ABSTRACT
Diabetes mellitus (DM) is a chronic metabolic disorder characterized by persistent hyperglycemia. It involves disturbances in carbohydrate, fat, and protein metabolism due to defects in insulin secretion, insulin action, or both. Novel therapeutic approaches are continuously being explored to enhance metabolic control and prevent complications associated with the disease. This study investigates the therapeutic potential of kaempherol-3-rhamnoside, a flavonoid, in managing diabetes by modulating the AMP-activated protein kinase (AMPK) pathway and improving metabolic enzyme activities in streptozotocin (STZ) -induced diabetic mice. Diabetic mice were treated with varying doses of kaempherol-3-rhamnoside and/or insulin over a 28-day period. Glycolytic and gluconeogenesis enzyme activities in the liver, fasting blood glucose levels, serum insulin levels, lipid profiles and oxidative stress markers were assessed. Treatment with kaempherol-3-rhamnoside significantly improved glycolytic enzyme activities, reduced fasting blood glucose, and enhanced insulin levels compared to diabetic controls. The compound also normalized lipid profiles and reduced oxidative stress in the liver, suggesting its potential in reversing diabetic dyslipidemia and oxidative damage. Furthermore, kaempherol-3-rhamnoside activated the AMPK pathway, indicating a mechanism through which it could exert its effects. Kaempherol-3-rhamnoside exhibits promising antidiabetic properties, potentially through AMPK pathway activation and metabolic enzyme modulation. These findings support its potential use as an adjunct therapy for diabetes management. Further clinical studies are warranted to validate these results in human subjects.
Subject(s)
AMP-Activated Protein Kinases , Diabetes Mellitus, Experimental , Liver , Animals , Diabetes Mellitus, Experimental/drug therapy , Diabetes Mellitus, Experimental/metabolism , Mice , Liver/drug effects , Liver/metabolism , AMP-Activated Protein Kinases/metabolism , Male , Blood Glucose/metabolism , Blood Glucose/drug effects , Oxidative Stress/drug effects , Insulin/metabolism , Insulin/blood , Streptozocin , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/therapeutic useABSTRACT
The lost dopaminergic neurons in the brain prevent mobility in Parkinson's disease (PD). It is impossible to stop the disease's progress by means of symptoms management. Research focuses on oxidative stress, mitochondrial dysfunction, and neuronal degeneration. Exploration of potential neuroprotective drugs against prosurvival B-cell lymphoma 2 (Bcl-2) protein is ongoing. An investigable cause behind PD, as well as preventive measures, could be discovered considering the association between such behavioural manifestations (cataleptic behaviours) and PD. The compound Afzelin, known to guard the nervous system, was chosen for this study. The study was done on rats divided into six different groups. First, there was a control group. The other group was treated with Reserpine (RES) (1 mg/kg). The third group received RES (1 mg/kg) and levodopa (30 mg/kg). The remaining three groups were given RES (1 mg/kg) in conjunction with Afzelin at the following doses: 5 mg/kg, 10 mg/kg, and 20 mg/kg. Cataleptic behavior and mobility in rats was assessed using the rotarod, open field, and modified forced-swim tests. thiobarbituric acid reactive substances (TBARS), nitric oxide (NO), biogenic amines, and Bcl-2 level in rat tissue homogenates were considered. According to the study's findings, the rats treated through co-administration of RES and Afzelin improved significantly in their cataleptic behaviours and locomotor activity. In addition, administering Afzelin itself caused Bcl-2 expression, which could have some neuroprotection properties. This study provides meaningful information on the effectiveness of Afzelin in handling catalepsy and other degenerative neurologic disorders. As a result, other studies need to be conducted to establish the reasons behind the reactions and determine the long-term effects of Afzelin on these conditions.
