Clausena anisata is one of the medicinal plants used traditionally for treatment of parasitic infections, irritation (boils, ringworm, and eczema), flatworm infestations, influenza, abdominal cramps, and constipation. Phytochemical screening test of dichloromethane/methanol (1 : 1) roots extract revealed the presence of flavonoids, phytosterols, coumarins, phenols, alkaloids, tannins, terpenoids, and free reducing sugars and the absence of saponins. Silica gel column chromatographic separation of the dichloromethane/methanol (1 : 1) extract afforded a carbazole alkaloid derivative of heptazoline ( 1 ) and three coumarins ( 2 – 4 ), including the known coumarins imperatorin ( 3 ) and chalepin ( 4 ). Structures of the compounds were elucidated by spectroscopic techniques (IR, 1 H NMR, 13 C NMR, and DEPT-135). Antibacterial activity of the crude extracts and isolated compounds was screened using agar diffusion method against strains of Staphylococcus aureus , Escherichia coli , Pseudomonas aeruginosa , and Bacillus substilis . The results of antibacterial test revealed derivative of heptaphylline ( 1 ) and imperatorin ( 3 ) exhibited comparable antibacterial activity against S. aureus and B. substilis (14 and 13 mm zone of inhibition, respectively) to that of ciprofloxacin (15 mm zone of inhibition) at a concentration of 20 µ g/mL. Chalepin ( 4 ) revealed more antibacterial activity against B. substilis (16 mm zone of inhibition) compared to ciprofloxacin (15 mm).
Bergapten (5-methoxypsoralen, 5-MOP) is a plant-derived furocoumarin with demonstrated anti-inflammatory action. The present study investigated its effects on allergic inflammation in two related pathways of mast cell degranulation. Compound 48/80 and lipopolysaccharide (LPS) were used to activate the IgE-independent pathway while bovine serum albumin (BSA) was used as allergen for the IgE-dependent pathway. The modulatory effect of bergapten on mast cell degranulation, neutrophil extravasation, protein concentration, lung histopathology, and oxidative stress was assessed. Bergapten at 10, 30, and 100 μ g/ml for 15 min stabilized mast cells in rat mesenteric tissue from disruption in vitro and when administered in vivo at 3, 10, and 30 mg kg −1 for 1 h protected mice from fatal anaphylaxis induced by compound 48/80. Similarly, treatment of LPS-challenged mice with bergapten (3, 10, and 30 mg kg −1 ) for 24 h significantly decreased neutrophil infiltration into bronchoalveolar lavage fluid, mean protein concentration, and inflammatory cell infiltration of pulmonary tissues when compared to the saline-treated LPS-challenged control. In addition, lung histology of the bergapten-treated LPS-challenged mice showed significantly less oedema, congestion, and alveolar septa thickening when compared to the saline-treated LPS-challenged disease control. LPS-induced oxidative stress was significantly reduced through increased tissue activities of catalase and superoxide dismutase and reduced malondialdehyde levels on treatment with bergapten. In the triple antigen-induced active anaphylaxis, daily administration of bergapten at 3, 10, and 30 mg kg −1 for 10 days, respectively, protected previously sensitized and challenged mice against anaphylactic shock. Overall, our study demonstrates the ability of bergapten to attenuate allergic airway-induced hypersensitivity in murine models of inflammation, suggesting its possible therapeutic benefit in this condition.
Honey Bee Venom has various biological activities such as inhibitory effect on several types of cancer. Cisplatin is an old and potent drug to treat the most of cancer. Our aims in this study were determination of the anti-mutagenic and cytotoxic effects of HBV on mammary carcinoma, lonely and in combination with cisplatin. In this study 4T1 cell line were cultured and incubated at 37 C in humidified CO2-incubator. The cell viabilities were examined by MTT assay. Also HBV was screened for its anti-mutagenic activity against sodium azide by Ames test. The result showed that 6μg/ml HBV, 20μg/ml cisplatin and 6μg/ml HBV with 10μg/ml cisplatin can induce an approximately 50% 4T1 cell death. 7mg/ml HBV with the inhibition of 62.76% sodium azide showed high potential in decreasing the mutagenic agents. MTT assay demonstrated that HBV and cisplatin can cause cell death in a dose-dependent manner. The cytotoxic effect of cisplatin is also promoted by HBV. Ames test results indicated that HBV can inhibit sodium azide as a mutagenic agent. Anti-mutagenic activity of HBV was increased significantly in presence of S9 mix. Hence, our findings reveal that HBV can enhance the cytotoxic effect of cisplatin drug and it has cancer preventing effects.
