Potential Pharmacological Benefits Research Articles

A Snake Venom Peptide and Its Derivatives Prevent Aβ42 Aggregation and Eliminate Toxic Aβ42 Aggregates In Vitro.

Over a century has passed since Alois Alzheimer first described Alzheimer's disease (AD), and since then, researchers have made significant strides in understanding its pathology. One key feature of AD is the presence of amyloid-β (Aβ) peptides, which form amyloid plaques, and therefore, it is a primary target for treatment studies. Naturally occurring peptides have garnered attention for their potential pharmacological benefits, particularly in the central nervous system. In this study, nine peptide derivatives of Crotamine, a polypeptide from Crotalus durissus terrificus Rattlesnake venom, as well as one d-enantiomer, were evaluated for their ability to modulate Aβ42 aggregation through various assays such as ThT, QIAD, SPR, and sFIDA. All tested peptides were able to decrease Aβ42 aggregation and eliminate Aβ42 aggregates. Additionally, all of the peptides showed an affinity for Aβ42. This study is the first to describe the potential of crotamine derivative peptides against Aβ42 aggregation and to identify a promising d-peptide that could be used as an effective pharmacological tool against AD in the future.

Global Perspectives on the Medicinal Implications of Green Walnut and Its Benefits: A Comprehensive Review

Green walnuts have been valued for their health and medicinal effects for many years. Green walnuts have several bioactive metabolites, including polyphenols, flavonoids, and tannins, that have antioxidant, anti-inflammatory, antimicrobial, and anticancer properties. With previous records of increased inclination towards natural or botanical sources of therapeutics, green walnuts have regained the uniqueness of therapeutic prominence globally. This comprehensive review provides a deep understanding of the use of green walnut (Juglans regia L.) around the globe and shows its potential pharmacological benefits. It explores the different therapeutic and medicinal uses of green walnuts, including their historical use in traditional medicine throughout different continents and regions, including Asia, Europe, America, Africa, and the Middle East. This review also provides the substantial studies conducted on green walnuts, which investigate the bioactive substances found in various parts of the walnut tree, including the kernel, shell, leaves, shoots, bark, and roots, indulging in their health advantages. It also diversifies the antibacterial, antioxidant, anti-inflammatory, cardiovascular, and antihypertensive activities of the green walnut, which clearly shows the prospective use of the walnut in nutraceutical and medicinal applications. This review continues by emphasizing the necessity for further research to focus on and attract global researchers to aim for a detailed understanding of the pharmacological implications of green walnuts and enhance their use in traditional and modern medicine.

Traditional uses, phytochemistry, pharmacological significance and toxicology of Argemone mexicana L. – A review approach

Argemone Mexicana L. (AM, Papaveraceae) is found and native to tropical America. Many cultures have traditionally used this annual herb to treat a variety of ailments, including skin disorders, digestive problems, eye issues, and anti-dotes. Argemone Mexicana (AM), a plant with a long history of traditional use, has recently gained renewed attention from researchers due to its potential pharmacological benefits. The possibility that this plant could be used to develop new therapies has inspired further research. Information about AM was collected from scientific databases published between January 2000 and March 2022. These databases include Elsevier, PubMed, Web of Science, NOPR, Google Scholar, ResearchGate, Wiley, SpringerLink, and ACS publications. Numerous chemical constituents present in AM have been found to have medicinal properties, such as alkaloids, flavonoids, tannins, phenolic compounds, saponin, terpenoids, and cardiac glycosides. Various parts of the AM plant exhibit antimicrobial, wound healing, antioxidant, antimalarial, larvicidal, anthelmintic, antidiabetic, hepatoprotective, anticancer effects, and have been used to treat sexually transmitted diseases. However, the plant is also known to be toxic, and its use can lead to a number of adverse effects, including dermatitis, gastrointestinal disturbances, and neurological damage. This review critically evaluates recent developments in the traditional use, phytochemistry, pharmacology, and toxicology of AM in order to provide a scientific basis for reasonable utilization and further research.