ABSTRACT
Myocardial infarction (MI) continues to be an important issue in healthcare systems worldwide, leading to high rates of morbidity and mortality. Despite ongoing efforts towards the development of preventive measures and treatments, addressing the challenges posed by MI remains difficult both in developed and developing countries. However, researchers recently investigated the potential cardioprotective effects of taraxerol utilizing an isoproterenol (ISO)-induced cardiotoxicity model among Sprague Dawley rats. Specifically, subcutaneous tissue injections consisting of 5.25 mg/kg or 8.5 mg/kg ISO were administered over two consecutive days as stimuli to induce cardiac injury. To investigate the possibility of preventing damage caused by ISO-induced cardiotoxicity by taraxerol treatment, five groups were formed: a normal control group (1% Tween 80), an ISO control group, an amlodipine group administered 5 mg/kg/day, and various doses of taraxerol. The study results showed that treatment significantly reduced cardiac marker enzymes. Additionally, pretreatment with taraxerol increased myocardial activity in SOD and GPx, leading to significant reductions in serum CK-MB levels along with MDA, TNF-α, and IL-6. Further histopathological analysis supported these observations, as treated animals had less cellular infiltration compared to untreated ones. These multifaceted findings suggest that oral administration of taraxerol could potentially protect hearts from ISO-caused damage by increasing endogenous antioxidant concentrations while decreasing pro-inflammatory cytokines.
Subject(s)
Cardiotoxicity , Myocardial Infarction , Rats , Animals , Isoproterenol/toxicity , Isoproterenol/metabolism , Cardiotoxicity/drug therapy , Cardiotoxicity/etiology , Cardiotoxicity/metabolism , Inflammation Mediators/metabolism , Rats, Sprague-Dawley , Myocardium/metabolism , Myocardial Infarction/drug therapy , Antioxidants/metabolism , Disease Models, Animal , Oxidative StressABSTRACT
Diabetic polyneuropathy is characterized by structural abnormalities, oxidative stress, and neuroinflammation. The current study aimed to determine the antinociceptive effects of isoeugenol and eugenol and their combinations in neuropathic pain resulting from streptozotocin (STZ)-induced diabetes and neuroinflammation. Female SD rats were categorized into normal control, diabetic control, and treatment groups. On the 28th day and 45th day, behavioral studies (allodynia and hyperalgesia) were performed to analyze the development and protection of diabetic polyneuropathy. The levels of inflammatory and oxidative mediators, such as superoxide dismutase (SOD), tumor necrosis factor-α (TNF-α), catalase, reduced glutathione, and thiobarbituric acid reactive substances (TBARS), were estimated. In addition, the level of nerve growth factor (NGF) was estimated at the end of the study in different groups. The anti-NGF treatment decreased its upregulation in the dorsal root ganglion significantly. The results showed that isoeugenol, eugenol, and their combination have therapeutic potential against neuronal and oxidative damage induced by diabetes. In particular, both compounds significantly affected behavioral function in treated rats and showed neuroprotection against diabetic neuropathy, and their combination had synergistic effects.
ABSTRACT
Mangiferin is a herbal drug that has proven anticancer potential. Owing to its lower aqueous solubility and poor oral bioavailability, the full pharmacological potential of this bioactive drug has not fully been explored. In the present study, phospholipid-based microemulsion systems were developed to bypass oral delivery. The globule size of the developed nanocarriers was less than 150 nm and the drug entrapment was >75% with a drug loading ~25%. The developed system offered a controlled release pattern following the Fickian drug release. This enhanced mangiferin's in vitro anticancer activity by four-fold, the cellular uptake was observed to be improved by three-fold on the MCF-7 cells. Ex vivo dermatokinetic studies showed substantial topical bioavailability with a prolonged residence time. The findings provide a simple technique to administer mangiferin via a topical route promising a safer, topically bioavailable and effective treatment option for breast cancer. Such scalable carriers with immense topical delivery potential may provide a better option for present-day topical products of a conventional nature.
ABSTRACT
The study was conducted to determine whether corosolic acid could protect the myocardium of diabetic rats from damage caused by isoproterenol (ISO) and, if so, how peroxisome proliferator-activated receptor gamma (PPAR-γ) activation might contribute into this protection. Diabetes in the rats was induced by streptozotocin (STZ), and it was divided into four groups: the diabetic control group, diabetic rats treated with corosolic acid, diabetic rats treated with GW9662, and diabetic rats treated with corosolic acid plus GW9662. The study was carried out for 28 days. The diabetic control and ISO control groups showed a decrease in mean arterial pressure (MAP) and diastolic arterial pressure (DAP) and an increase in systolic arterial pressure (SAP). The rat myocardium was activated by corosolic acid treatment, which elevated PPAR-γ expression. A histopathological analysis showed a significant reduction in myocardial damage by reducing myonecrosis and edema. It was found that myocardial levels of CK-MB and LDH levels were significantly increased after treatment with corosolic acid. By decreasing lipid peroxidation and increasing endogenous antioxidant levels, corosolic acid therapy showed a significant improvement over the ISO diabetic group. In conclusion, our results prove that corosolic acid can ameliorate ISO-induced acute myocardial injury in rats. Based on these results, corosolic acid seems to be a viable new target for the treatment of cardiovascular diseases and other diseases of a similar nature.