Nutraceuticals are the pharmaceutically blended products that possess both nutritional as well as the medicinal value. Such a product is designed to improve the physical health, fight against day-to-day challenges such as stress, increase longevity, etc. Nowadays, emphasis is given to those herbs which are used as food and medicine due to its greater acceptance. Due to dynamic action, the popularity of nutraceuticals among people as well as healthcare providers has been increased over medicines and health supplements. This review documents herbs with a wide variety of therapeutic values such as immunity booster, antidiabetic, anticancer, antimicrobial, and gastroprotective. These herbs could be better options to formulate as nutraceuticals. Several nutraceuticals are described based on their availability as food, chemical nature, and mechanism of action.
Different solvent extracts of Pereskia bleo leaves were evaluated for total phenolic content (TPC) and antioxidant activities based on the Folin–Ciocalteu test and DPPH scavenging activities. The antibacterial activities against four bacteria, namely, Gram-positive bacteria: Streptococcus pyogenes ATCC 19615 (SP) and Staphylococcus aureus ATCC 29737 (SA) and Gram-negative bacteria: Escherichia coli ATCC 10536 (EC) and Pseudomonas aeruginosa ATCC 9027 (PA), were also performed based on the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) assays. The findings demonstrated that both the methanolic and chloroform extracts displayed strong activities against SA, SP, EC, and PA while the hexane extract demonstrated the weakest activities towards all the four bacteria. The methanolic extract also exhibited higher TPC and possessed higher antioxidant activity with the IC50 value 33.83 µg/mL compared to the chloroform and hexane extracts. As such, the methanolic extract has a higher ability to scavenge free radical compared to other extracts. Due to the interesting result, activities are shown by the methanolic and chloroform crude extracts of P. bleo; hence, the study has been extended to the isolation of bioactive compounds to uncover its great potential as a natural source for antibacterial and antioxidant agents.
This study evaluated the effect of combined inositol hexakisphosphate (IP6) and inositol supplement on organ weight, intestinal ATPase activities, complete blood count, and serum analytes in streptozotocin (STZ)-induced type 2 diabetic rats. High-fat diet and a single intraperitoneal injection of streptozotocin (35 mg/kg body weight) were used to induce type 2 diabetes mellitus in Sprague–Dawley rats. The diabetic groups were then treated with either combined IP6 and inositol supplement or glibenclamide for four weeks. Organ weights, intestinal ATPase activities, complete blood count, serum α -amylase, total protein, albumin, and globulin content were determined. Pancreatic weight was significantly reduced while relative kidney and liver weights were elevated in the group treated with combined IP6 and inositol supplement compared to the nondiabetic control. Serum α -amylase activity for the glibenclamide and combination treated groups was significantly improved compared to that of the untreated diabetic group. Red cell distribution width percentage was significantly lower in the combination treated group compared to that in the untreated diabetic group, while intestinal ATPase activities were unaffected by the treatment regime. Combined IP6 and inositol supplement consumption may protect people with diabetes from increased risk of cardiovascular diseases due to the supplement's ability to maintain red cell distribution width percentage towards the normal control group.
The aim of this study was to evaluate the effects of the aqueous extract of Baillonella toxisperma stem bark on dexamethasone-induced insulin resistance in rats. A quantitative phytochemical study was done on the aqueous extract of Baillonella toxisperma for the total phenol, flavonoid, and flavonol determination. Insulin resistance was induced by intraperitoneal injection of dexamethasone (1 mg/kg) for 8 days, one hour before oral administration of different treatments (extract at doses of 60, 120, and 240 mg/kg and metformin at 40 mg/kg). During the test, body weight and blood glucose level were evaluated on days 1 and 8. At the last day of treatment, the glucose tolerance test was performed in rats; after that, blood samples were collected for triglycerides, total cholesterol, LDL and HDL cholesterols, transaminases (ALT and AST), and total protein level determination. Organs (heart, liver, pancreas, and kidneys) were also collected for the relative organ weight determination. The results showed that the aqueous extract of B. toxisperma is rich in total phenols, flavonoids, and flavonols. This extract significantly reversed the metabolic alterations (lipid profile, protein level, and transaminase activity) induced by dexamethasone in rats. At doses of 120 and 60 mg/kg, Baillonella toxisperma also significantly decreases (p<0.05; p<0.01) postprandial hyperglycemia in insulin resistance rats. The results suggest that Baillonella toxisperma can manage insulin resistance and may be useful for the treatment of type 2 diabetes mellitus.