Synthesis, Charecterization, Antibacterial and Cytotoxicity of Novel Metal Complexes Derived from Azomethine Ligand (Bis Azo-Schiff Base) In Vitro and In Silico

Background: Schiff bases, especially Azo-Schiff bases, are significant ligands in organic chemistry due to their coordination capabilities. They find applications in various industrial sectors and biological studies. Metal complexes of Schiff bases, particularly with tetradentate ligands, have gained attention for their potential pharmacological benefits. However, there is limited information on the biological activities of certain Schiff base complexes, such as 1H-indole-3-ethylenesalicyldamine derivatives. Method: The synthesis of bis azo-Schiff base ligands and their metal complexes, including Ni(II), Co(II), Pd(II), and Pt(IV) complexes, was conducted. Various analytical techniques were employed to characterize the compounds using FTIR, NMR, UV-Vis spectroscopy, mass spectrometry, and molar conductivity. Biological activities, including antibacterial and cytotoxicity studies, were evaluated. Results: The synthesized compounds demonstrated stability and structural characteristics consistent with the intended coordination geometries. IR spectra confirmed the coordination of metal ions with the ligands. The complexes were evaluated for the antimicrobial activity against two types strains of Gram-negative Escherichia coli and Gram-positive bacteria Staphylococcus aureus and showed good significant against these bacteria. The Pd(II) complex demonstrated higher efficacy against cancer cells compared to normal cells, highlighting its potential as an anticancer agent. The cytotoxicity of the Pd (II) complex on human malignant melanoma A375 and Normal cell WRL-68 were IC50 23.83 and IC50 153.7, respectively. Molecular docking studies provide insights into the interaction of the complexes with target proteins, offering potential modes of action. Conclusion: The study successfully synthesized and characterized bis azo-Schiff base ligands and their metal complexes, demonstrating their stability and promising biological activities.

Antihypertensive Medications Can Prevent Fostamatinib-Induced Blood Pressure Elevation

Fostamatinib is a tyrosine kinase inhibitor that has been shown in clinical trials to be effective against spleen tyrosine kinase in patients suffering from rheumatoid arthritis. Fostamatinib medication was linked in clinical trials to a slight increase in systemic arterial Blood Pressure (BP). This observation is consistent with other kinase inhibitors, particularly those that obstruct VEGFR2 signaling. In conscious rats, we examined the relationship between the elevation of blood pressure caused by fostamatinib and the plasma levels of the fostamatinib-active metabolite R940406. We discovered that there was a strong correlation between changes in R940406 plasma concentration and the time course of the blood pressure effect, suggesting a direct pharmacological relationship. The experiments yielded free plasma levels of R940406 up to 346 nmol/L, which is greater than the mean peak free plasma concentration of 49 nmol/L that has been recorded in clinical settings. We beyond the clinically noted mean peak free plasma concentration of 49 nmol/L, up to 346 nmol/L. We’ve shown that there are several effective ways to reduce the blood pressure elevation caused by fostamatinib dosing, including simple drug withdrawal or condoning with a variety of common antihypertensive medications like atenolol, captopril, and nifedipine. These results provide credence to prospective strategies for preserving patient safety during fostamatinib therapy. Additionally, we have shown—using nifedipine as an example drug—that this blood pressure control was not brought about by a decrease in R940406’s plasma exposure, indicating that potential pharmacological benefits of the investigational drug may be preserved while blood pressure control is managed with the use of conventional medications.