Subject(s)
Diabetes Mellitus, Experimental , PPAR gamma , Rats , Animals , PPAR gamma/metabolism , Rats, Wistar , Diabetes Mellitus, Experimental/metabolism , Myocardium/metabolism , Isoproterenol/metabolismABSTRACT
BACKGROUND: Numerous studies have shown that various products of Citrus sinensis, for example, crude extracts, essential oil, and purified components, possess anti-acne properties. However, the development of chlorogenic acid-functionalized silver nanoparticles of C. sinensis in gel matrix aiding QbD design has not been evaluated for acne treatment. AIM: In this study, we have developed chlorogenic acid-functionalized silver nanoparticles of C. sinensis in a gel matrix employing a QbD approach for acne treatment. MATERIAL AND METHOD: Citrus sinensis extract-loaded silver nanoparticles were functionalized with chlorogenic acid, which acted as a bio-reducing agent and further improved anti-acne properties. The developed formulation was optimized via Box-Behnken Design. The formulation morphology was evaluated by transmission electron microscopy (TEM). The release profile of C. sinensis extract formulation was assessed by an in vitro release study and confocal laser scanning microscopy (CLSM). Moreover, the characterization study of the gel was performed that included an evaluation of the extrudability and spreadability of the developed gel. Furthermore, the anti-oxidant efficacy of AgN-CA formulation was validated using the DPPH test. RESULTS: The results showed a particle size of 71.78 nm, a polydispersity index of 0.297, a zeta potential of -36.12 mV, and an entrapment efficiency of 79.42% ± 6.79%. The results also indicated a uniform particle size. The release profile of C. sinensis extract revealed that 73.95% of the drug was released, whereas CLSM pictures of mice skin evidently demonstrated that the rhodamine B-treated AgN-CA gel penetrated much more extensively in comparison to the control. Furthermore, the anti-oxidant efficacy of AgN-CA formulation was validated using the DPPH test. Moreover, the characterization study of the developed gel, including its extrudability and spreadability, was found to be 16.02 ± 3.21 g and 30.73 ± 5.94 g cm/s, respectively. Also, texture analysis findings revealed that AgN-CA gel had firmness, consistency, cohesiveness, and viscosity index of 159.69 g, 634.95 g s, -116.33 g, and -501.80 g s, respectively, indicating that the AgN-CA gel was stable. CONCLUSION: The current study showed that AgN-CA is an effective drug carrier system for the topical administration of C. sinensis extract for the treatment of acne.
Subject(s)
Acne Vulgaris , Citrus sinensis , Metal Nanoparticles , Nanoparticles , Mice , Animals , Chlorogenic Acid/therapeutic use , Silver , Metal Nanoparticles/chemistry , Antioxidants/therapeutic use , Microwaves , Acne Vulgaris/drug therapy , Particle Size , Nanoparticles/chemistryABSTRACT
Opophytum forsskalii (O. forsskalii) is a desert plant that belongs to the Aizoaceae family. Although it is a natural food source for Bedouin tribes in northern Saudi Arabia, there is little information on its active metabolites. Therefore, the secondary metabolites of the hydroalcoholic extract from the leaves of this species were analyzed by liquid chromatography-mass chromatography (LC-MS). LC-MS identified a total of 30 secondary metabolites. These compounds represented two main categories among sixteen classes. Among them, flavonoids represented the largest proportion with eleven metabolites while fatty acids provided seven compounds. In addition, the extract was evaluated for its gastroprotective effect against gastric lesions induced by different models, such as indomethacin, stress, and necrotizing agents (80% ethanol, 0.2 mol/L NaOH, and 25% NaCl), in rats. For each method, group 1 was used as the control group while groups 2 and 3 received the leaf extract at doses of 200 and 400 mg/kg, respectively. The ulcer index (UI) and intraluminal bleeding score (IBS) were measured for each method. In addition, gastric tissue from the ethanol method was used for the analysis of nonprotein sulfhydrates (NP-SH), malondialdehyde (MDA), total protein (TP), and histopathologic evaluation. Pretreatment with O. forsskalii significantly decreased UI (p < 0.01) and IBS (p < 0.01) at 400 mg/kg. Pretreatment with O. forsskalii significantly improved total protein levels (p < 0.01) and NP-SH (p < 0.001) compared to the ethanol ulcer groups. MDA levels increased from 0.5 to 5.8 nmol/g in the normal groups compared to the ethanol groups and decreased to 2.34 nmol/g in the O. forsskalii pretreatment. In addition to the gastroprotective markers, histopathological examination of gastric tissue confirmed the gastroprotective potential of O. forsskalii extract against ethanol.
