Major Bioactive Compounds Research Articles

Phenolic enriched fraction of Clerodendrum glandulosum Lindl. leaf extract ameliorates hyperglycemia and oxidative stress in streptozotocin-nicotinamide induced diabetic rats

BackgroundClerodendrum glandulosum Lindl. is an important ethnomedicinal shrub of Northeast India, used by traditional healers to control various ailments like diabetes, hypertension, arthritis, etc. ObjectivesThe present study was conducted to explore the anti-hyperglycemic and antioxidative effects of the polyphenol-rich fraction (PRF) of C. glandulosum leaf extract and identification of its major bioactive compounds. Further, an in-silico molecular docking study was also performed to understand the molecular interactions of the identified major compounds with some target proteins associated with diabetic complications. Materials and methodsPRF was purified from the hydromethanolic (80% MeOH) extract of leaves and subjected to assessment of in-vitro antioxidant and anti-diabetic properties. It was also subjected to evaluate the ameliorative effect during streptozotocin-nicotinamide-induced hyperglycemia in Wistar albino rats. An in-silico molecular docking study was also performed to complement the in-vitro/in-vivo studies. ResultsChemical analysis of PRF showed the presence of phenolics like caffeic acid, verbascoside, isoverbascoside, and apigenin, of which verbascoside (598.14 ± 1.24 mg/g) was found to be the principal compound. In-vitro studies showed potent antioxidant (IC50 of DPPH:32.45 ± 2.16 μg/mL; ABTS:39.08 ± 0.53 μg/mL) properties and excellent aldose reductase inhibition potential (IC50 2.18 ± 0.10 μg/mL). Treatment with PRF showed reduced blood glucose levels and increased plasma insulin levels. The results also indicate an improvement of endogenous antioxidants and suppression of inflammatory cytokines (IL-6 and TNF-α) comparable to the standard. Molecular docking studies predicted promising interactions between the identified molecules and the crucial amino acid residues of the enzymes involved in the development of hyperglycemia. ConclusionThis study revealed the antihyperglycemic and antioxidant potential of partially purified fraction PRF of C. glandulosum leaves.

Optimizing ultrasound-assisted extraction of bioactive compounds from Canthium horridum blume leaves utilizing polyols: A study on skin-related activities

The focus on reducing organic solvent usage, owing to their negative environmental and health impacts, is driving a search for innovative green alternative solvents in academia and industry. Canthium horridum Blume (CH) exhibits many therapeutic activities, including antioxidant and anti-inflammatory efficacy. The objective of this study is to evaluate the optimal solvent concentration using a simplex-lattice design with an aqueous-polyols mixture and to optimize the parameters for extracting bioactive compounds and antioxidant activities from ultrasound-assisted extraction (UAE) of CH leaves through central composite design (CCD) in response surface methodology (RSM). This study examines the total phenolic content (TPC), antioxidant activities, comparison of different extraction conditions, identification of bioactive compounds, cell cytotoxicity, cellular antioxidant activity, and melanin content reduction efficacy of the extracts. According to the findings from the simplex-lattice model, the ideal solvent composition consisted of 32.57%w/w butylene glycol, 32.92%w/w glycerine, and 34.51%w/w water. Furthermore, based on the response model, optimal extraction conditions were identified as a 15-min extraction time and a solvent-to-sample ratio of 32.94:1. In comparison to alternative extraction methods, ultrasonic-assisted extraction using the aqueous-glycerine-butylene glycol (GB-UAE) extract resulted in notably elevated TPC and antioxidant responses (p < 0.05). Major antioxidant bioactive compounds included 4-(Butoxymethyl) phenol, 3-O-Caffeoyl-4-O-methylquinic acid, Quercetin 3-(2G-glucosylrutinoside), 2,4-Dihydroxybenzoic acid and other bioactive compounds. The GB-UAE extract revealed greater cell viability than UAE using ethanol (EtOH-UAE) extract in both cytotoxicity and cellular antioxidant assays at the same concentration. Additionally, it exhibited comparable melanin content reduction efficacy at a higher concentration compared to that of EtOH-UAE extract. The researcher anticipates that the current study will advance the utilization of an aqueous-polyols system for extracting bioactive compounds extending beyond CH leaves. Although the potential applications of CH leaves in cosmetics and pharmaceutical formulations have been identified, further comprehensive mechanistic and clinical studies are required to fully understand their effects.

