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

Justicia schimperiana, known as "Dhumuugaa" in Afan Oromo and "Sensel" or "Smiza" in Amharic, is traditionally used to treat ailments such as scabies, fever, asthma, diarrhea, malaria, and more. This study explored the chemical composition and biological activity of its extracts and isolated compounds. The essential oils were extracted using the hydrodistillation method, and their chemical composition was evaluated using GC-MS. GC-MS analysis identified 54 and 52 chemical components in the essential oils (EOs) from roots and leaves, respectively. The structures of the isolated compounds have been identified using 1D and 2D-NMR techniques. Six compounds - β-sitosterol (1), 5-methoxy durmillone (2), trans-resveratrol (3), tricuspidatol A (4), kaempferol-3-O-α-rhamnopyranoside (5), and kaempferol-3-O-rutinoside (6) - were isolated from the root extracts and reported for the first time in this species. The antimicrobial activity was evaluated using the broth microdilution technique. EOs extracts showed significant antibacterial activity, particularly against Staphylococcus aureus, Streptococcus agalactiae, while compound 6 showed potent activity with an MIC of 0.25 μg/mL. The antioxidant activity revealed strong radical scavenging for compounds 5 and 6, with extracts also demonstrating significant α-amylase inhibitory effects and moderate cytotoxicity against the MCF-7 cell line. Molecular docking and ADMET analysis highlighted compounds 5 and 6 as promising therapeutic agent. These findings highlight the medicinal potential of J. schimperiana roots, warranting further exploration.

Drought stress remains a serious concern in Oryza sativa L. var indica, cultivar Satabdi (IET4786) production, particularly during the earliest growth phases, ultimately affecting yield due to the recent trend of delayed rain arrival in West Bengal, India. This study aimed to develop a cost-effective strategy to improve the drought tolerance capacity of rice seedlings by priming the seeds with flavonoid-enriched extract (FEE) of French marigold (Tagetes patula) petals to withstand the initial drought milieu. The morpho-physiological and biochemical responses of rice seedlings were evaluated to perceive the priming efficacy in alleviating water stress-induced untoward effects. The findings revealed that mechanical priming of the IET4786 seeds with FEE (50 mg/mL for 30 min) significantly improved seedling survival against initial drought stress for 14 days. After 24 h of recovery from drought stress, the primed seed-derived seedlings exhibited significantly improved morphological, physiological, biochemical, and redox parameters compared to the seedlings derived from unprimed seeds under net house conditions. In search of mechanistic insights, seed priming significantly increased proline content by endorsing Δ¹-pyrroline-5-carboxylate synthetase activities, endorsed methylglyoxal clearance homeostasis by improving glyoxalase I and II activities through restoring glutathione (GSH) level, and enhanced polyamine accumulation in the leaves of seedlings to endure drought stress.

Diabetes mellitus (DM) is a group of metabolic disorders characterized by hyperglycemia due to insufficient insulin secretion or action. Contributing factors include genetic predisposition, obesity, family history, inactivity, and environmental risks. Type 2 diabetes mellitus (T2DM), the most common form, involves impaired insulin secretion by pancreatic β-cells, leading to insulin resistance. By 2045, it is projected that India and China will have approximately 134.3 and 110.8 million diabetic individuals, respectively. Although synthetic drugs are effective in managing DM, they often come with side effects. Consequently, plant-based phytochemicals with antidiabetic properties are gaining attention. Research indicates that around 115 medicinal plants (MPs) have antidiabetic effects, particularly those from the Fabaceae, Liliaceae, and Lamiaceae families. Bioactive compounds like alkaloids, triterpenoids, flavonoids, and phenolics are known to combat DM. Traditional medicinal systems, particularly in developing countries, offer effective DM management. This review highlights the importance of MPs and their bioactive compounds in treating diabetes and underscores the need for further research to commercialize plant-based antidiabetic drugs.

In order to search for new chemotypes and to carry out a comparative study with the literature, the current study investigated the chemical composition of the essential oil of the flowers of Daucus carota (L.) ssp. carota using gas chromatography coupled with mass spectrometry (GC-MS). Moreover, the antimicrobial and insecticidal potentials of essential oil were studied. Hydrodistillation was used to extract the essential oil. Due to the immiscibility of essential oils in water and, therefore, in the culture medium, emulsification was carried out using a 0.2 % agar solution to promote germ/composite contact. Fumigation with the oil phase of the essential oil was carried out in airtight and transparent plastic boxes, with a capacity of 1 L as an exposure chamber to test the lightness of essential oils against adults of Sitophilus oryzae (L.). In each box, five Petri dishes were placed. Each replicate consisted of five adults of S. oryzae (L.). The essential oils were spread on Wathman filter paper and placed inside the exposure chamber. Mortality control was carried out by counting insect deaths from the first day of treatment until the death of all individuals. α-Pinene (22.2 %) was the major compound in the essential oil of the oil phase of D. carota (L.) ssp. carota followed by β-asarone (15.1 %), sabinene (12.4 %), and α-himachalene (10.1 %), as well as the crystallized phase containing β-asarone. In terms of antimicrobial activity, the essential oils showed significant inhibition of the six bacteria and seven molds studied at a concentration of 0.45 mg/mL. The essential oils were found to be highly effective against S. oryzae (L.). This approach can help reduce the amount of synthetic antibiotics applied and, therefore, decrease the negative impact of artificial agents, such as residues, resistance, and environmental pollution.