OBJECTIVE:This study aims to investigate the effect of combining calcium and vitamin D supplements with metformin on menstrual cycle abnormalities, gonadotropins, and IGF-1 system in vitamin D-deficient/insufficient PCOS women.STUDY DESIGN:This is a randomized, placebo-controlled clinical trial.SETTING:This study was performed in Damascus University of Obstetrics and Gynecology Hospital and Orient Hospital, in Damascus, Syria.MATERIALS AND METHODS:Forty PCOS women with 25-OH-vitamin D < 30 ng/ml were randomly assigned to take either metformin (1500 mg/daily) plus placebo or metformin (1500 mg/daily) plus calcium (1000 mg/daily) and vitamin D3 (6000 IU/daily) orally for 8 weeks. Serum levels of gonadotropins (luteinizing hormone (LH) and follicle-stimulating hormone (FSH)), insulin-like growth factor-1 (IGF-1), and insulin-like growth factor binding protein-1 (IGFBP-1) were detected at the baseline during the early follicular phase of a spontaneous or induced menstrual cycle and after 8 weeks of intervention (except for the final gonadotropins levels which were assayed from samples obtained during the early follicular phase of a spontaneous menstrual cycle).RESULTS:Thirty-four patients (85%) completed the study. After 8 weeks of intervention, calcium and vitamin D co-supplementation led to a significant increase in 25-OH-vitamin D levels and calcium levels in the supplementation group compared to the other group (change in 25-OH-vitamin D levels: +19.38 ± 7.78 vs +0.11 ± 4.79 ng/ml, respectively; p value=0.0001) (change in calcium levels: +0.83 ± 0.82 vs +0.01 ± 0.86 mg/dl, respectively; p value=0.014). An improvement in menstrual cycle irregularity was detected in 38.5% and 58.8% of patients in metformin-placebo group and metformin-calcium-vitamin D group, respectively; but the change was statistically significant only in the supplementation group (p value=0.002). Nevertheless, the means of changes from baseline in gonadotropins levels (serum levels of LH, FSH, and LH to FSH ratio) and the studied parameters of IGF-1 system (serum levels of IGF-1, IGFBP-1, and IGF-1 to IGFBP-I ratio) did not differ significantly between the two groups.CONCLUSIONS:Calcium and vitamin D supplements can support metformin effect on regulation of menstrual cycle irregularity in vitamin D-deficient/insufficient PCOS patients, but this effect is not associated with any significant changes in gonadotropins or IGF-1 system. These results suggest a possible role of calcium and vitamin D supplements in managing PCOS. However, further studies are needed to identify the underlying mechanisms. The Clinical Trial Registration Number is NCT03792984.
Betula alnoides is a medicinal plant in Thai traditional longevity preparations. The crude extracts of this plant possess various biological activities. However, the isolated compounds from this plant have no reports of anti-HIV-1 integrase (IN) activity. Therefore, the present study aims to investigate the anti-HIV-1 integrase and anti-inflammatory effects of isolated compounds from this plant and predict the interaction of compounds with integrase active sites. From the bioassay-guided fractionation of the ethanol extract of B. alnoides stems using chromatographic techniques, five pentacyclic triterpenoid compounds were obtained. They are betulinic acid ( 1 ), betulin ( 2 ), lupeol ( 3 ), oleanolic acid ( 4 ), and ursolic acid ( 5 ). Compound 2 exhibited the most potent inhibitory activity against HIV-1 IN, with an IC 50 value of 17.7 μ M. Potential interactions of compounds with IN active sites were investigated using computational docking. The results indicated that active compounds interacted with Asp64, a residue participating in 3′-processing, and Thr66, His67, and Lys159, residues participating in strand-transfer reactions of the integration process. Regarding anti-inflammatory activity, all compounds exerted significant inhibitory effects on LPS-induced nitric oxide production (IC 50 < 68.7 μ M). Thus, this research provides additional scientific support for the use of B. alnoides in traditional medicine for the treatment of HIV patients.
erefore, this issue will hopefully pave a way for researchers and encourage the scientific research community for further research in this field for the development of safer, selective, and cost-effective drugs from natural products.
The aim of this study was to synthesize a series of nickel(II)phthalocyanines (NiPcs) bearing four 4(3H)-quinazolinone ring system units, (qz)(4)NiPcs 4a-d. The electronic factors in the 4(3H)-quinazolinone moiety that attached to the NiPc skeleton had a magnificent effect on the antibacterial activity of the newly synthesized (qz)(4)NiPcs 4a-d against Escherichia coli. The minimum MICs and MBCs value were recorded for compounds 4a, 4b, 4c, and 4d, respectively. The results indicated that the studied (qz)(4)NiPcs 4a-d units possessed a broad spectrum of activity against Escherichia coli. Their antibacterial activities were found in the order of 4d>4c>4b>4a against Escherichia coli, and the strongest antibacterial activity was achieved with compound 4d.