Cinnamaldehyde, A Bioactive Compound from the Leaves of Cinnamomum osmophloeum Kaneh, Ameliorates Dextran Sulfate Sodium-Induced Colitis in Mice by Inhibiting the NLRP3 Inflammasome.

Inflammatory bowel disease (IBD) comprises a group of idiopathic intestinal disorders, including ulcerative colitis and Crohn's disease, significantly impacting the quality of life for affected individuals. The effective management of these conditions remains a persistent challenge. The NOD-like receptor family pyrin domain-containing 3 (NLRP3) inflammasome, a complex molecular structure, regulates the production of pro-inflammatory cytokines such as interleukin-1β. Abnormal activation of the NLRP3 inflammasome plays a pivotal role in the development of IBD, making it a compelling target for therapeutic intervention. Our research revealed that cinnamaldehyde (CA), a major bioactive compound found in the leaves of Cinnamomum osmophloeum kaneh, demonstrated a remarkable ability to alleviate colitis induced by dextran sulfate sodium (DSS) in a mouse model. This effect was attributed to CA's ability to downregulate the activation of the NLRP3 inflammasome and reduce the expression of pro-inflammatory mediators in the colon. In the mechanism study, we observed that CA inhibited the NLRP3 inflammasome in macrophages, at least partially, by enhancing the autophagic response, without reducing mitochondrial damage. These findings collectively suggest that CA holds significant potential as a therapeutic agent for enhancing the management of IBD, offering a promising avenue for further research and development.

Exploring Bioactive Compounds in Cajanus cajan (L.) Millsp. Stem and their biological activities: Integration of GC-MS and LC-MS Techniques

Cajanus cajan, a well-known legume crop with nutritional significance, has been used traditionally for various therapeutic purposes. Despite its ethnomedicinal importance and rich metabolite composition, there have been limited investigations into the secondary metabolites present in its stems using advanced analytical techniques. This study aimed to enhance our understanding of the chemical composition and biological activities of underutilized C. cajan stems. GC-MS &amp; LC-MS analysis revealed flavonoids as the stem's predominant secondary metabolites. The methanol extract exhibited potent antibacterial activity against E. coli, S. aureus, and C. albicans. Major bioactive compounds, including rutin, apiin, quercetrin, and aesculine, contributed to these beneficial effects. The study also revealed a high total phenolic content of 121.5 mg GAE/g in the stem extract, further establishing C. cajan stems as a valuable source of therapeutic molecules.

Exploring the Therapeutic Potential of Spilanthol from Acmella paniculata (Wall ex DC.) R. K. Jansen in Attenuating Neurodegenerative Diseases: A Multi-Faceted Approach Integrating In Silico and In Vitro Methodologies

Neurodegenerative diseases (NDDs) are marked by progressive degeneration of neurons within the central nervous system. A notable rise in the prevalence of NDDs has been noticed in the recent past. There is an undeniable requirement for the discovery of innovative therapies aimed at treating NDDs, as current medications predominantly address symptoms rather than provide cures. Approved therapies often experience a decline in therapeutic efficacy over time and are associated with significant side effects. The current investigation explores the potential of spilanthol, the major bioactive compound isolated from Acmella paniculata, in attenuating NDDs through a multi-faceted approach combining in silico, and in vitro methodologies. In silico pharmacokinetic and toxicity screening of spilanthol indicated favorable characteristics for oral delivery, blood–brain barrier permeability, and minimal toxicity. Network pharmacology predicts that spilanthol attenuates neuroinflammation in NDDs by suppressing the toll-like receptor signaling pathway. Molecular docking and dynamics simulations demonstrate robust binding affinities between spilanthol and key proteins in the TLR4 pathway. In vitro experiments conducted using BV-2 microglial cells demonstrate the potential of spilanthol to reduce the production of proinflammatory cytokines and mediators such as NO, TNF-α, and IL-6 induced by lipopolysaccharide. The cumulative findings of the present study indicate that spilanthol mitigates neurodegeneration by alleviating neuroinflammation.

Ameliorative Effect of Natural Sesquiterpene Alcohol Cedrol Against Cerebral Ischemia Infarction-In Vitro and In Vivo Studies.