Subacute Toxicity of Microgranulated Myrmecodia platytyrea Aqueous Tuber Extract (gMPAE)

Introduction: Myrmecodia platytyrea, locally known as ‘Sarang Semut’, is an epiphytic plant native to Asia and the Asia Pacific. The tubers were traditionally used to manage cancer, hyperuricemia, and coronary heart diseases. Scientifically, the aqueous tuber extract has potential pharmacological benefits, including anti-cancer, anti-diabetic, and anti-inflammatory properties. Since the extract had no acute or subacute toxic effects, it might be used as a supplement to reduce inflammation and improve physiological functioning with better bioavailability than conventional preparations. This study aims to investigate the subacute toxicity of the microgranulated aqueous extract of M. platytyrea tuber (gMPAE). Methods: The formulation of the microgranules was established and analysed using a scanning electron microscope (SEM). The subacute oral toxicity study was carried out. The female nulliparous and non-pregnant ICR mice were divided into three groups (n=5), a group treated with normal saline (control group), a group treated with a placebo (blank microgranules), and a group treated with gMPAE, orally once daily for 28 days. Results: The gMPAE was produced using a spray-dry method and displayed microparticles with irregular shapes typical for spray-dried formulations. The sub-acute toxicity study showed no physical or behavioural changes in both placebo or gMPAE-treated mice compared to the control mice, with no mortality observed after 28 days of treatment and no signs of delayed occurrence of toxic effects 14 days post-treatment. Conclusion: Standardised spray-dried microgranules of M. platytyrea tuber aqueous extract were successfully developed to enhance the extract’s efficacy and are safe to be used as health supplements.

The Inhibition Activities of the Fruit Extract of Plinia cauliflora against Melanoma Cells and the Single-Stranded DNA-Binding Protein (SSB) from Klebsiella pneumoniae

Plinia cauliflora has been associated with numerous ethnobotanical applications. In this study, we uncovered that the fruit extract of P. cauliflora, obtained using 50% ethanol, possesses inhibition activity against the Klebsiella pneumoniae single-stranded DNA-binding protein (KpSSB). SSB plays a critical role in cell survival, making it an attractive target for the development of anti-infective drugs. The inhibition activity against KpSSB by the P. cauliflora extract demonstrated an IC50 value of 73 ± 8 μg/mL. By using gas chromatography–mass spectrometry, the chemical content of this extract was tentatively determined. The top 15 compounds (>0.7%) were as follows: 5-hydroxymethylfurfural, 2,3-dihydro-3,5-dihydroxy-6-methyl-4h-pyran-4-one, 2,5-diformylfuran, furfural, ace-tic acid, citraconic anhydride, formic acid, ethyl 4-hydroxy-3-methylbut-2-enoate, furfuryl alcohol, furyl hydroxymethyl ketone, 3-acetyl-3-hydroxyoxolane-2-one, 2,3-dihydro-5-hydroxy-2-(hydroxymethyl)-4H-pyran-4-one, 2(3H)-furanone, dihy-dro-4-hydroxy-, hydroxyacetone, and 1-hydroxybut-3-en-2-one. To analyze the possible binding modes, the three most abundant compounds were then subjected to docking analysis. We also investigated whether the P. cauliflora extract exhibited any cytotoxic and antiproliferative effects on the survival of B16F10 melanoma cells. Additionally, we found that the extract of P. cauliflora could inhibit the migration and induce apoptosis of B16F10 cells. The results of this study collectively suggest that P. cauliflora holds potential pharmacological benefits, warranting further exploration for therapeutic applications.

Licochalcone a improves cardiac functions after ischemia-reperfusion via reduction of ferroptosis in rats

