Pharmaceutical Sciences
Volume:28 Issue: 4, Oct 2022

Vitamin C (ascorbic acid) is a micronutrient imperative for many bodily functions, with research revealing its functional support of leukocytes. The purpose of this meta-analysis was to determine the effects of surgery on leukocyte vitamin C concentrations by assessing the amount and longevity of post-operative leukocyte vitamin C change.

We searched the PubMed, Scopus and the Cochrane Library databases for relevant research papers. Studies were included until January 2022, with no time limits. Studies that reported means and standard deviations of leukocyte/buffer layer vitamin C concentrations before and after surgery were included into the meta-analysis. The meta-analysis comprised of eight studies.

Seven studies (which included eight individual studies) were included into our meta-analysis. Combined data from the meta-analysis displayed a significant depletion in mean leukocyte vitamin C concentrations during the first 24 hours following the surgery by a mean of 5.37 µg/108 (32.3%) (CI = -6.35, -4.40) (n = 6, p < 0.001) and during the first post-operative week by 4.43 µg/108 (23%) (-7.27, -1.58) (n = 7, p < 0.001). However, this depletion was followed by an uprise in mean ascorbic acid leukocyte concentrations of 0.93 µg/108 (4.8%) (-0.79, 2.66) (n = 6, p = 0.29) at 7 days (or beyond) post-operatively.

Significant post-operative leukocyte vitamin C depletions were particularly observed during the first post-operative week. Further research is required to validate the observed results and to determine whether the observed depletions may be linked to compromised immunological function and pathophysiologies that arise during the post-operative period.

High blood pressure is the main risk factor for cardiovascular disease and should be controlled primarily by changes in lifestyle, such as regular exercise, a low-salt diet, and weight loss in overweight or obesity. If lifestyle changes are not enough, many types of medications can be used to control high blood pressure; however, side effects constitute one of the most critical limitations of conventional medicines associated with high blood pressure. For this reason, the use of traditional and herbal medicines has been welcomed by the public for many years. Hibiscus sabdariffa is one of the most suitable herbal medicines for hypertension. According to research results, it has the same effect as conventional medicines without serious side effects. The present study introduces sour tea as a suitable herbal medicine for high blood pressure to provide readers of this article with a comprehensive understanding of the medicinal properties of Hibiscus sabdariffa for the treatment of hypertension and its effects on several other common diseases, including cancer.

Nicotine, a psychoactive compound from the tobacco plant, produces a reward effect that potentially causes addiction. It is postulated that nicotine addiction occurs through increased reactive oxygen species production in nucleus accumbens, which causes damage to the endogenous antioxidant defense system resulting in an increased need for nicotine intake, which leads to addiction. The antioxidants, andrographolide and epigallocatechin gallate (EGCG), are expected as potential substances to decrease the risk of nicotine addiction. This study aimed to analyze the effect of andrographolide and EGCG on the risk of addiction induced by nicotine and cigarette smoke extract (CSE) in mice.

Thirty-five Balb/c male mice, divided into seven groups, were used in this study. The administered drugs were normal saline 1.0 mL/kg BW as control group, nicotine 0.5 mg/kg BW, CSE 1.0 mg/kg BW, andrographolide 50 mg/kg BW, and EGCG 50 mg/kg BW as pre-treatment. Conditioned place preference (CPP) with a biased design method was used to evaluate the reward effects induced by nicotine and CSE. Several stages were carried out, namely pre-conditioning, conditioning, post-conditioning, extinction, and reinstatement tests.

Based on the CPP score, both nicotine (p<0.001) and CSE (p<0.001) groups increased the reward effect significantly compared to that of the normal saline group. The andrographolide + nicotine (p<0.001) and EGCG + nicotine (p<0.001) groups decreased the reward effect significantly compared to that of the nicotine group without pharmacological treatment. Similarly, the andrographolide + CSE (p<0.001) and EGCG + CSE (p<0.01) groups decreased the reward effect significantly compared to that of the CSE group without pharmacological treatment.

Andrographolide and EGCG lower the risk of addiction induced by nicotine and CSE.

As the use of Gentamicin became more widespread, the drug’s harmful effects, particularly nephrotoxicity, became increasingly well-known. Antibacterial and anti-inflammatory properties have long been associated with Mirazid. The goal of this research was to find out more about frameworks for the protection of Mirazid against nephrotoxicity triggered by Gentamicin.

Three groups of albino male rats were created; the normal group received only saline. In the second group, nephrotoxicity was produced for 10 days with Gentamicin (100 mg/kg; i.p.). In the third group; Mirazid (10 mg/kg; p.o.) was administered for 10 days before receiving Gentamicin. This was done to investigate the kidney/body weight index, serum creatinine, urea, lactate dehydrogenase (LDH), malondialdehyde (MDA), and Glutathione (GSH) levels. Moreover, immunohistochemical staining was done to study Jun N- terminal kinase 1 (JNK1), inducible nitric oxide synthase (iNOS), and caspase3 expressions along with histopathological changes. Additionally, a molecular docking study was performed for the seventeen isolated and identified compounds from myrrh, JNK1 is inhibited by an oleo-gum resin derived from the Commiphora species of plants (Burseraceae).

The Gentamicin group showed an increase in kidney/ body weight index, serum creatinine, urea, LDH, and MDA, while decreasing GSH levels. Furthermore, immunohistochemical staining revealed increased JNK1, iNOS, and caspase3 expressions along with histopathological changes. All of these indicators were significantly reduced by mirazid, which also restored oxidant/antioxidant hemostasis. Furthermore, the histological architecture of tissues has been significantly conserved. Concerning the docking study, the isolated compound (12) was found to be superior to the co-crystallized inhibitor (18) with a binding score of -7.19 kcal/mol compared to -6.95, respectively.