Cedrol is a major bioactive compound present in the Cedrus atlantica with numerous biological properties. In this study, we elucidated the neuroprotective properties of cedrol against ischemic infarction in animal and in vitro studies. A cerebral ischemic/reperfusion model was induced in adult Wistar rats, and oxygen-glucose deprivation/reperfusion was induced in SH-SY5Y neuronal cells and treated with different concentrations of cedrol. The percentage of water content, cerebral infarct, and neurological deficit score was assessed in experimental rats. The acetylcholinesterase activity and inflammatory cytokines were quantified to analyze the anti-inflammatory potency of cedrol. Oxidative stress marker malondialdehyde and antioxidants were quantified to evaluate the antioxidant potency of cedrol in an ischemic condition. The neuroprotective potency of cedrol was confirmed by histopathological analysis of the brain tissue of cedrol-treated I/R-induced rats. In in vitro studies, the MTT and LDH assays were performed in cedrol-treated OGD/R SH-SY5Y cells to analyze the cytoprotective effect of cedrol. The anti-inflammatory property of cedrol was confirmed by quantifying the pro-inflammatory cytokine levels in OGD/R-induced cedrol-treated SH-SY5Y cells. The results obtained prove that cedrol significantly prevents brain edema, neurological deficits, acetylcholinesterase activity, and oxidative damage in ischemic-induced rats. It inhibited neuroinflammation in ischemic-induced rats and also in in vitro models. The neuroprotective effect of cedrol during an ischemic condition was authentically established with histological analysis in an animal model and cell survival assays in an in vitro model. Overall, our results confirm that cedrol is a potent alternative drug to treat cerebral ischemia in the future.

Dual action effects of ethyl-p-methoxycinnamate against dengue virus infection and inflammation via NF-κB pathway suppression

Dengue virus (DENV) infection can lead to severe outcomes through a virus-induced cytokine storm, resulting in vascular leakage and inflammation. An effective treatment strategy should target both virus replication and cytokine storm. This study identified Kaempferia galanga L. (KG) extract as exhibiting anti-DENV activity. The major bioactive compound, ethyl-p-methoxycinnamate (EPMC), significantly reduced DENV-2 infection, virion production, and viral protein synthesis in HepG2 and A549 cells, with half-maximal effective concentration (EC50) values of 22.58 µM and 6.17 µM, and impressive selectivity indexes (SIs) of 32.40 and 173.44, respectively. EPMC demonstrated efficacy against all four DENV serotypes, targeting the replication phase of the virus life cycle. Importantly, EPMC reduced DENV-2-induced cytokines (IL-6 and TNF-α) and chemokines (RANTES and IP-10), as confirmed by immunofluorescence and immunoblot analyses, indicating inhibition of NF-κB activation. EPMC's role in preventing excessive inflammatory responses suggests it as a potential candidate for dengue treatment. Absorption, distribution, metabolism, excretion, and toxicity (ADMET) and drug-likeness for EPMC were predicted using SwissADME and ProTox II servers, showing good drug-like properties without toxicity. These findings highlight KG extract and EPMC as promising candidates for future anti-dengue therapeutics, offering a dual-action approach by inhibiting virus replication and mitigating inflammatory reactions.

Triterpenoid saponin from Panax ginseng increases the sensitivity of methicillin-resistant Staphylococcus aureus to β-lactam and aminoglycoside antibiotics.