Parkinson's disease (PD) is a common neurodegenerative disorder characterized by selective loss of dopamine neurons in the substantia nigra pars compacta of the midbrain. Reports from postmortem studies in the human PD brain, and experimental PD models reveal that endoplasmic reticulum (ER) stress is implicated in the pathogenesis of PD. In times of stress, the unfolded or misfolded proteins overload the folding capacity of the ER to induce a condition generally known as ER stress. During ER stress, cells activate the unfolded protein response (UPR) to handle increasing amounts of abnormal proteins, and recent evidence has demonstrated the activation of the ER chaperone GRP78/BiP (78 kDa glucose-regulated protein/binding immunoglobulin protein), which is important for proper folding of newly synthesized and partly folded proteins to maintain protein homeostasis. Although the activation of this protein is essential for the initiation of the UPR in PD, there are inconsistent reports on its expression in various PD models. Consequently, this review article aims to summarize current knowledge on neuroprotective agents targeting the expression of GRP78/BiP in the regulation of ER stress in experimental PD models.
The nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly prescribed by medical practitioners in many clinical conditions for the symptomatic treatment of pain and fever. Due to their anti-inflammatory properties, these drugs have been investigated for their anticancer effects in numerous studies. This is because chronic inflammation has long been linked to carcinogenesis. As such, anti-inflammatory drugs are believed to play a role in cancer treatment and prevention. In the past few decades, research has shown that NSAIDs may decrease the risk of certain types of cancer. However, there is also a growing body of research that proves the contrary. Furthermore, NSAIDs are well known for many side effects, including some life-threatening ones. This review will discuss the relationship between chronic inflammation and cancer, the role of NSAIDs in cancer prevention and cancer promotion, and some of the potentially lethal side effects of these drugs.
Spondyloarthritis or spondyloarthropathy (SpA) is a group of related rheumatic disorders, which presents with axial and nonaxial features, affecting structures within the musculoskeletal system, as well as other bodily systems. Both pharmacological and nonpharmacological therapeutic options are available for SpA. For decades, nonsteroidal anti-inflammatory drugs (NSAIDs) have been used as the first-line drugs to treat the disease. Research has shown that other than pain relief, NSAIDs have disease-modifying effects in SpA. However, to achieve these effects, continuous and/or long-term NSAID use is usually required. This review will give an overview of SpA, discuss NSAIDs and their disease-modifying effects in SpA, and highlight some of the important adverse effects of long-term and continuous NSAID use, particularly those related to the gastrointestinal, renal, and cardiovascular systems.
Depression is currently recognized as a crucial problem in everyday clinical practice, in light of ever-increasing rates of prevalence, as well as disability, morbidity, and mortality related to this disorder. Currently available antidepressant drugs are notoriously problematic, with suboptimal remission rates and troubling side-effect profiles. Their mechanisms of action focus on the monoamine hypothesis for depression, which centers on the disruption of serotonergic, noradrenergic, and dopaminergic neurotransmission in the brain. Nevertheless, views on the pathophysiology of depression have evolved notably, and the comprehension of depression as a complex neuroendocrine disorder with important systemic implications has sparked interest in a myriad of novel neuropsychopharmacological approaches. Innovative pharmacological targets beyond monoamines include glutamatergic and GABAergic neurotransmission, brain-derived neurotrophic factor, various endocrine axes, as well as several neurosteroids, neuropeptides, opioids, endocannabinoids and endovanilloids. This review summarizes current knowledge on these pharmacological targets and their potential utility in the clinical management of depression.
The current focus of nanotechnology is to develop environmentally safe methodologies for the formulation of nanoparticles. The phytochemistry of Zingiber officinale inspired us to utilize it for the synthesis of iron nanoparticles. GC-MS analysis revealed the phytochemical profile of ginger. Out of 20 different chemicals, gingerol was found to be the most potent phytochemical with a retention time of 40.48 min. The present study reports a rapid synthesis method for the formation of iron nanoparticles and its potential efficacy as an antibacterial agent and an antioxidant. Because of its antibacterial property, ginger extract was used to coat surgical cotton. Synthesized ginger root iron nanoparticles (GR-FeNPs) were characterized by UV-visible spectroscopy, Fourier-transform infrared spectroscopy (FT-IR), X-ray diffraction analysis, and particle size analysis. XRD confirmed the crystalline structure of iron oxide nanoparticles as it showed the crystal plane (2 2 0), (3 1 1), (2 2 2), and (4 0 0). The particle size analyzer (PSA) showed the average size of the particles, 56.2 nm. The antimicrobial activity of the FeNPs was tested against different Gram-positive and Gram-negative bacteria. E. coli showed maximum inhibition as compared with the other organisms. Antioxidant activity proved the maximum rate of free radicals at 160 µg/mL produced by nanoparticles. In addition, the antimicrobial activity of nanocoated surgical cotton was evaluated on the first day and 30th day after coating, which clearly showed excellent growth inhibition of organisms, setting a new path in the field of medical microbiology. Hence, iron-nanocoated surgical cotton synthesized using green chemistry, which is antimicrobial and cost effective, might be economically helpful and provide insights to the medical field, replacing conventional wound healing treatments, for better prognosis.
