Chemistry and Bioactivity of the Genus Persea ‐ A Review

Posted on 23 September 2023 by

Abstract

This review provides the first comprehensive appraisal of bioactive compounds and their biological activities in Persea species from 1950 to 2023. Relevant articles from reputable databases, including PubMed, Web of Science, Science Direct and Google Scholar were collected, leading to the isolation of about 141 metabolite compounds, mainly flavonoids, terpenoids, fatty alcohols, lignoids, and γ-lactone derivatives. These compounds exhibit diverse biological activities, including insecticidal, antifeedant, nematicidal, antibacterial, antifungal, antiviral, cytotoxic, anti-inflammatory, and antioxidant properties. The review emphasizes the significant chemical and pharmacological potential of different Persea species, encouraging further research in various fields and medicine. Valuable insights into potential applications of Persea plants are provided.

Phytochemical Profiling by UPLC‐ESI‐QTOF‐MS of Kalaharia uncinata (Schinz) Moldenke, Widely Used in Traditional Medicine in DR Congo

Posted on 23 September 2023 by

Abstract

Kalaharia uncinata (Schinz) Moldenke, is a tropical erect bushy shrub or subshrub of the Lamiaceae family. It is an endemic plant species of Southern Africa, widely used in the pharmacopoeia against upper respiratory tract infections. A previously conducted ethnobotanical survey revealed that it is believed to contain bioactive substances. However, no relevant phytochemical information was available. This study aimed to perform a phytochemical characterization of K. uncinata and also to discuss the potential bioactivity of the identified phytochemical constituents based on documented data. Ultra-performance liquid chromatography with electrospray ionization quadrupole time-of-flight mass spectrometry (UPLC-ESI-QTOF-MS) was used for profiling and identification of the main phytochemical constituents from leaf extracts (MeOH 90 %, DCM, AcOEt, BuOH, hexane and residue) of K.uncinata. Twenty-four constituents, representing mainly flavonoids (14), followed by phenylethanoid glycosides (7), phenolic acids (2), and an iridoid glycoside (1) were tentatively identified. Most of the identified compounds are documented to have antiviral and anti-inflammatory properties, which could possibly be the rationale behind the use of K. uncinata against upper respiratory tract infections.

Synthesis and Computational Exploration of Morpholine Bearing Halogenated Sulfonamides as Potential Tyrosinase Inhibitors

Posted on 23 September 2023 by

Abstract

In the presented work, a new series of three different 4-((3,5-dichloro-2-[(2/4-halobenzyl)oxy]phenyl)sulfonyl)morpholines was synthesized and the structure of these compounds were corroborated by ¹H-NMR & ¹³C-NMR studies. The in vitro results established all the three compounds as potent tyrosinase inhibitors relative to the standard. The Kinetics mechanism plots established that compound 8 inhibited the enzyme non-competitively. The inhibition constants K_i calculated from Dixon plots for this compound was 0.0025 μM. Additionally, computational techniques were used to explore electronic structures of synthesized compounds. Fully optimized geometries were further docked with tyrosinase enzyme for inhibition studies. Reasonably good binding/interaction energies and intermolecular interactions were obtained. Finally, drug likeness was also predicted using the rule of five (RO5) and Chemical absorption, distribution, metabolism, excretion, and toxicity (ADMET) characteristics. It is anticipated that current experimental and computational investigations will evoke the scientific interest of the research community for the above-entitled compounds.

Effect of Ultrasonic Treatment on Structure, Antibacterial Activity of Sugarcane Leaf Polysaccharides

Posted on 23 September 2023 by

Abstract

This study investigated the impact of ultrasonic extraction (UE) on the structure and in vitro antibacterial activity of polysaccharides from sugarcane leaves (SLW). Native sugarcane leaf polysaccharides were treated with ultrasound (480 W) for 3 h to yield sugarcane leaf polysaccharides (SLU). Compared to SLW (33.59 kDa), the molecular weight of SLU (13.08 kDa) was significantly decreased, while the monosaccharide composition of SLU was unchanged. The results of SEM and XRD indicated that UE significantly changed the surface morphology of SLW and destroyed its inner crystalline structure. In vitro experiments showed that SLU had stronger antibacterial activity. These findings revealed that UE treatment could alter the tertiary structure of SLW but had no impact on its primary structure. Furthermore, the antibacterial activity of SLW could be greatly enhanced after UE treatment. As a bioactive additive, SLU has great application potential in functional foods, cosmetics, and pharmaceuticals.