The triterpenoid saponins, ginsenosides, are the major bioactive compound of red ginseng and can exert various physiological activities. In the present study, we examined whether red ginseng extract (RGE) exerts antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA). RGE had no bactericidal activity, at least in the range of dissolvable concentration. However, RGE reduced 0.03-0.25-fold the minimum inhibitory concentration (MIC) values of β-lactam antibiotics (oxacillin, ampicillin, carbenicillin, and cefazolin) and aminoglycoside antibiotics (kanamycin and gentamicin) against the two laboratory strains of MRSA. Moreover, the fractional inhibitory concentration index indicated the synergistic activity of RGE with each of the antibiotics. RGE also increased the kanamycin sensitivity of 15 MRSA strains isolated from human volunteers and increased the ampicillin sensitivity of five MRSA strains isolated from dairy cows diagnosed with bovine mastitis. In contrast, RGE did not alter the MIC values of fosfomycin, tetracycline, and erythromycin, suggesting that RGE acts selectively. In contrast, Triton X-100, which was reported to reduce the MIC value of β-lactam antibiotics to MRSA by increasing membrane permeability, reduced the MIC values of fosfomycin and tetracycline. These results indicate that RGE increases the bactericidal effect of antibiotics via a mechanism different from that used by Triton X-100. We found that ginsenoside Rg3 (Rg3), a component of RGE, was an essential compound that exhibits synergy activity with antibiotics. Furthermore, the non-natural compound K, which contains a common protopanaxadiol aglycon moiety with Rg3, also showed synergistic activity with antibiotics. Thus, Rg3 and compound K are potentially new antibiotic adjuvants against MRSA.IMPORTANCEMethicillin-resistant Staphylococcus aureus (MRSA) is a multidrug-resistant organism that is prevalent worldwide. Therefore, the research and development of new agents against MRSA are required. We first found that ginsenoside Rg3 (Rg3) in red ginseng, made from the roots of Panax ginseng C. A. Meyer, increased the sensitivity of β-lactam antibiotics and aminoglycoside antibiotics to MRSA. Furthermore, we identified that compound K, an unnatural ginsenoside analog, also increased the sensitivity of antibiotics to MRSA, similar to Rg3. By contrast, neither Rg3 nor compound K increased the sensitivity of fosfomycin, tetracycline, and erythromycin to MRSA, suggesting that these act selectively. In the present study, the natural compound Rg3 and its structural isomer, compound K, are potentially new antibiotic adjuvants against MRSA. Currently, multiple antibiotics are used to treat MRSA, but the use of these adjuvants is expected to enable the treatment of MRSA with a single antibiotic and low concentrations of antibiotics.

Effects of geographical origin and post-harvesting processing on the bioactive compounds and sensory quality of Brazilian specialty coffee beans

Specialty coffee beans are those produced, processed, and characterized following the highest quality standards, toward delivering a superior final product. Environmental, climatic, genetic, and processing factors greatly influence the green beans’ chemical profile, which reflects on the quality and pricing. The present study focuses on the assessment of eight major health-beneficial bioactive compounds in green coffee beans aiming to underscore the influence of the geographical origin and post-harvesting processing on the quality of the final beverage. For that, we examined the non-volatile chemical profile of specialty Coffea arabica beans from Minas Gerais state, Brazil. It included samples from Cerrado (Savannah), and Matas de Minas and Sul de Minas (Atlantic Forest) regions, produced by two post-harvesting processing practices. Trigonelline, theobromine, theophylline, chlorogenic acid derivatives, caffeine, caffeic acid, ferulic acid, and p-coumaric acid were quantified in the green beans by high-performance liquid chromatography with diode array detection. Additionally, all samples were roasted and subjected to sensory analysis for coffee grading. Principal component analysis suggested that Cerrado samples tended to set apart from the other geographical locations. Those samples also exhibited higher levels of trigonelline as confirmed by two-way ANOVA analysis. Samples subjected to de-pulping processing showed improved chemical composition and sensory score. Those pulped coffees displayed 5.8% more chlorogenic acid derivatives, with an enhancement of 1.5% in the sensory score compared to unprocessed counterparts. Multivariate logistic regression analysis pointed out altitude, ferulic acid, p-coumaric acid, sweetness, and acidity as predictors distinguishing specialty coffee beans obtained by the two post-harvest processing. These findings demonstrate the influence of regional growth conditions and post-harvest treatments on the chemical and sensory quality of coffee. In summary, the present study underscores the value of integrating target metabolite analysis with statistical tools to augment the characterization of specialty coffee beans, offering novel insights for quality assessment with a focus on their bioactive compounds.

Withania somnifera (L.) Dunal: Enhanced production of withanolides and phenolic acids from hairy root culture after application of elicitors

