Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences最新文献

In the present work, one of the leading health issues i.e. cancer was targeted by synthesizing and biologically investigating the potential of pyrazine-based thiazolidinone derivatives (1-13). The basic structure of the synthesized compounds was determined using a variety of spectroscopic techniques, including ¹H NMR, ¹³C NMR, and HREI-MS. These scaffolds were studied for their biological profiles as anti-cancer as well as anti-urease agents. The biological effectiveness of these compounds was compared using the reference tetrandrine (IC₅₀ = 4.50 ± 0.20 µM) and thiourea (IC₅₀ = 5.10 ± 0.10 µM), respectively. Among novel compounds, scaffold 3, 6, 7 and 10 demonstrated an excellent potency with highest inhibitory potential (IC₅₀ = 1.70 ± 0.10 and 1.30 ± 0.20 µM), (IC₅₀ = 4.20 ± 0.10 and 5.10 ± 0.30 µM), (IC₅₀ = 2.10 ± 0.10 and 3.20 ± 0.20 µM) and (IC₅₀ = 2.70 ± 0.20 and 4.20 ± 0.20 µM), respectively, out of which scaffold 3 emerged as the leading compound due to the presence of highly reactive -CF₃ moiety which interacts via hydrogen bonding. Molecular docking investigations of the potent compounds was also carried out which revealed the binding interactions of ligands with the active sites of enzyme. Moreover, the electronic properties, nucleophilic and electrophilic sited of the lead compounds were also studied under density functional theory (DFT).

Cordyceps sinensis, known as the caterpillar fungus, constitutes an invaluable and irreplaceable part of traditional Chinese medicine (TCM) and is now gaining widespread global recognition and dedicated attention owing to both highly promising characteristics as well as grave dangers that are suggestive of an impending doom. C. sinensis possibly holds the key to the treatment of many human ailments with minimal side effects due to a wide array of biologically active chemical constituents. The powerful potential harbored by this fungus has led to a meteoric rise in its prices in the domestic and international markets which has caused the involvement of an increasing number of harvesters, traders, and buyers and unchecked overexploitation of this bioresource thus threatening its long-term survival in its natural habitat of the Himalayan region. This review focuses on the ethnopharmacology of C. sinensis, and various aspects related to its conservation, such as natural distribution, sale and revenue, decline in population density, and conservational practices prevalent in the current scenario of fungal depletion. The paper concludes with a comprehensive evaluation of the discrete therapeutic capabilities possessed by C. sinensis, the mechanistic insights into the remarkable treatment of chronic ailments using the fungus or its derivatives, and a suggested strategic roadmap that may be adopted for fruitful conservation of this natural miracle.

The aim of the present work was to investigate some of the molecular mechanisms and targets of the anticancer action of the bioflavonoid fustin isolated from the heartwood of Cotinus coggygria Scop. in the triple-negative breast cancer cell line MDA-MB-231. For this purpose, we applied fluorescence microscopy analysis to evaluate apoptosis, necrosis, and mitochondrial integrity, wound healing assay to study fustin antimigratory potential and quantitative reverse transcription-polymerase chain reaction to analyze the expression of genes associated with cell cycle control, programmed cell death, metastasis, and epigenetic alterations. A complex network-based bioinformatic analysis was also employed for protein-protein network construction, hub genes identification, and functional enrichment. The results revealed a significant induction of early and late apoptotic and necrotic events, a slight alteration of the mitochondria-related fluorescence, and marked antimotility effect after fustin treatment. Of 34 analyzed genes, seven fustin targets were identified, of which CDKN1A, ATM, and MYC were significantly enriched in pathways such as cell cycle, intrinsic apoptotic signaling pathway in response to DNA damage and generic transcription pathway. Our findings outline some molecular mechanisms of the anticancer action of fustin pointing it out as a potential oncotherapeutic agent and provide directions for future in vivo research.