Myocardial ischemia-reperfusion (I/R) injury triggers several cell death types, including apoptosis, autophagy, and ferroptosis. Licochalcone A (LCA), a natural flavonoid compound isolated from the root of Glycyrrhiza glabra, has been demonstrated to exert potential pharmacological benefits, such as antioxidant, antitumor, and anti-inflammatory activities. The present study aimed to investigate the involvement of ferroptosis in the pathogenesis of I/R and determine whether LCA can inhibit ferroptosis to prevent the myocardial I/R injury in rats. The effects of LCA on myocardial I/R injury were detected by examining the left ventricular-developed pressure and triphenyltetrazolium chloride staining. We conducted Western blotting analyses, ELISA assay, and quantitative real-time PCR to determine the levels of ferroptosis-related molecules. To demonstrate the cardioprotective effect of LCA in vitro, H9c2 and primary neonatal rat cardiomyocytes were co-treated with ferroptosis inducers (erastin, RSL3, or Fe-SP) and LCA for 16 and 24 h. Our ex vivo study showed that LCA increased the cardiac contractility, and reduced the infarct volume and ferroptosis-related biomarkers in rat hearts after I/R. Moreover, LCA reduced the levels of ferroptosis inducers-induced reactive oxygen species generation, lipid peroxidation, and ferroptosis-related biomarkers in cultured H9c2 cells and cardiomyocytes. LCA also reduced the Fe-SP-increased nuclear factor erythroid 2-related factor 2 and heme oxygenase-1 protein levels in cultured cardiomyocytes. In the present study, we showed that the LCA-induced cardioprotective effects in attenuating the myocardial I/R injury were correlated with ferroptosis regulation, and provided a possible new therapeutic strategy for prevention or therapy of the myocardial I/R injury.

The Role of Nrf2 in Relieving Cerebral Ischemia-Reperfusion Injury.

Ischemic stroke includes two related pathological damage processes: brain injury caused by primary ischemia and secondary ischemia reperfusion (I/R) injury. I/R injury has become a worldwide health problem. Unfortunately, there is still a lack of satisfactory drugs for ameliorating cerebral I/R damage. Nrf2 is a vital endogenous antioxidant protein, which combines with Keap1 to maintain a dormant state under physiological conditions. When pathological changes such as I/R occurs, Nrf2 dissociates from Keap1 and activates the expression of downstream antioxidant proteins to exert a protective effect. Recent research have shown that the activated Nrf2 not only effectively inhibits oxidative stress, but also performs the ability to repair the function of compromised mitochondria, alleviate endoplasmic reticulum stress, eliminate inflammatory response, reduce blood-brain barrier permeability, inhibit neuronal apoptosis, enhance the neural network remolding, thereby exerting significant protective effects in alleviating the injuries caused by cell oxygen-glucose deprivation, or animal cerebral I/R. However, no definite clinical application report demonstrated the efficacy of Nrf2 activators in the treatment of cerebral I/R. Therefore, further efforts are needed to elaborate the role of Nrf2 activators in the treatment of cerebral I/R. Here, we reviewed the possible mechanisms underlying its potential pharmacological benefits in alleviating cerebral I/R injury, so as to provide a theoretical basis for studying its mechanism and developing Nrf2 activators.

Oxidative Stability of Nano-Encapsulated Candlenut Oil

Candlenut has a lot of potential pharmacological benefits including in hair care, in treating skin problems such as psoriasis, and in its use as an emollient. However, the high unsaturated fatty acid content of candlenut oil causes it to be easily degraded by oxidation due to exposure to air, light, and humidity. Nanoencapsulations were found to be an alternative in protecting the materials from degradation. The purpose of this study was to investigate the effect of polymer-based nanoencapsulations on the oxidative stability of candlenut oil. Polyvinyl alcohol (PVA) was used as a polymer wall material. A lower peroxide value indicates better oil stability against oxidation. Results showed that nano-encapsulated candlenut oil has a significantly lower average peroxide value of 0.41 meq/100g over 35 days storage time, compared to 3.8 meq/100g in pure candlenut oil. Furthermore, based on its physical characterization, it was found that the reduction of particle size with the optimal size of 172±12 nm was achieved by increasing the amount of PVA. A well-chosen and well-calculated amount of polymer material, therefore, plays an important role to obtain optimal nano-encapsulated candlenut oil.
 Keywords: nanoencapsulation, candlenut oil, oxidative stability, polymeric materials

Sea urchins: an update on their pharmacological properties.