Withania somnifera (L.) Dunal is an important indigenous medicinal plant with extensive pharmaceutical potential. The root is the main source of major bioactive compounds of this plant species including withanolides, withanine, phenolic acids, etc. Hairy root culture (HRC) is a crucial method for low-cost production of active compounds on a large scale. Four different Agrobacterium rhizogenes strains have been used for the hairy root induction. Maximum transformation efficiency (87.34 ± 2.13%) was achieved with A4 bacterial strain-mediated transformed culture. The genetic transformation was confirmed by using specific primers of seven different genes. Seven HR (Hairy root) lines were selected after screening 29 HR lines based on their fast growth rate and high accumulation of withanolides and phenolic acids content. Two biotic and three abiotic elicitors were applied to the elite root line to trigger more accumulation of withanolides and phenolic acids. While all the elicitors effectively increased withanolides and phenolic acids production, among the five different elicitors, salicylic acid (4.14 mg l–1) induced 11.49 -fold increase in withanolides (89.07 ± 2.75 mg g–1 DW) and 5.34- fold increase in phenolic acids (83.69 ± 3.11 mg g− 1 DW) after 5 days of elicitation compared to the non-elicited culture (7.75 ± 0.63 mg g–1 DW of withanolides and 15.66 ± 0.92 mg g–1 DW of phenolic acids). These results suggest that elicitors can tremendously increase the biosynthesis of active compounds in this system; thus, the HRC of W. somnifera is cost-effective and can be efficiently used for the industrial production of withanolides and phenolic acids.

Simultaneous quantitation of 15 bioactive components in Yupingfeng granules by LC-MS/MS.

Yupingfeng granules (YPFG) is commonly used in the treatment of immunological diseases, inflammations, and pulmonary diseases. Several studies have found that chromones, flavones, and saponins were the major bioactive compounds of YPFG. However, few studies have reported accurate quantification methods of these compounds. This study aimed to establish a simple and rapid method by using liquid chromatography-tandem mass spectrometry (LC-MS/MS) to determine 15 bioactive compounds in YPFG. The experimental parameters including extraction methods, extraction solvents, extraction time, solid-liquid ratio, and LC-MS/MS condition were optimized. The linearity, precision, repeatability, stability, and recovery of the established method were evaluated. The contents of 15 bioactive compounds in seven batches of YPFG samples were analyzed by the established method and the results were compared with the values determined by HPLC. The optimal extraction condition was to extract 0.1 g of YPFG by ultrasound with 50 mL 50% ethanol for 30 min. A Waters ACQUITY UPLCBEH C18 column using the 0.1% formic acid water solution and acetonitrile as mobile phase with a gradient elution was applied to the chromatographic separation. The linearity, precision, repeatability, stability, and recovery of the method were within acceptable ranges. Compared with HPLC analysis methods in Chinese Pharmacopoeia and literature, the established method was faster, simpler, more accurate, and more reliable. The method of simultaneous determination of 15 components in YPFG by LC-MS might provide a basis for the study of the bioactive compounds and the improvement of the quality standard of YPFG.

A Review with a Focus on Vaccinium-Berries-Derived Bioactive Compounds for the Treatment of Reproductive Cancers.

Cancers of the reproductive organs, including prostate, bladder, ovarian, and cervical cancers, are considered the most common causes of death in both sexes worldwide. The genus Vaccinium L. (Ericaceae) comprises fleshy berry crop species, including cranberries, blueberries, lingonberries, bilberries, and bog bilberries, and are widely distributed in many countries. Flavonols, anthocyanins (ACNs), proanthocyanidins (PACs), and phenolic acids are the most bioactive compounds naturally found in Vaccinium berries and have been extensively used as anticancer agents. However, it remains uncertain whether Vaccinium bioactives have a therapeutic role in reproductive cancers (RCs), and how these bioactives could be effective in modulating RC-related signalling pathways/molecular genes. Therefore, this article aims to review existing evidence in the PubMed/MEDLINE database on Vaccinium berries' major bioactive compounds in RC treatment and unravel the mechanisms underlying this process.

&lt;i&gt;In Silico&lt;/i&gt; Evaluation of Bioactive Compounds from Gokshura (&lt;i&gt;Tribulus terrestris&lt;/i&gt; L.) and &lt;i&gt;Punarnava&lt;/i&gt; (&lt;i&gt;Boerhavia diffusa&lt;/i&gt; L.) for their Nephroprotective Activity in Chronic Kidney Disease and Related Complications