This study focused on analyzing the pharmacological activities of AgNPs synthesized from an aqueous plant extract of Anchusa arvensis. The effectiveness of AgNPs was evaluated for protein kinase inhibition, antioxidant, antibacterial, and antifungal activities. The AgNPs and plant were used to regulate the protein kinase activity using the liquid TSB and ISP4 medium protein kinase inhibition study demonstrated that nanoparticles exhibited a larger zone of inhibition (9.1 ± 0.8) compared to the plant extract (8.1 ± 0.6). The antioxidant activity was assessed using DPPH reagent, and the results indicated that AgNPs displayed potent free radical scavenging properties. In terms of antibacterial activity, AgNPs showed higher efficacy against Enterobacter aerogens (20.1 ± 0.9), Bordetella bronchiseptaca (19.1 ± 0.9), and Salmonella typhimurium (17.2 ± 0.8) at 4 mg/mL. The antifungal activity of AgNPs was prominent against Aspergillus fumagatus (14.1 ± 0.9), Mucor species (19.2 ± 0.8), and Fusarium solani (11.2 ± 0.8) at 20 mg/mL. These findings suggest that AgNPs possess multiple beneficial properties, including bactericidal/fungicidal effects, protein kinase inhibition, and potential free radical scavenging abilities. Therefore, AgNPs have potential applications in various fields, such as biomedicine and industry, due to their ability to counteract the harmful effects of free radicals.

Lemongrass (Cymbopogon flexuosus) essential oil (LGEO) contains α-citral, β-citral and other phytochemicals extracted using various methods. This research extracted essential oils using steam distillation (SD) and microwave-assisted hydro distillation (MAHD) to maximize quantity and purity. LGEO was tested for antibacterial properties. LGEO was extracted using SD and compared to MAHD output based on oil production and chemical composition. We performed GCMS to characterize LGEO. Fourier transform infrared spectroscopy (FTIR) used for quantum chemical analysis. Spectroscopic analysis showed that SD extracted secondary metabolites (ethyl-linalool, isogeranial, β-citral, α-citral, geranyl acetate, and caryophyllene) yielded 9.7 %, 11.5 %, 35.4 %, 13.4 %, 6.4 %, and 6.4 %, respectively, while MAHD yielded 10.2 %, 13.4 %, 43.2 %, 17.3 %, 6.9 %, and 7.3 %. MAHD extracted α and β citral content was better than SD extraction technique. FTIR spectroscopy and quantum chemistry analysis showed extracted oil chemical composition, electronic structure of α and β citral isomers. In the disc-diffusion experiment, both extracts were effective against Gram-positive and Gram-negative bacteria and harmful fungi. LGEO from SD and MAHD extraction (30 mg/mL) demonstrated disc diffusion assay antibacterial efficacy against microorganisms. The two extracts effectively inhibited microorganisms with MIC values of 3.75 and 7.5 μg/mL. It can be concluded that, LGEO have greater antimicrobial activity in MAHD extraction.

Fluorescent liposomes are pivotal in cancer research, serving as adaptable vehicles for imaging and therapeutics. These small lipid vesicles, capable of encapsulating fluorescent dyes, offer precise visualization and monitoring of their targeted delivery to cancer cells. This review delves into the critical role fluorescent liposomes play in enhancing both cancer diagnosis and treatment. It provides an in-depth analysis of their structural features, fluorescent labeling techniques, targeting strategies, and the challenges and opportunities they present. In the domain of cancer diagnosis, the article sheds light on various imaging modalities enabled by fluorescent liposomes, including fluorescence imaging and multimodal techniques. Emphasis is placed on early detection strategies, exhibiting the utility of targeted contrast agents and biomarker recognition for enhanced diagnostic precision. Moving on to cancer treatment, the review discusses the sophisticated drug delivery mechanisms facilitated by fluorescent liposomes, focusing on chemotherapy and photodynamic therapy. Moreover, the exploration extends to targeted therapy, explaining the applications of fluorescent liposomes in gene delivery and RNA interference. In a nutshell, his article comprehensively explores the multifaceted impact of fluorescent liposomes on advancing cancer diagnosis and treatment, combining existing knowledge with emerging trends.