Antioxidant and Enzyme Inhibitory Activities of Rhoifolin Flavonoid: In Vitro and in Silico Studies

Posted on 23 September 2023 by nGokhan Zengin, nNada M. Mostafa, nYasmin M. Abdelkhalek, nOmayma A. Eldahshann

Abstract

Rhoifolin (apigenin-7-O-β-neohesperidoside) belongs to the class of flavonoids and was reported to exhibit anti-inflammatory, cytotoxic, antidiabetic, hepatoprotective, and cardioprotective activities. The current study presents the in-vitro evaluation of the antioxidative effects of rhoifolin by many assays, namely DPPH, CUPRAC, ABTS, phosphomolybdenum, and FRAP. Enzyme inhibitory potential was also evaluated for acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, amylase, and glucosidase enzymes. While results revealed weak antioxidant activities for rhoifolin, the compound demonstrated some promising enzyme inhibitory effects against BChE (4.03 mg GALAE/g) and tyrosinase (7.44 mg KAE/g) but was not active on AChE. Regarding anti-diabetic enzymes, the compound was active on amylase but did not show any inhibition effect on glucosidase. In-silico molecular docking study was performed for rhoifolin on the active site of NADPH oxidase, BChE, and amylase enzymes to verify the observed enzyme inhibitory effect. Good binding affinities were observed for rhoifolin on all the docked enzymes, revealing numerous hydrogen bonds, carbon-hydrogen, van der Waals interactions. This is the first study to evaluate the enzyme inhibition potential of rhoifolin. We concluded that the increase in the degree of glycosylation might decrease the antioxidant abilities of flavonoids and that rhoifolin had moderate enzyme inhibition abilities to be investigated in future studies.

The Phytochemical Tactics for Battling Antibiotic Resistance in Microbes: Secondary Metabolites and Nano Antibiotics Methods

Posted on 23 September 2023 by nMujahid Habib Adam, nNitin Tandon, nIqubal Singh, nRunjhun Tandonn

Abstract

One of the most serious threats to human health is antibiotic resistance, which has left the world without effective antibiotics. While continuous research and inventions for new antibiotics are going on, especially those with new modes of action, it is unlikely that this alone would be sufficient to win the battle. Furthermore, it is also important to investigate additional approaches. One such strategy for improving the efficacy of existing antibiotics is the discovery of adjuvants. This review has collected data from various studies on the current crisis and approaches for combating multi-drug resistance in microbial pathogens using phytochemicals. In addition, the nano antibiotic approaches, are discussed, highlighting the high potentials of essential oils, alkaloids, phenolic compounds, and nano antibiotics in combating antibiotic resistance.

Citrus Honeys from Three Different Regions of Turkey: HPLC‐DAD Profiling and in Vitro Enzyme Inhibition, Antioxidant, Anti‐Inflammatory and Antimicrobial Properties with Chemometric Study

Posted on 23 September 2023 by

Abstract

The objectives of the present study are to compare the phenolic profiles and biological activities of 15 citrus honey samples from three different locations in Turkey using a chemometric approach. The HPLC-DAD analysis was used to determine phenolic profiles. Nineteen phenolic compounds were identified. Gallic acid (107.14–717.04 μg/g) was recorded as the predominant compound. AF (Antalya-Finike) had the highest antioxidant activity in ABTS⋅⁺ (IC₅₀: 18.01±0.69 mg/mL), metal chelating (IC₅₀: 6.20±0.19 mg/mL) and CUPRAC (A_0.50: 12.05±0.68 mg/mL) assays, while it revealed the best anti-inflammatory activity against COX-2 (17.28±0.22 %) and COX-1 (43.28±0.91 %). AM (Antalya-Manavgat) was the most active in β-carotene-linoleic acid (IC₅₀: 10.05±0.19 mg/mL), anti-urease (38.90±0.69 %), anti-quorum sensing and antimicrobial activities. AKO1 (Adana-Kozan-1) in DPPH⋅ (IC₅₀: 34.25±0.81 mg/mL) assay, AKU1 (Antalya-Kumluca-1) in tyrosinase inhibition activity (37.73±0.38 %) assay, AKU2 (Antalya-Kumluca-2) in AChE (10.55±0.63 %) and BChE (9.18±0.45 %) inhibition activity assays showed the best activity. Chemometric tools were applied to the phenolic compositions and biological properties. PCA and HCA ensured that 15 citrus honey samples were grouped into 3 clusters. The results showed that myricetin, kaempferol, vanillin, protocatechuic acid, rosmarinic acid, rutin, vanillic acid, gallic acid, catechin and p-hydroxyphenyl acetic acid are phenolic compounds that can be used in the classification of citrus honeys.