Kidney diseases are one of the leading causes of mortality worldwide. Diabetes and hypertension are the main causes of kidney failure resulting in 3 out of 4 new cases. Most of the conventional drugs used in various disease conditions are reported for their nephrotoxic actions and their continuous use can also damage the kidneys. Ayurveda recommends certain herbal drugs like Gokshura (Tribulus terrestris L.) and Punarnava (Boerhavia diffusa L.) which can control endstage kidney disease and its complications through the rejuvenation of the kidneys. The present study is an effort to show the nephroprotective potential of bioactive compounds present in Tribulus terrestris L. and Boerhavia diffusa L. against critical nephroprotective targets carbonic anhydrase II, renin, HIF propyl hydroxylase 2/ EGLN1, angiotensin-converting enzyme II, vasopressin receptor 2 against their respective standard drugs through in silico technique and to verify the probable efficacy of these herbs in chronic kidney disease against modern medication. Discovery Studio (DS Visualizer 2016) and Auto Dock tool (ADT Tools-1.5.6) were used for molecular docking. Among the major bioactive compounds screened, chlorogenin, hecogenin, diosgenin, neotigogenin and beta-sitosterol from Tribulus terrestris L., Beta-sitosterol, boerhavisterol, liriodenine, boerhadiffusene and ursolic acid from Boerhavia diffusa L. observed to exhibit significantly higher binding energy (BE) and inhibition constant (IC50) towards CA II, Renin, EGLN1, ACE II and V2R than their respective standard drugs. The study has demonstrated the nephroprotective activity of Tribulus terrestris L. and Boerhavia diffusa L. by inhibiting receptor activity against standard drug molecules.

Chemical profiling and in-silico prediction of bioactive compounds from Wrightia tinctoria R.Br to treat psoriatic arthritis

Psoriatic arthritis (PsA) is an autoimmune-mediated inflammatory skin condition with limited remedies. This study mainly focuses on exploring the therapeutic efficiencies of Wrightia tinctoria R.Br (WT) for the treatment of PsA. Quantification and chemical profiling for the WT leaves were tested using standard in vitro biochemical assays. The ethanol extract of WT has been found to have high amounts of phenolic (24.48±0.03 mg/mL) and flavonoid (29.2±0.16 mg/mL) contents when compared to other solvent fractions. We also conducted a series of in vitro assays, including DPPH, nitric oxide radical scavenging, and protein denaturation inhibition assays, to assess the overall antioxidant and anti-inflammatory capabilities of WT extracts. The GC-MS analysis of WT leaf extract displayed Lup-20(29)-en-3-yl acetate, 24-Norursa-3,12-diene, and 3-O-Methyl-D-fructose as major bioactive compounds. The screened bioactive compounds, via pharmacokinetic and pharmacodynamic analysis, were subjected to density functional theory for energy minimization. Further, the hub targets of PsA were filtered from the Open Target online database to study the drug-target interaction. CD4, CXCL12, KLRD1, MMP9, and SERPINA1 were found to be the primary targets, which have a central role in the disease pathway. Selected disease targets were then docked with the energy-minimized bioactive compounds from WT leaves using PyRx. The results suggest that the ethanolic leaf extract from WT leaves could alter the progression of pathway mediators and effectively manage the PsA.

Eucommia ulmoides Leaves Alleviate Cognitive Dysfunction in Dextran Sulfate Sodium (DSS)-Induced Colitis Mice through Regulating JNK/TLR4 Signaling Pathway.

Ulcerative colitis (UC) is one of the inflammatory bowel diseases (IBD) that is characterized by systemic immune system activation. This study was performed to assess the alleviative effect of administering an aqueous extract of Eucommia ulmoides leaves (AEEL) on cognitive dysfunction in mice with dextran sulfate sodium (DSS)-induced colitis. The major bioactive compounds of AEEL were identified as a quinic acid derivative, caffeic acid-O-hexoside, and 3-O-caffeoylquinic acid using UPLC Q-TOF/MSE. AEEL administration alleviated colitis symptoms, which are bodyweight change and colon shortening. Moreover, AEEL administration protected intestinal barrier integrity by increasing the tight junction protein expression levels in colon tissues. Likewise, AEEL improved behavioral dysfunction in the Y-maze, passive avoidance, and Morris water maze tests. Additionally, AEEL improved short-chain fatty acid (SCFA) content in the feces of DSS-induced mice. In addition, AEEL improved damaged cholinergic systems in brain tissue and damaged mitochondrial and antioxidant functions in colon and brain tissues caused by DSS. Also, AEEL protected against DSS-induced cytotoxicity and inflammation in colon and brain tissues by c-Jun N-terminal kinase (JNK) and the toll-like receptor 4 (TLR4) signaling pathway. Therefore, these results suggest that AEEL is a natural material that alleviates DSS-induced cognitive dysfunction with the modulation of gut-brain interaction.