ABSTRACT
Antibiotics have completely transformed medical practice by enabling the treatment of infections that were formerly fatal. However, misuse of antibiotics encourages the formation and spread of germs that are resistant to therapy, hastening the emergence of bacterial resistance. This was a retrospective study that aimed to gather information about the variation in bacterial susceptibility of various patient age groups in a public hospital in Qassim, Saudi Arabia from January 2020 to December 2021. The study included reviewing bacterial susceptibility results that were collected from the laboratory department of the hospital. Four thousand seven hundred and sixty-two isolates were collected. The age of 46.41% of the patients was more than 63 years and the age of 28.96% of the patients was less than 48 years. The most prevalent bacteria were Staphylococcus aureus, Escherichia coli, and Klebsiella pneumoniae. The resistance of gram-positive and gram-negative bacteria to different antibiotics in the elderly group was generally higher than the resistance rates in younger patients. For example, in patients less than 48 years old, the resistance of Staphylococcus haemolyticus to clindamycin (53.3%), ampicillin (91.4%), ciprofloxacin (68.2%), erythromycin (86.1%), and penicillin (93.18%) was high. In patients aged more than 63 years, Staphylococcus haemolyticus was highly resistant to sulfamethoxazole (54.8%), clindamycin (63.9%), ampicillin (98.1%), ciprofloxacin (79.1%), erythromycin (93.2%), gentamicin (63.6%), and penicillin (98.7%). Before prescribing the antibiotics, it is important to assess the microbes that patients have and to be aware of the bacterial isolates' patterns of antibiotic susceptibility among patients of various age groups.
ABSTRACT
The herbal plant Petroselinum crispum (P. crispum) (Mill) is commonly available around the world. In this study, the leaves of the herbal plant P. crispum were collected from the central region of Al-Kharj, Saudi Arabia, to explore their in vitro pharmacological activity. Essential oil from the leaves of P. crispum was isolated using the hydrodistillation method. The composition of P. crispum essential oil (PCEO) was determined using Gas chromatography-mass spectrometry (GC-MS). A total of 67 components were identified, representing approximately 96.02% of the total volatile composition. Myristicin was identified as the principal constituent (41.45%). The in vitro biological activity was assessed to evaluate the antioxidant, antimicrobial, and anti-inflammatory potential of PCEO. PCEO showed the highest antimicrobial activity against Candida albicans and Staphylococcus aureus among all the evaluated microbial species. In vitro anti-inflammatory evaluation using albumin and trypsin assays showed the excellent anti-inflammatory potential of PCEO compared to the standard drugs. An in silico study of the primary PCEO compound was conducted using online tools such as PASS, Swiss ADME, and Molecular docking. In silico PASS prediction results supported our in vitro findings. Swiss ADME revealed the drug likeness and safety properties of the major metabolites present in PCEO. Molecular docking results were obtained by studying the interaction of Myristicin with an antifungal (PDB: 1IYL and 3LD6), antibacterial (PDB: 1AJ6 and 1JIJ), antioxidant (PDB: 3NM8 and 1HD2), and anti-inflammatory (3N8Y and 3LN1) receptors supported the in vitro results. Therefore, PCEO or Myristicin might be valuable for developing anti-inflammatory and antimicrobial drugs.