Rapid, eco-friendly, and cost-effective one-pot synthesis of copper nanoparticles is reported here using medicinal plants like Gnidia glauca and Plumbago zeylanica . Aqueous extracts of flower, leaf, and stem of G. glauca and leaves of P. zeylanica were prepared which could effectively reduce Cu 2+ ions to CuNPs within 5 h at 100°C which were further characterized using UV-visible spectroscopy, field emission scanning electron microscopy, high-resolution transmission electron microscopy, energy dispersive spectroscopy, dynamic light scattering, X-ray diffraction, and Fourier-transform infrared spectroscopy. Further, the CuNPs were checked for antidiabetic activity using porcine pancreatic α -amylase and α -glucosidase inhibition followed by evaluation of mechanism using circular dichroism spectroscopy. CuNPs were found to be predominantly spherical in nature with a diameter ranging from 1 to 5 nm. The phenolics and flavonoids in the extracts might play a critical role in the synthesis and stabilization process. Significant change in the peak at ∼1095 cm −1 corresponding to C-O-C bond in ether was observed. CuNPs could inhibit porcine pancreatic α -amylase up to 30% to 50%, while they exhibited a more significant inhibition of α -glucosidase from 70% to 88%. The mechanism of enzyme inhibition was attributed due to the conformational change owing to drastic alteration of secondary structure by CuNPs. This is the first study of its kind that provides a strong scientific rationale that phytogenic CuNPs synthesized using G. glauca and P. zeylanica can be considered to develop candidate antidiabetic nanomedicine.
One of the main focuses of tissue engineering is to search for tridimensional scaffold materials, complying with nature’s properties for tissue regeneration. Determining material biocompatibility is a fundamental step in considering its use. Therefore, the purpose of this study was to analyze osteoblast cell adhesion and viability on different materials to determine which was more compatible for future bone regeneration. Tridimensional structures were fabricated with hydroxyapatite, collagen, and porous silica. The bovine bone was used as material control. Biocompatibility was determined by seeding primary osteoblasts on each tridimensional structure. Cellular morphology was assessed by SEM and viability through confocal microscopy. Osteoblast colonization was observed on all evaluated materials’ surface, revealing they did not elicit osteoblast cytotoxicity. Analyses of four different materials studied with diverse compositions and characteristics showed that adhesiveness was best seen for HA and viability for collagen. In general, the results of this investigation suggest these materials can be used in combination, as scaffolds intended for bone regeneration in dental and medical fields.
The objective of the present study was to evaluate “DXB-2030,” a polyherbal combination of Trigonella foenum-graecum, Aloe vera, Sphaeranthus indicus, Nardostachys jatamansi, and Symplocos racemosa extracts in an experimental model of testosterone propionate (TP), induced polycystic ovary syndrome (PCOS) in female rats. Thirty animals were divided into 3 groups of 10 each; group 1 served as normal control; group 2 was administered with TP and served as positive control; along with TP, group 3 was treated with “DXB-2030” at a dose of 100 mg/kg p.o., for 60 days. At the end of the study period, the animals were subjected for the estimation of serum testosterone levels, oral glucose tolerance test (OGTT), weight of the ovaries, estrous cycle, and histopathological evaluation. An in vitro assay on GLUT4 expression was carried out to understand the effect of “DXB-2030” on insulin resistance. Results showed that treatment with “DXB-2030” reversed the TP-induced changes by increasing the GLUT4 expression and decreasing the body weight, testosterone levels, AUC of glucose in OGTT, and the cystic follicles of the ovaries, thus indicating its beneficial effect in PCOS by ameliorating the metabolic dysfunction and reproductive impairment, which are the pathophysiological conditions associated with PCOS. From the results obtained, it can be concluded that “DXB-2030” was effective in the management of experimental PCOS and hence may be recommended in the treatment of PCOS.