Evaluation of Neuroprotective effect of Bioactive compounds of Mucuna monosperma in PD lines of Drosophila melanogaster

Parkinson's Disease (PD) is a progressive neurodegenerative disorder that affects the nervous system. Oxidative stress (OS) plays an important role in the degeneration of dopaminergic neurons in PD. Ongoing research is focused on discovering new plant sources and developing alternative methods of production to meet the increasing demand for the treatment of Parkinson's disease. Ethnopharmacognosy plays a vital role in bridging traditional knowledge with modern science, and the screening of natural compounds from edible plants is a valuable approach to discovering new therapeutic agents. Hence, the exploration of plants and their bioactive compounds for drug development is an ongoing and promising field. This paper embodies results on neuroprotective property of Mucuna monosperma (MM), two major bioactive compounds namely l-3,4-dihydroxyphenylalanine (L-DOPA) and Ursolic acid were identified and isolated by Prep-HPLC and Column chromatography respectively. Further, quantified the isolated compounds by HPLC. The antioxidant property of crude, L-Dopa and Ursolic acid were scrutinized and verified through DPPH and Nitric oxide scavenging assay. To evaluate the neuroprotective property and anti-ageing effect of bioactive compounds, negative geotaxis, courtship behavior and longevity studies were made in Transgenic PD line of Drosophila melanogaster against oxidative stress status. Result reveals that the climbing ability, courtship behaviors and longevity were significantly increased in PD lines (Elva/SNCA-A30P) under stress conditions. Further it was noticed that synergetic effects of Ursolic acid along with L-Dopa showed excellent result.

How does harvest time affect the major fatty acids and bioactive compounds in hazelnut cultivars (Corylus avellana L.)?

This study was conducted to investigate the effects of harvest time on the protein, oil, fatty acids and bioactive compounds in hazelnut cultivars (Corylus avellana L. cvs. ‘Tombul’, ‘Palaz’, ‘Çakıldak’, ‘Okay 28’ and ‘Allahverdi’). The harvest was carried out at 7 different periods with weekly intervals from 20 July to 31 August. As the harvest time progressed, increases and decreases were detected in protein, oil, fatty acids and bioactive compounds. The highest oil content was measured in the H5 and H6 harvest periods. The highest content was determined in H3 for oleic acid. Higher total phenolics, total flavonoids and antioxidant activity were obtained in the first 3 harvest periods than in the other periods. The present findings revealed that the protein, fatty acids and bioactive compounds in hazelnut cultivars may differ according to the harvest time. The results obtained will provide clearer ideas to both the industry and the producers about the optimum harvest time for the intended use of these cultivars.

Ultrasonication assisted percolation extraction, isolation, identification and in silico studies of secondary metabolites from Caesalpinia bonduc (L.) Roxb. seeds with special reference to the target proteins involved in Benign Prostatic Hyperplasia

Medicinal plant-derived phytochemicals provide a vast pool of diverse bioactive compounds for novel drug development. Caesalpinia bonduc L. Roxb. is a traditional medicinal plant that is reported for diverse pharmacological properties. This study aims to compare conventional (maceration) and novel extraction techniques (ultrasonication assisted maceration extraction) to evaluate their efficiency, yield and bioactive potential of hydroalcoholic extracts from C. bonduc seeds. Furthermore, the study also aimed to isolate the bioactive compounds from the hydroalcoholic seed extract obtained from ultrasonication assisted maceration and in-silico studies of isolated compounds against the protein targets involved in Benign Prostatic Hyperplasia (BPH). For comparing the influence of extraction methods, the seeds were extracted using a novel and conventional techniques. Chemical profiling, antioxidant activities, cytotoxic and apoptotic studies were conducted using obtained extracts. The extract yielded from the novel technique recorded the highest yield, significant antioxidant activity, cytotoxicity and chemical content when compared to the conventional technique. From the hydroalcoholic extract, three major bioactive compounds, namely ethyl glucoside, methyl lineolate and linoleic acid, were isolated using column chromatography. The structures of the compounds were elucidated on the basis of extensive NMR (1H, 13C, DEPT, 2D NMR- HMBC and HSQC) and HR-ESI-MS analysis. In-silico anti-BPH activity of isolated compounds clearly reveals that the compounds were targeting 5α‒Reductase and α1-Adrenoceptor linked to the BPH progressions. Based on this investigation, it is demonstrated that isolated molecules or active molecule-enriched fractions of C. bonduc should be further researched to confirm the anti-BPH activity through in-depth preclinical and clinical research for the development of products. Ethyl glucoside and methyl lineolate were isolated for the first time from C. bonduc.