Subject(s)
Magnoliopsida/chemistry , Plant Leaves/chemistry , Anti-Infective Agents/analysis , Anti-Inflammatory Agents/pharmacology , Antifungal Agents/pharmacology , Computer Simulation , In Vitro Techniques , Plant Leaves/growth & development , Saudi ArabiaABSTRACT
Healthcare-associated infections are widely considered one of the most common unfavorable outcomes of healthcare delivery. Ventilator-associated pneumonia, central line-associated bloodstream infections, and catheter-associated urinary tract infections are examples of healthcare-associated infections. The current study was a retrospective study conducted at a public hospital in Unaizah, Saudi Arabia, to investigate the frequency of healthcare-associated illnesses and adherence to healthcare-associated infection prevention techniques in the year 2021. Surgical site infections occurred at a rate of 0.1%. The average number of catheter-associated urinary tract infections per 1000 catheter days was 0.76. The average number of central line-associated bloodstream infections per 1000 central line days was 2.6. The rate of ventilator-associated pneumonia was 1.1 per 1000 ventilator days on average. The average number of infections caused by multidrug-resistant organisms per 1000 patient days was 2.8. Compliance rates were 94%, 100%, 99%, and 76% for ventilator-associated pneumonia, central line-associated bloodstream infections, catheter-associated urinary tract infections, and hand hygiene bundles, respectively. It is critical to participate in more educational events and workshops, particularly those that emphasize hand cleanliness and personal safety equipment.
ABSTRACT
Abstract Some plants of the genus Pulicaria have been used in traditional medicines for treating back pain and inflammation. They possess various bioactivities such as antipyretic, analgesic, and hepatoprotective. This study aimed to investigate the potential analgesic, antipyretic, anti- inflammatory, and hepatoprotective activities of Pulicaria crispa (P. crispa) extract (PCE). Analgesic activity was evaluated using the hot plate and acetic acid-induced writhing tests. Antipyretic and anti-inflammatory activities were evaluated using rectal temperature and carrageenan-induced hind paw edema methods, respectively. CCl4-intoxication was used for hepatoprotective activity. Also, liver histopathology was assessed. PCE, at 500 mg/kg, exhibited significant analgesic, antipyretic, and anti-inflammatory effects. The increased serum levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), gamma-glutamyl transferase (GGT), and bilirubin of CCl4-exposed rats reflects their liver injury. PCE significantly decreased the elevated liver markers. The hepatoprotective effect of PCE was confirmed, as it successfully reversed the altered levels of total protein, malondialdehyde (MDA), and non-protein sulfhydryls (NP-SH) in the liver tissues of CCl4-exposed rats. Histopathological studies confirmed the hepatoprotective nature of PCE. Pretreatment of rats with PCE reduced the severity of CCl4-induced liver damage. These findings concluded that PCE possesses analgesic, antipyretic, anti-inflammatory, and hepatoprotective activities.
Subject(s)
Plant Extracts/analysis , Asteraceae/classification , Pulicaria/anatomy & histology , Antipyretics/classification , Analgesics/classificationABSTRACT
The aim of this study was to explore the composition and evaluate the in silico and in vitro antioxidants and antimicrobial and anti-inflammatory effects of Apium graveolens var. dulce leaves essential oil (AGO) collected from Al-Kharj (Saudi Arabia). AGO was isolated using the hydro-distillation method, and its composition was studied using gas-chromatography-mass Spectrometry (GC-MS), antimicrobial activities using well diffusion assay, and antioxidant and anti-inflammatory activities using spectrophotometric methods. The pharmacological activities of their major compounds were predicted using PASS (prediction of activity spectra for substances) and drug-likening properties by ADME (absorption, distribution, metabolism, and excretion) through web-based online tools. Isocnidilide (40.1%) was identified as the major constituent of AGO along with ß-Selinene, Senkyunolide A, Phytyl acetate, and 3-Butylphthalide. AGO exhibited a superior antibacterial activity, and the strongest activity was detected against Gram-positive bacteria and Candida albicans. Additionally, it exhibited a weaker antioxidant potential and stronger anti-inflammatory effects. PASS prediction supported the pharmacological finding, whereas ADMET revealed the safety of AGO. The molecular docking of isocnidilide was carried out for antibacterial (DNA gyrase), antioxidant (tyrosinase), and anti-inflammatory (cyclooxygenase-2) activities. The docking simulation results were involved hydrophilic interactions and demonstrated high binding affinity of isocnidilide for anti-inflammatory protein (cycloxygenase-2). The presence of isocnidilide makes AGO a potential anti-inflammatory and antimicrobial agent. AGO, and its major metabolite isocnidilide, may be a suitable candidate for the future drug development.