Sea urchins are a group of benthic invertebrates characterized by having rigid globose bodies, covered in spines, and have an innate immune system that has allowed them to survive in the environment and defend against many pathogens that affect them. They are consumed for their unique flavor, but also for possessing a rich source of bioactive compounds which make them a source for a wide array of medicinal properties. Thus, these may be used to discover and develop new drugs such as anti-bacterials, anti-carcinogenics and anti-virals. Precisely for those reasons, this revision is centered on the known biological activities in various sea urchin species. Recently, the potential pharmacological benefits of nine sea urchin species [Diadema antillarum (Philippi 1845), Echinometra mathaei (de Blainville), Evechinus chloroticus (Valenciennes), Mesocentrotus nudus (Agassiz, 1863), Paracentrotus lividus (Lamarck, 1816), Scaphechinus mirabilis (Agazzis, 1863), Stomopneustes variolaris (Lamarck, 1816), Tripneustes depressus (Agassiz, 1863), and Tripneustes ventricosus (Lamarck, 1816)] have been evaluated. Our work includes a comprehensive review of the anti-fungal, anti-parasitic, anti-inflammatory, hepatoprotective, anti-viral, anti-diabetic, anti-lipidemic, gastro-protective and anti-cardiotoxic effects. Furthermore, we revised the compounds responsible of these pharmacological effects. This work was intended for a broad readership in the fields of pharmacology, drugs and devices, marine biology and aquaculture, fisheries and fish science. Our results suggest that organic extracts, as well as pure compounds obtained from several parts of sea urchin bodies are effective in vitro and in vivo pharmacological models. As such, these properties manifest the potential use of sea urchins to develop emergent active ingredients.

β-Caryophyllene suppresses ferroptosis induced by cerebral ischemia reperfusion via activation of the NRF2/HO-1 signaling pathway in MCAO/R rats

BackgroundIschemic stroke is a complex brain disease regulated by several cell death processes, including apoptosis, autophagy, and ferroptosis. β-Caryophyllene (BCP), a natural bicyclic sesquiterpene abundantly found in essential oils, has been demonstrated to have potential pharmacological benefits in many diseases, including ischemic stroke. PurposeThis research was to determine the existence of ferroptosis in the pathogenesis of acute ischemic stroke and investigate whether BCP can inhibit ferroptosis to improve cerebral ischemia injury by activating the NRF2/HO-1 signaling pathway in rats. MethodsFirst, we verified ferroptosis by assessing proferroptotic changes after middle cerebral artery occlusion reperfusion (MCAO/R), along with protein and lipid peroxidation levels. Then male rats were divided randomly into Sham, MCAO/R, ML385 (NRF2-specific inhibitor) and BCP groups. The effects of BCP on cerebral injury were detected by the modified neurological severity score, TTC staining, and hematoxylin-eosin staining. We conducted western blotting analyzes of proteins, including those involved in ferroptosis and related signaling pathways. To demonstrate the neuroprotective effect of BCP in vitro, primary astrocytes were pretreated with different concentrations of BCP (10, 20, and 40 μM) for 24 h before oxygen-glucose deprivation/re-oxygenation (ODG/R). ResultsWe concluded that ferroptosis was engaged in the process of I/R-induced neurological damage, implying that this novel type of cell death might provide new therapeutic options for the clinical treatment of ischemic stroke. In vivo study proved that BCP improved neurological scores, infarct volume, and pathological features after MCAO/R. We demonstrated that BCP evidently enhanced NRF2 nuclear translocation, activated the NRF2/HO-1 pathway, which protected against ferroptosis. In vitro investigation revealed the same results. BCP decreased OGD/R-induced ROS generation and iron accumulation. Furthermore, the neuroprotective effects of BCP were reversed by the NRF2 inhibitor ML385. ConclusionOur results indicated the critical role of ferroptosis in cerebral I/R injury. For the first time, we showed that the significant neuroprotective effects of BCP in attenuating ischemic stroke injury are correlated with ferroptosis regulation, and its mechanism is associated with activation of the NRF2/HO-1 axis.