Phytochemical Screening and Gas Chromatography-Mass Spectrometry Analysis of Bioactive Compounds Present in Stem Bark of &amp;lt;i&amp;gt;Picralima nitida &amp;lt;/i&amp;gt;(stapf)

Over the years, traditional societies and ethnic nationalities have engaged plants with medicinal properties for the treatment of a range of diseases without any scientific knowledge of it inherent bioactive compounds that are responsible for its medicinal and pharmacological potentials. The aim of this study is to screen for the presence of phytochemical constituents and to identify the bioactive compounds domicile in the stem bark of &amp;lt;i&amp;gt;Picralima nitida &amp;lt;/i&amp;gt;by the use of Gas Chromatography - Mass Spectrometry. The result of the quantitative investigation of the stem bark extract of &amp;lt;i&amp;gt;P. nitida&amp;lt;/i&amp;gt; showed the presence of some phytochemical compounds such as saponins (3.22%), alkaloids (2.43%), flavonoids (6.05%) tannins (6.25%), oxalate (12.70%), phytate (2.87%), anthracene glycosides (2.14%) and cyanogenic glycosides (1.37%). Eleven (11) different bioactive compounds were recognized in the stem bark extract of &amp;lt;i&amp;gt;P. nitida&amp;lt;/i&amp;gt; by Gas Chromatography - Mass Spectrometry analysis. The percentage of major bioactive compounds were vitamin E (69.31%), Cis-Myrtanol (5.57%), Octadecanoic acid methyl ester (4.52%), 11-Octadecenoic acid methyl ester (4.42%), 9-Methyl-2-phenyl-9H-imidazo (1,2-a) benzimidazole (3.70%), Pentadecanoic acid 14-methyl- methylester (3.21%) and 7,9-Dimethyl-6H-Indolo (2,3-b) quinoxaline (3.11%). From these findings, it could be concluded that &amp;lt;i&amp;gt;P. nitida &amp;lt;/i&amp;gt;stem bark is rich in various bioactive compounds which possess antioxidant, laxative and other diverse medicinal properties. Therefore, it can be recommended as a plant of phytomedicinal value.

Physiologically based pharmacokinetic modeling for confirming the role of CYP3A1/2 and P-glycoprotein in detoxification mechanism between glycyrrhizic acid and aconitine in rats.

Fuzi, an effective common herb, is often combined with Gancao to treat disease in clinical practice with enhancing its efficacy and alleviating its toxicity. The major toxic and bioactive compounds in Fuzi and Gancao are aconitine (AC) and glycyrrhizic acid (GL), respectively. This study aims to elucidate detoxification mechanism between AC and GL from pharmacokinetic perspective using physiologically based pharmacokinetic (PBPK) model. In vitro experiments exhibited that AC was mainly metabolized by CYP3A1/2 in rat liver microsomes and transported by P-glycoprotein (P-gp) in Caco-2 cells. Kinetics assays showed that the Km and Vmax of AC towards CYP3A1/2 were 2.38 μM and 57.3pmol/min/mg, respectively, whereas that of AC towards P-gp was 11.26 μM and 147.1pmol/min/mg, respectively. GL markedly induced the mRNA expressions of CYP3A1/2 and MDR1a/b in rat primary hepatocytes. In vivo studies suggested that the intragastric and intravenous administration of GL significantly reduced systemic exposure of AC by 27% and 33%, respectively. Drug-drug interaction (DDI) model of PBPK predicted that co-administration of GL would decrease the exposure of AC by 39% and 45% in intragastric and intravenous dosing group, respectively. The consistency between predicted data and observed data confirmed that the upregulation of CYP3A1/2 and P-gp was the crucial detoxification mechanism between AC and GL. Thus, this study provides a demonstration for elucidating the compatibility mechanisms of herbal formula using PBPK modeling and gives support for the clinical co-medication of Fuzi and Gancao.