Subject(s)
Anti-Infective Agents/chemistry , Anti-Inflammatory Agents/chemistry , Antioxidants/chemistry , Apium/chemistry , Oils, Volatile/chemistry , Anti-Infective Agents/pharmacology , Anti-Inflammatory Agents/pharmacology , Antioxidants/pharmacology , Humans , Molecular Docking Simulation , Oils, Volatile/pharmacology , Plant Leaves/chemistry , Saudi ArabiaABSTRACT
BACKGROUND: In the present study, we explored the composition of Cilantro (Coriandrum sativum L. leaves) essential oil (CEO) cultivated in Saudi Arabia (Al-Kharj) and explored its antioxidant, antimicrobial, and anti-inflammatory effects in vitro. METHODS: Gas chromatography-mass spectroscopy was used to detect the CEO composition. The 2, 2-diphenyl-1-picrylhydrazyl (DPPH)-induced free radical and ferric chloride scavenging methods were used to determine the antioxidant activity. Antimicrobial activity was investigated using the well diffusion method. Anti-inflammatory activity was evaluated using egg albumin and trypsin-induced inflammation methods. RESULTS: Forty-six compounds representing 90.17% of the total aroma were identified in the CEO; the major constituents were found to be 1-decanol (17.85%), decanal (11.04%), trans-2-dodecen-1-ol (7.87%), menthone (6.71%), 2-decen-1-ol, trans- (5.44%), dodecanal (4.76%), trans-tetradec-2-enal (3.14%), sedanolide (3.02), and thymol (3.01%). DPPH-induced free radical and ferric chloride scavenging assays demonstrated low antioxidant effects of CEO, and the antioxidant activity was observed at a high CEO concentration. The antimicrobial activity of CEO was assessed against 5 microorganisms (bacteria and fungi) by using well diffusion methods; CEO was found to possess excellent antimicrobial activity against all microorganisms, except Escherichia coli. Moreover, CEO demonstrated strong anti-inflammatory activity against egg albumin- and trypsin-induced inflammation. CONCLUSION: The essential oil extracted from C. sativum chemotype grown in Al-Kharj region of Saudi Arabia possesses low antioxidant potential, superior antimicrobial activity, and outstanding anti-inflammatory effects.
ABSTRACT
This research deals with the determination of solubility, Hansen solubility parameters, dissolution properties, enthalpy-entropy compensation, and computational modeling of a naturally-derived bioactive compound trans-resveratrol (TRV) in water, methanol, ethanol, n-propanol, n-butanol, propylene glycol (PG), and various PG + water mixtures. The solubility of TRV in six different mono-solvents and various PG + water mixtures was determined at 298.2-318.2 K and 0.1 MPa. The measured experimental solubility values of TRV were regressed using six different computational/theoretical models, including van't Hoff, Apelblat, Buchowski-Ksiazczak λh, Yalkowsly-Roseman, Jouyban-Acree, and van't Hoff-Jouyban-Acree models, with average uncertainties of less than 3.0%. The maxima of TRV solubility in mole fraction was obtained in neat PG (2.62 × 10-2) at 318.2 K. However, the minima of TRV solubility in the mole fraction was recorded in neat water (3.12 × 10-6) at 298.2 K. Thermodynamic calculation of TRV dissolution properties suggested an endothermic and entropy-driven dissolution of TRV in all studied mono-solvents and various PG + water mixtures. Solvation behavior evaluation indicated an enthalpy-driven mechanism as the main mechanism for TRV solvation. Based on these data and observations, PG has been chosen as the best mono-solvent for TRV solubilization.