Rhus ruspolii Engl. plant is traditionally used in Ethiopia to treat various diseases. However, the biological and phytochemical properties of the leaves are not well documented. Hence, this study aimed to isolate phytochemicals from R. ruspolii leaves and evaluate their antibacterial and DPPH radical scavenging activities. GC-MS analysis identified 16 compounds from combined fractions 6-10. Chromatographic separation and NMR analysis resulted in the isolation and characterization of palmitic acid (7), 3,4-dihydroxybenzoic acid (17), cupressuflavone (18), amentoflavone (19), shikimic acid (20), avicularin (21), and myricetin-3-O-5''-acetylarabinofuranoside (22). The inhibition zones of extracts (100 mg/mL) and isolated compounds (5 mg/mL) ranged from 8.33 ± 0.50 to 16.33 ± 0.47 mm against all evaluated bacteria. Of all isolated compounds, compounds 18 and 21 showed good activity against Gram-negative (supported by in silico molecular docking studies) and Gram-positive bacteria, respectively. The lowest (49.1 %) and the highest (91.3 %) DPPH radicals were inhibited by combined fractions 6-10 and compound 17, respectively, at 62.5 μg/mL. The SwissADME online analysis showed compounds 17 and 20 have good solubility and permeability. The Pro Tox 3.0 online analysis revealed none of the isolated compounds are fatal if swallowed. Therefore, the findings of this study support the traditional use of the plant for treating bacteria diseases.

United Nations General Assembly declared that 2023 will be celebrated as the International Year of Millets. Millets are a group of coarse grains from the Poaceae family that offer numerous benefits that align with various United Nations Sustainable Development Goals (UN SDGs). This review explores diverse contributions of millet cultivation, consumption, and value addition with UN SDGs. The millets help in combating hunger by providing economical sources of essential nutrients and diversifying diets, improving health through mitigating malnutrition and diet-related diseases. Millet's lower water demand and resilience to climatic stress help in sustainable water management. Millets reduce the risks associated with monoculture farming and promote sustainable agricultural practices. Similarly, millet plants need few chemical fertilizers, and the ecological damage associated with these plants is minimized. Millets can prevent soil degradation and conserve biodiversity. They can adapt to diverse cropping systems and support sustainable land practices. Millet cultivation reduces inequalities by empowering smallholder farmers and maintaining economic balance. The cultivation and trading of millets promote partnerships among governments, NGOs, and businesses for sustainable development. The ability of millet to contribute to poverty reduction, hunger alleviation, health improvement, environmental sustainability, and economic development makes millet a sustainable choice for a better world.

Psoriasis, recognized as a chronic inflammatory skin disorder, disrupts immune system functionality. Global estimates by the World Psoriasis Day consortium indicate its impact on approximately 130 million people, constituting 4 to 5 percent of the worldwide population. Conventional drug delivery systems, mainly designed to alleviate psoriasis symptoms, fall short in achieving targeted action and optimal bioavailability due to inherent challenges such as the drug's brief half-life, instability, and a deficiency in ensuring both safety and efficacy. Liposomes, employed in drug delivery systems, emerge as highly promising carriers for augmenting the therapeutic efficacy of topically applied drugs. These small unilamellar vesicles demonstrate enhanced penetration capabilities, facilitating drug delivery through the stratum corneum layer of skin. This comprehensive review article illuminates diverse facets of liposomes as a promising drug delivery system to treat psoriasis. Addressing various aspects such as formulation strategies, encapsulation techniques, and targeted delivery, the review underscores the potential of liposomes in enhancing the efficacy and specificity of psoriasis treatments.