An ideal drug carrier system should demonstrate optimal payload and release characteristics, thereby ensuring prolonged therapeutic index while minimizing adverse effects. The field of drug delivery has undergone significant advancements, particularly within the last two decades, owing to the revolutionary impact of biomaterials. The use of biomaterials presents significant due to their biocompatibility and biodegradability, which must be addressed in order to achieve effective drug delivery. The properties of the biomaterial and its interface are primarily influenced by their physicochemical attributes, physiological barriers, cellular trafficking, and immunomodulatory effects. By attuning these barriers, regulating the physicochemical properties, and masking the immune system's response, the bio interface can be effectively modulated, leading to the development of innovative supramolecular structures with enhanced effectiveness. With a comprehensive understanding of these technologies, there is a growing demand for repurposing existing drugs for new therapeutic indications within this space. This review aims to provide a substantial body of evidence showcasing the productiveness of biomaterials and their interface in drug delivery, as well as methods for mitigating and modulating barriers and physicochemical properties along with an examination of future prospects in this field.

Diabetes mellitus (DM) is a disorder which is raised at the alarming level and it is characterized by the hyperglycemia results from the impaired action of insulin, production of insulin or both of these simultaneously. Consequently, it causes problems or failure of different body organs such as kidneys, heart, eyes, nerve system. Since this disease cannot be completely cured until now, we aimed to design series of enzymes inhibitors and tested them for DM treatment. In this series, benzimidazole-based thiazolidinone bearing chalcone derivatives completed in a four step reaction and their structures were confirmed through various spectroscopic techniques. A significant efficacy on antidiabetic enzymes was observed, with IC₅₀ values ranging from 25.05 ± 0.04 to 56.08 ± 0.07 μM for α-amylase and 22.07 ± 0.02 to 53.06 ± 0.07 μM for α-glucosidase. The obtained results were compared to those of the standard glimepiride drug (IC₅₀ = 18.05 ± 0.07 µM for α-amylase and IC₅₀ = 15.02 ± 0 .03 µM for α-glucosidase). The synthesized compounds showed promising antidiabetic potency. Moreover, a molecular docking study was conducted on the most active analogs of the compounds to better understand their interactions with the active sites of the targeted enzymes.

This study investigated the effects of flavonoid-rich extract from Hibiscus sabdariffa L. (Malvaceae) leaves on liver damage in streptozotocin-induced diabetic rats by evaluating various biochemical parameters, including the molecular gene expressions of Nrf-2 and HO-1 as well as histological parameters. The extract was found to significantly reduce liver damage, as evidenced by lower levels of fragmented DNA and protein carbonyl concentrations. Oxidative stress markers, including malondialdehyde (MDA) level, were also significantly (p < 0.05) decreased, while antioxidant biomarkers, like reduced glutathione (GSH), catalase (CAT), superoxide dismutase (SOD), glutathione peroxidase (GPx), and glutathione-S-transferase (GST) were enhanced. Additionally, the extract improved the activities of key liver enzymes, including phosphatases and transaminases, and increased albumin levels. Importantly, the study demonstrated that H. sabdariffa extract effectively regulated the expression of Nrf-2 and HO-1, suggesting a significant role in mitigating liver damage. These findings highlight its potential as a therapeutic agent for liver protection in diabetic conditions.

The current work describes an efficient synthesis of Morita-Baylis-Hillman adducts (MBHAs) derived heterocycles (4, 5, 6, 7, 10, 11, 12, 13, 16 and 17) with the Michael addition of piperidine and piperazine heterocycles. The comparative studies of mono and di-hydrogen bond acceptors heterocycles, meta and para substituted nitro-phenyl rings and the isolated single diastereomer 16 through molecular docking coupled with in vivo bioactivities displayed very important results. The biological significances were observed against urease enzyme (IC₅₀ = 3.95 ± 0.10 µM). Almost all the compounds displayed different ranges of inhibition potential whereas the di-hydrogen bond donor diastereomers 12 and 13 were found to be highly potent against the targeted enzyme while the remaining had shown comparable inhibitory activity. The diastereomers 12 and 13 were the most active having minimum inhibitory concentration (MIC) IC₅₀ = 3.95 ± 0.10 µM. All the synthesized compounds were docked and their best poses were explored for enhanced biological properties. The molecular docking studies revealed better binding interactions of the ligand with the target enzyme. Furthermore, ADMET predictions were also observed which revealed drug like properties for all the novel MBHAs based piperidine and piperazine derivatives.

Inflammation, a natural process of the innate immune system, involves elevated levels of various proinflammatory mediators, such as, nitric oxide (NO) and prostaglandin (PGE₂), cytokines such as interleukin 6 (IL-6), interleukin 10 (IL-10) and tumor necrosis factor alpha (TNF-α), and enzymes including inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). This study investigated the anti-inflammatory effects of homalolide A (1) and homalomenol A (2), two sesquiterpenoids isolated from the rhizome of Homalomena pendula, on lipopolysaccharide (LPS)- stimulated macrophage cells. The results demonstrated that both 1 and 2 dose-dependently inhibited the production of PGE₂, TNF-α and IL-6 in RAW 264.7 macrophages. Furthermore, 2 also stimulated IL-10 production in RAW 264.7 cells. Consistent with these findings, these compounds suppressed the LPS-stimulated protein levels of iNOS and COX-2 in RAW 264.7 cells. These results suggested that 1 and 2 could be effective candidates for ameliorating inflammatory-associated complications.

Two new compounds (1-2) and a new artificial product (3) together with fifteen known compounds (4-18) were isolated from Viscum coloratum (Kom.) Nakai. Their structures were established by analysis of their spectroscopic data including MS, 1D and 2D NMR spectra, and comparison with existing literature. All the compounds were assessed for their cytotoxic activity against 4T1 and LN229 cells (with cisplatin as the positive control), and the anti-LN229 cytotoxicity of compounds 3, 4 and 5 were greater than that of 4T1 cells.