Subject(s)
Propylene Glycol/chemistry , Resveratrol/chemistry , Solvents/chemistry , Water/chemistry , Models, Chemical , Solubility , Thermodynamics , UncertaintyABSTRACT
This article studies the solubility, Hansen solubility parameters (HSPs), and thermodynamic behavior of a naturally-derived bioactive thymoquinone (TQ) in different binary combinations of isopropanol (IPA) and water (H2O). The mole fraction solubilities (x3) of TQ in various (IPA + H2O) compositions are measured at 298.2-318.2 K and 0.1 MPa. The HSPs of TQ, neat IPA, neat H2O, and binary (IPA + H2O) compositions free of TQ are also determined. The x3 data of TQ are regressed by van't Hoff, Apelblat, Yalkowsky-Roseman, Buchowski-Ksiazczak λh, Jouyban-Acree, and Jouyban-Acree-van't Hoff models. The maximum and minimum x3 values of TQ are recorded in neat IPA (7.63 × 10-2 at 318.2 K) and neat H2O (8.25 × 10-5 at 298.2 K), respectively. The solubility of TQ is recorded as increasing with the rise in temperature and IPA mass fraction in all (IPA + H2O) mixtures, including pure IPA and pure H2O. The HSP of TQ is similar to that of pure IPA, suggesting the great potential of IPA in TQ solubilization. The maximum molecular solute-solvent interactions are found in TQ-IPA compared to TQ-H2O. A thermodynamic study indicates an endothermic and entropy-driven dissolution of TQ in all (IPA + H2O) mixtures, including pure IPA and pure H2O.
Subject(s)
2-Propanol/chemistry , Benzoquinones/chemistry , Chemistry, Pharmaceutical/methods , Water/chemistry , Chemistry Techniques, Analytical , Drug Design , Regression Analysis , Reproducibility of Results , Solubility , Solvents , Temperature , ThermodynamicsABSTRACT
Various analytical methodologies have been reported for the determination of 6-shogaol (6-SHO) and 6-gingerol (6-GIN) in ginger extracts and commercial formulations. However, green analytical methods for the determination of 6-SHO and 6-GIN, either alone or in combination, have not yet been reported in literature. Hence, the present study was aimed to develop a rapid, simple, and cheaper green reversed phase high-performance thin-layer chromatography (RP-HPTLC) densitometry method for the simultaneous determination of 6-SHO and 6-GIN in the traditional and ultrasonication-assisted extracts of ginger rhizome, commercial ginger powder, commercial capsules, and commercial ginger teas. The simultaneous analysis of 6-SHO and 6-GIN was carried out via RP-18 silica gel 60 F254S HPTLC plates. The mixture of green solvents, i.e., ethanol:water (6.5:3.5 v/v) was utilized as a mobile phase for the simultaneous analysis of 6-SHO and 6-GIN. The analysis of 6-SHO and 6-GIN was performed at λmax = 200 nm for 6-SHO and 6-GIN. The densitograms of 6-SHO and 6-GIN from traditional and ultrasonication-assisted extracts of ginger rhizome, commercial ginger powder, commercial capsules, and commercial ginger teas were verified by obtaining their single band at Rf = 0.36 ± 0.01 for 6-SHO and Rf = 0.53 ± 0.01 for 6-GIN, compared to standard 6-SHO and 6-GIN. The green RP-HPTLC method was found to be linear, in the range of 100-700 ng/band with R2 = 0.9988 for 6-SHO and 50-600 ng/band with R2 = 0.9995 for 6-GIN. In addition, the method was recorded as "accurate, precise, robust and sensitive" for the simultaneous quantification of 6-SHO and 6-GIN in traditional and ultrasonication-assisted extracts of ginger rhizome, commercial ginger powder, commercial capsules, and commercial ginger teas. The amount of 6-SHO in traditional extracts of ginger rhizome, commercial ginger powder, commercial capsules, and commercial ginger teas was obtained as 12.1, 17.9, 10.5, and 9.6 mg/g of extract, respectively. However, the amount of 6-SHO in ultrasonication-assisted extracts of ginger rhizome, commercial ginger powder, commercial capsules, and commercial ginger teas were obtained as 14.6, 19.7, 11.6, and 10.7 mg/g of extract, respectively. The amount of 6-GIN in traditional extracts of ginger rhizome, commercial ginger powder, commercial capsules, and commercial ginger teas were found as 10.2, 15.1, 7.3, and 6.9 mg/g of extract, respectively. However, the amount of 6-GIN in ultrasonication-assisted extracts of ginger rhizome, commercial ginger powder, commercial capsules, and commercial ginger teas were obtained as 12.7, 17.8, 8.8, and 7.9 mg/g of extract, respectively. Overall, the results of this study indicated that the proposed analytical technique could be effectively used for the simultaneous quantification of 6-SHO and 6-GIN in a wide range of plant extracts and commercial formulations.