Alpha-Mangostin and Gamma-Mangostin Isolated from Mangosteen (Garcinia mangostana L.) as Promising Candidates against SARS-CoV-2: A Bioinformatics Approach

The world is endangered by the COVID‐19 pandemic caused by SARS‐CoV‐2, people are dying in thousands every day, and without an actual treatment, it seems that bringing this global health problem to a quit is impossible. Natural products have been in constant use since ancient times and are proven by time to be effective. Medicinal plants from Indonesia may lead to the discovery of the novel drugs. Mangosteen or Garcinia mangostana L. is a native tropical fruit from Southeast Asia and is known to contain bioactive compounds. Interestingly, the main xanthone derivatives are alpha-mangostin and gamma-mangostin, these compounds have a variety of pharmacological activities such as antiviral activity. In summary, this study showed potential pharmacological benefits of alpha-mangostin and gamma-mangostin isolated from mangosteen against SARS-CoV-2. Thus, mangosteen exhibits as a valuable plant and a candidate for future drug development to fight SARS-CoV-2. However, further trials, such as in vitro and in vivo evaluation, are needed to prove the validity of these findings

Alpha-Mangostin and Gamma-Mangostin Isolated from Mangosteen (Garcinia mangostana L.) as Promising Candidates against SARS-CoV-2: A Bioinformatics Approach

The world is endangered by the COVID‐19 pandemic caused by SARS‐CoV‐2, people are dying in thousands every day, and without an actual treatment, it seems that bringing this global health problem to a quit is impossible. Natural products have been in constant use since ancient times and are proven by time to be effective. Medicinal plants from Indonesia may lead to the discovery of the novel drugs. Mangosteen or Garcinia mangostana L. is a native tropical fruit from Southeast Asia and is known to contain bioactive compounds. Interestingly, the main xanthone derivatives are alpha-mangostin and gamma-mangostin, these compounds have a variety of pharmacological activities such as antiviral activity. In summary, this study showed potential pharmacological benefits of alpha-mangostin and gamma-mangostin isolated from mangosteen against SARS-CoV-2. Thus, mangosteen exhibits as a valuable plant and a candidate for future drug development to fight SARS-CoV-2. However, further trials, such as in vitro and in vivo evaluation, are needed to prove the validity of these findings.

N‐(Biphenyl‐3‐ylmethyl)ethanamines as G protein‐biased agonists of 5‐HT7R

AbstractThere has been much attention to biased ligands of G protein‐coupled receptors (GPCRs) for potential pharmacological benefits. Recently, we reported N‐((6‐chloro‐2'‐methoxy‐[1,1'‐biphenyl]‐3‐yl)methyl)ethanamine 1 as G protein‐biased agonist of 5‐HT7R, which could be used as a chemical probe for the study on treatment discovery of autism spectrum disorder. Herein, we describe the synthesis of derivatives of the compound 1 and their biological evaluations in both G protein and β‐arrestin signaling pathway. Total 16 compounds were synthesized and evaluated, and the compounds 3c, 3f, 3i, and 3p could be called as G protein‐biased agonists like the compound 1. Among the four compounds, the compound 3c was the best in efficacy with an Emax value of 73% and the compound 3f was the most potent agonist with an EC50 value of 0.094 μM.

Ethanol-Induced Hepatotoxicity and Alcohol Metabolism Regulation by GABA-Enriched Fermented Smilax china Root Extract in Rats.

Chronic alcohol consumption can cause hepatic injury and alcohol-induced toxicities. Extracts from Smilax china root have been widely used in traditional medicine and for their potential pharmacological benefits. We aimed to determine if fermented Smilax china extract (FSC) regulates alcoholic fatty liver and liver injury using two in vivo experiments. Sprague-Dawley rats were administered ethanol (3 g/kg b.w.; po) with or without FSC pretreatment to induce an acute hangover. In another experiment, rats were fed either a normal or Lieber-DeCarli ethanol (6.7%) diet with or without FSC pretreatment (125, 250, and 500 mg/kg b.w.; po) for 28 days. Serum biomarkers, liver histopathology, and the mRNA levels of anti-inflammatory, antioxidant, lipogenic, and lipolytic genes were analyzed. FSC pretreatment significantly reduced blood alcohol and acetaldehyde concentrations, upregulated the mRNA expression of alcohol dehydrogenase, aldehyde dehydrogenase, and superoxide dismutase, and decreased the activities of liver enzymes in a dose-dependent manner. It also downregulated SERBP-1c and upregulated PPAR-α and reduced the gene expression of the anti-inflammatory cytokine IL-6 in the liver. The final extract after fermentation had increased GABA content. Furthermore, FSC was found to be safe with no acute oral toxicity in female rats. Thus, FSC increases alcohol metabolism and exhibits antioxidant and anti-inflammatory effects to induce hepatoprotection against alcohol-induced damage. It may be used as a functional food ingredient after excess alcohol consumption.

