolites, whereas taxonomically different genera can produce the same compounds. The genus Salvia L. (Family Lamiaceae) comprises myriad distinct medicinal herbs used in traditional medicine worldwide that show different pharmacological activities due to the presence of a variety of interesting specialized metabolites, including mono-, sesqui-, di-, sester-, tri-, tetra-, and higher terpenoids as well as phenylpropanoids, phenolic acid derivatives, lignans, flavonoids, and alkaloids. We herein summarize the research progress on some uncommon terpenoids, isolated from members of the genus Salvia, which are well recognized for their potential pharmacological activities. This review also provides a current knowledge on the biosynthesis and occurrence of some interesting phytochemicals from Salvia species, viz. C₂₃-terpenoids, sesterterpenoids (C₂₅), dammarane triterpenoids (C₃₀), and uncommon triterpenoids (C₂₀+C₁₀). The study was carried out by searching various scientific databases, including Elsevier, ACS publications, Taylor and Francis, Wiley Online Library, MDPI, Springer, Thieme, and ProQuest. Therefore, 106 uncommon terpenoids were identified and summarized. Some of these compounds possessed a variety of pharmacological properties, such as antibacterial, antiviral, antiparasitic, cytotoxic and tubulin tyrosine ligase inhibitory activities. Due to the lack of pharmacological information for the presented compounds gathered from previous studies, biological investigation of these compounds should be reinvestigated.