ABSTRACT
Two new sesquiterpenoids belonging to the guaiane, 4α,9α,10α-trihydroxyguaia-11(13)en-12,6α-olide (1), and germacrane, 9ß-hydroxyparthenolide-9-O-ß-D-glucopyranoside (2), classes have been isolated from the leaves of the Saudi medicinal plant Anvillea garcinii along with seven known compounds (3-9). The structures of the new metabolites were elucidated by spectroscopic analysis, including one-dimensional (1D) and two-dimensional (2D) Nuclear Magnetic Resonance (NMR) and high-resolution electrospray ionization mass spectrometry (HR-ESIMS). The antimicrobial properties of 1-9 were screened against seven different pathogenic microbes, and compounds 1-3 showed a potent antifungal activity.
Subject(s)
Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Asteraceae/chemistry , Plant Components, Aerial/chemistry , Sesquiterpenes/chemistry , Sesquiterpenes/pharmacology , Magnetic Resonance Spectroscopy , Microbial Sensitivity Tests , Molecular Structure , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plants, MedicinalABSTRACT
Four new sesquiterpene lactones, 4α-hydroxy-guaia-10(14),11(13)-diene-12,6α-olide (1), 4α-hydroxy-9α-acetoxy-guaia-1(10),2-diene-12,6α-olide (4), 4α-hydroxy-9ß-acetoxy-guaia-1(10),2-diene-12,6α-olide (5), and 1α,4α-dihydroxy-9α-acetoxy-guaia-10(14),2-diene-12,6α-olide (6), were isolated from the aerial parts of Anthemis scrobicularis. Their structures were elucidated on the basis of their IR, NMR, and MS spectroscopic data. In addition, two known sesquiterpene lactones micheliolide (2) and achillin (3) were also isolated. The cytotoxicity of some of the isolated compounds was tested against HCT 116, HepG-2, and MCF-7 cell lines. Micheliolide and 4α-hydroxy-guaia-10(14),11(13)-diene-12,6α-olide showed pronounced inhibitory activity while 4α-hydroxy-9α-acetoxy-guaia-1(10),2-diene-12,6α-olide showed weak activity.
Subject(s)
Anthemis/chemistry , Antineoplastic Agents, Phytogenic/isolation & purification , Antineoplastic Agents, Phytogenic/pharmacology , Lactones/isolation & purification , Lactones/pharmacology , Sesquiterpenes/isolation & purification , Sesquiterpenes/pharmacology , Antineoplastic Agents, Phytogenic/chemistry , Drug Screening Assays, Antitumor , HCT116 Cells , Hep G2 Cells , Humans , Lactones/chemistry , MCF-7 Cells , Molecular Structure , Sesquiterpenes/chemistry , Sesquiterpenes, Guaiane/chemistry , Sesquiterpenes, Guaiane/isolation & purification , Sesquiterpenes, Guaiane/pharmacologyABSTRACT
Date palm, Phoenix dactylifera L. (Arecaceae), grows commonly in the Arabian Peninsula and is traditionally used to treat various diseases. The aim of the present study was to identify chemical composition of the essential oil and to investigate the repellent activity. The essential oil of P. dactylifera was obtained by hydrodistillation from the spathe, a specialized leaf structure that surrounds the pollinating organs of the palm. The oil was subsequently analyzed by GC-FID and GC-MS. The oil showed promising repellent activity against yellow fever mosquito - Aedes aegypti. Sixteen components were characterized, constituting 99% of the oil. The main components were 3,4-dimethoxytoluene (73.5%), 2,4-dimethoxytoluene (9.5%), ß-caryophyllene (5.5%), p-cresyl methyl ether (3.8%), and caryophyllene oxide (2.4%). The minimum effective dosage (MED) for repellency for the P. dactylifera oil was 0.051mg/cm(2), which had moderately lower potency compared to reference standard N,N-diethyl-3-methylbenzamide, DEET (0.018mg/cm(2)) in the "cloth patch assay". The five major compounds were individually assayed for repellency to determine to what extent each is responsible for repellency from the oil. 3,4-Dimethoxytoluene and 2,4-dimethoxytoluene showed the best repellent activity with the same MED value of 0.063mg/cm(2), respectively. The results indicate that these two constituents which comprise a large proportion of the P. dactylifera oil (83%) are likely responsible for the observed repellent activity. In this aspect, the P. dactylifera spathe oil is a sustainable, promising new source of natural repellents.