Effects of loline-alkaloid-containing seeds or seed extract on in vitro gas production and apparent dry matter digestibility

Loline alkaloids produced by Epichloë endophytes in pastoral grass species have suggested potential antimicrobial and anthelmintic properties. Loline is considered nontoxic, but the known effects of loline and derivatives on ruminal fermentation are limited. Negative effects could outweigh potential pharmacological benefits in vivo. Therefore, loline’s effect on ruminal fermentation was assessed using an in vitro gas production technique. Two experiments with 24-h in vitro gas production were conducted using an ANKOM gas production system. In Exp. 1, treatments were Festuca pratensis seeds either with loline (LS, 330 µg/mL) or without loline (NLS) as the sole substrate. In Exp. 2, treatments were Lolium perenne (perennial ryegrass) only (RGS), ryegrass with loline-containing seed extract (RGL, 330 µg/mL), or ryegrass with non-loline-containing seed extract (RGN). Cumulative gas production was measured over 24 h, and apparent DM digestibility and pH were collected at the end. Data were analyzed using a linear mixed effect regression in Exp. 1, and in Exp. 2 data were fitted to Ørskov’s nonlinear model to determine rate and extent of gas production. At 24 h, NLS had a 9% greater ( P < 0.01) gas yield than LS with similar apparent DM digestibility. Potential gas production was similar among ryegrass treatments. However, the fractional rate (%/h) was greatest ( P < 0.05) for RGN at 0.112 ± 0.02 and lowest for RGS at 0.093 ± 0.02, with RGL (0.109 ± 0.02) being intermediate and different than RGN and RGS. Apparent DM digestibility (73.2 ± 0.07, 63.3 ± 0.06, and 60.7 ± 0.06%) was greater ( P < 0.05) for RGS compared with RGL and RGN. Loline had little antimicrobial effect on ruminal microbes and fermentation, but the fermentation kinetics were altered. Loline needs further study as a potential pharmaceutical to be used on gut-dwelling organisms without negatively affecting rumen fermentation.

Melatonin and Phytomelatonin: Chemistry, Biosynthesis, Metabolism, Distribution and Bioactivity in Plants and Animals-An Overview.

Melatonin is a ubiquitous indolamine, largely investigated for its key role in the regulation of several physiological processes in both animals and plants. In the last century, it was reported that this molecule may be produced in high concentrations by several species belonging to the plant kingdom and stored in specialized tissues. In this review, the main information related to the chemistry of melatonin and its metabolism has been summarized. Furthermore, the biosynthetic pathway characteristics of animal and plant cells have been compared, and the main differences between the two systems highlighted. Additionally, in order to investigate the distribution of this indolamine in the plant kingdom, distribution cluster analysis was performed using a database composed by 47 previously published articles reporting the content of melatonin in different plant families, species and tissues. Finally, the potential pharmacological and biostimulant benefits derived from the administration of exogenous melatonin on animals or plants via the intake of dietary supplements or the application of biostimulant formulation have been largely discussed.