Design, Synthesis, Molecular Modelling and in Vitro Evaluation of Indolyl Ketohydrazide‐Hydrazone Analogs as Potential Pancreatic Lipase Inhibitors

Posted on 23 September 2023 by nSakshi Jagetiya, nPrashant S. Auti, nAtish T. Pauln

Abstract

Inhibition of Pancreatic lipase (PL) is considered to be a promising target for the management of obesity, owing to its crucial role in the digestion of dietary triglycerides. A series of 31 indolyl ketohydrazide-hydrazone analogs (5 aa–cm) were designed, synthesized and evaluated for their PL inhibitory potential. The analogs were designed using molecular modelling studies. The designed analogs were then synthesized by condensation of indolyl oxoacetohydrazide with various substituted benzaldehydes. All the synthesized analogs showed PL inhibitory activity in the range of 4.13–48.35 μM, as compared with orlistat (0.86±0.09 μM). The most potent analog 5 bi (IC₅₀=4.13±0.95 μM) was found to show a competitive type of inhibition with K_i value of 0.725 μM. Additionally, the molecular docking study proved the binding of analog 5 bi at the active site of PL (PDB ID: 1LPB) with MolDock score of −141.279 kcal/mol. It also exhibited various interactions with the key amino acids namely Phe77, Phe215, Tyr114, Ser152, Arg256, His263, etc. Furthermore, the protein-ligand complex of analog 5 bi was found to be stable in molecular dynamics simulation for 100 ns with RMSD of less than 3.2 and 4 Å for the protein and ligand, respectively. The current work hereby provides a basis for the potential role of indolyl ketohydrazide-hydrazone analogs in PL inhibition and further optimization could result in the generation of new leads as anti-obesity agents.

Nutritional Composition Profiles and Quality Evaluation of Different Cultivars of Asparagus Officinalis with Potential as Functional Foods and Health‐Care Products

Posted on 23 September 2023 by nWei Liu, nMengyu Sun, nDongxue Yin, nGuofeng Zhang, nZhihao Wang, nXiaoqiang Cuin

Abstract

Asparagus officinalis is a health-care vegetable with homology value of medicine and food. The quality of A. officinalis is greatly different from various cultivars. It is essential to reveal the relationship between the variety and quality. This study investigated six nutritional compositions in ten A. officinalis cultivars, including amino acid, mineral substance, carbohydrate, vitamin C, protein and total sugar. Five chemometrics methods were further employed to evaluate their quality. The results consistently showed that ten varieties were divided into three grades as nutritional composition differences. HuaMiaoF1, JinGuan and FeiCuiMingZhu were grouped into cluster3 with the best quality, and Atlas and Jersey Giant were grouped into cluster1 with the lowest quality. Therefore, HuaMiaoF1, JinGuan and FeiCuiMingZhu can be suggested as good raw materials for medicine, food and health-care products industries. Meanwhile, the comprehensive application of five chemometrics methods was confirmed as a reliable methodology for quality evaluation of A. officinalis.

Research on the Chemical Constituents against Alzheimer’s Disease of the Fruits of Physalis alkekengi L. var. franchetii (Mast.) Makino

Posted on 23 September 2023 by nYang Teng, nQi Yuan, nYou Wu, nShuang Wu, nJin Su, nPengxia Zhang, nYu Zhangn

Abstract

Physalis alkekengi L. var. franchetii (Mast.) Makino (PA) is a natural plant which is utilised as a traditional herbal medicine. It has properties that make it effective against inflammation and free radical damage. In the present study, the major constituents of four extraction parts of the fruits of PA (PAF) were investigated by combining ultra-performance liquid chromatography with quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS). The mice model of Alzheimer's disease (AD) induced by aluminum chloride (AlCl₃) combined with D-galactose (D-gal) was established to comprehend the mechanism behind PAF's anti-AD activity from both behavioural and pathological perspectives. The results showed that four extraction parts of PAF (PAFE) had favorable anti-AD effects and the ethyl acetate (EA) group showed the best activity. UPLC-Q-TOF-MS analysis identified Physalin B, Nobiletin and Caffeic acid as the main anti-AD active constituents in EA extract. This study reveals that PAF can reduce neuroinflammatory damage by inhibiting p38 mitogen-activated protein kinase (p38 MAPK) signaling pathway, which is the theoretical basis for clinical development and utilization of PAF in AD therapy.