Phytosomes: A Promising Strategy for Enhanced Therapeutic Beneϐits of Phytochemicals

Phytosomes are phytochemical based novel drug delivery systems that lead to better absorption, greater bioavailability in addition to improved therapeutic efficacy of numerous phytoconstituents. It is a supremely advanced form of herbal formulations which contains the active phytoconstituent of herbal extract bound by phospholipid molecule. Additionally, these also act as vesicular systems for various fascinating and significant phytoactive. The phytosomes technique produces remarkable minute spheres or tiny cells, which is helpful in the protection of active phytochemical constituent from destruction by the gastric environment. Furthermore, phytosomes also reveal efficient pharmacokinetic as well as pharmacodynamic profile compared to conventional herbal extracts. The current manuscript is a cogent attempt to review the potential pharmacological benefits of herbal extracts by forming an impressive and successful phytophospholipid complex. Salient attributes, as well as promising and imperative applications of phytosomes, are illustrated in the manuscript. Recent advances in research endeavours, along with major inferences on effective phytosomal drug delivery systems, have also been highlighted.

Standardization Using Analytical Techniques (UV, NMR, FTIR, HPLC, Mass) and Pharmacognostic Evaluation of the Roots of Selinum vaginatum: A Rare Himalayan Plant of the Rohtang Region

Introduction: Selinum vaginatum is an endemic Indian plant present on high altitude and is known as “Bhootkeshi,” by the locals. The root of plant Selinum vaginatum commonly known as “Bhootkeshi” from the family Umbellifercae is an aromatic herbal drug. Selinum vaginatum has been used traditionally for curing seizures, epilepsy, mental illness, and hysteria. This plant has shown therapeutic effects as used by the locals. There is no data available regarding standardization of the roots of Selinum vaginatum. It is a novel work as the plant is rarely found and shows medicinal values but no quality control work has been performed. Objective: The aim of this paper is to study quality control and carry out physicochemical analysis and standardization of the roots of Selinum vaginatum for determining its quality and purity. As no work has been performed on the roots of this plant, so standardization will help in keeping a record of the parameters exhibited during the evaluation of the roots of Selinum vaginatum. Methods: The organoleptic characteristics were studied and physicochemical tests, phytochemical analysis, fluorescence analysis, TLC, UV, FTIR, NMR, and Electrospray Ionisation - Mass spectroscopy, HPLC and other parameters were carried out for the standardization of the test drug. The procedures were carried out as per the WHO standards. The total ash values, swelling index, foaming index, moisture content, alcohol, and water-soluble extractive values were calculated. The TLC profile of Selinum vaginatum was observed and the UV, FTIR, HPLC, NMR and Mass spectroscopies of the plant were also performed. Results: The microscopic results showed the presence of schizogenous canals in abundance, cork cells, oil and globules, while medullary rays and pith were absent and around 10-17 layers of cells were seen. The presence of active compounds like phenols, terpenoids, alkaloids, coumarins, essential oils, tannins, saponins, carbohydrates, and acids was reported by phytochemical tests, TLC, UV, NMR, HPLC, Mass, and FTIR spectroscopy methods. These compounds can be studied in detail for understanding the potential pharmacological benefits and decoding the traditional uses. The spectroscopic analysis and physicochemical tests have shown the presence of phenols, esters, organic halogens, carbohydrate, carboxylic acids, alcohols, ethers, and glycosides which must be responsible for the medicinal properties of the plant. Conclusion: This study has provided a set of information that will be useful for the identification of fresh batches of the roots of Selinum vaginatum and this can be used as a reference set of information for accessing the purity, quality and identification, and analysis of the authenticity of the plant roots. Spectroscopic techniques have shown peaks, which on interpretation have reported the presence of active compounds - (coumarins like selenidin, angelicin, vaginidine, furocoumarin - oroselol and coumarin derivative- lomatin, isovaleric acid, Valeranone, Tricyclene, p-Cymene, α-Pinene, β-Pinene, Camphene, Borneol, p- Camphene, cholorgenic acid, β-Myrcene, Limonene and α-Pineneoxide which can be studied for understanding and identifying the pharmacological actions of the rhizomatous roots of S. vaginatum. All the information collected by research on the roots of S. vaginatum will help in the identification of crude drugs and also in the development of a standard for the drug Selinum vaginatum.