Mirazid was found to be a potential method for suppressing the nephrotoxicity caused by Gentamycin by inhibiting the JNK1/ iNOS pathways, therefore preserving kidney function. The antioxidant, anti-inflammatory, and anti-apoptotic properties of mirazid are thought to be responsible for its preventive efficacy.

There is a well-documented cross-talk between the gut and brain. Evidence is accumulating to suggest beneficial effects of psychobiotics [prebiotics, probiotics or synbiotics] on psychological distress in disease states. However, their role in healthy status remains relatively unclear. The present study was aimed to clarify if psychobiotics could influence behavioral responses and physiological stress in healthy rats.

In the present experiment, 28 male Wistar rats were divided into four groups (healthy rats treated by Lactobacillus plantarum (L. plantarum), inulin, and their combination (synbiotic), as well as control group). Then, psychobiotics were administered to the intervention groups for 8 weeks. Behavioral tests (Morris water maze, Elevated plus maze, and Forced swimming test) were performed at endpoint. Then, serum and brain levels of superoxide dismutase, malondialdehyde, glutathione peroxidase, total antioxidant capacity, brain-derived neurotrophic factor (BDNF), and serotonin were measured.

Our findings indicated that unlike inulin, the administration of L. plantarum and synbiotic could ameliorate depression and anxiety-like behavior and cognitive performance (P<0.05). Serum and brain oxidative stress markers were significantly improved by synbiotic consumption. The intake of L. plantarum led to decreased oxidative stress in the hippocampus and amygdala (P<0.05). A significant increase in the hippocampal serotonin and BDNF concentration was also observed after both synbiotic and L. plantarum intake (P<0.05). In addition, there was a strong correlation of serum and brain markers with behavioral performance (P< 0.05).

The present study suggests that psychobiotics therapy may have favorable effects on the amelioration of some psychological disorders.

Combinatorial medicine includes promising therapeutic methods for diseases such as cancer, whereby various biochemical and physical agents are simultaneously used to remove tumors. For example, the effectiveness of hyperthermia as a new technique for cancer therapy, can be enhanced, if it is combined with chemical compounds. Herein, the influence of quercetin as a heat shock protein (HSP) inhibitor on the efficiency of cobalt ferrite-graphene oxide (CoFe2O4-GO) nanoparticles-based hyperthermia was investigated in an in vitro study.

Firstly, the surface of graphene sheets was decorated with CoFe2O4 nanoparticles (5-8 nm) and assayed using transmission electron microscopy (TEM), vibrating-sample magnetometer (VSM) and X-ray diffraction (XRD). The cytotoxic effect of the corresponding co-implementation was then examined in MCF7 cell line with or without hyperthermia by (3-(4,5-dimethyl thiazolyl-2)-2,5-diphenyltetrazolium bromide) (MTT) test for 24, 48 and 72 hrs. In addition, the expression of Bax, Bcl2 and HSP70 genes and the production of radicals were evaluated by Real-Time PCR and DPPH (2,2-diphenyl-1-picrylhydrazyl) assays respectively.

The study showed that the doses associated with the IC50 points for quercetin and the CoFe2O4-GO nanocomposite were 0.02 mg/ml and 0.001 g/ml, respectively. The results showed that the simultaneous treatment of the cancer cells with quercetin, the nanocomposite, and hyperthermia significantly improves the cytotoxicity effect, increases the expression of Bax gene and down-regulates HSP70 and Bcl2 genes. In addition, the greatest attenuation of DPPH free radicals was observed in the corresponding group.

The hybrid treatment of quercetin and the nanoparticle in the presence of hyperthermia could be considered as a promising approach for cancer therapy with minor side effects.

The development of the pyrazole-based complexes is greatly enhanced due to the identification of their structure as medicinal application. Keeping in view therapeutic and biological activities of pyrazoles based compounds and the potential of transition metals in the antimicrobial application area, we find it vital to join the chemistry of both moieties in designing and developing biometal compounds which could aggressively work against various bacterial species and cancer cells. In this work, we report the synthesis and characterization of copper (II), nickel (II) and cobalt (II) complexes of dihydrobis(pyrazolyl)borate ligands. Also, antibacterial activities, MTT assay and molecular docking of these compounds were investigated.

A bidentate N-donor pyrazole-based ligand abbreviated as K[H2B(PzMe2)2] and corresponding complexes with Cu(II), Ni(II) and Co(II) were synthesized and characterized. The anticancer activities of the synthesized compounds were studied against the (MDA-MB-231) cell lines. The antibacterial investigations of the synthesized compounds against the gram-positive (B. subtilis) and the gram-negative (S. enterica) bacteria were performed. In addition, molecular docking of the synthesized compounds with YmaH (PDB ID: 3HSB) protein, ecKAS III (PDB ID:1HNJ) protein and DNA dodecamer (PDB ID: 1BNA) as the possible targets was studied.

The result showed among the investigated compounds, complex [Cu(H2B(PzMe2)2)2] indicated the highest cytotoxicity and bacterial inhibition.

In summary, we have synthesized a type of N- donor pyrazole-based ligand and corresponding metal complexes. In silico molecular docking along with the experimental MTT assay and antibacterial studies, indicated the metal complexes are more bioactive than free ligand and can be excellent candidates for further evaluations in the biological area.

Lamotrigine is widely used in the management of partial epilepsy, generalized tonic-clonic epilepsy and Lenox-Gastut syndrome and is an add-on therapy in the treatment of complex and simple partial seizures and secondarily generalized tonic-clonic seizures resistant to multiple drug therapy.

In the current study, a fluorometric nanoprobe based on metal–organic frameworks (MOF) was designed for the determination of lamotrigine in exhaled breath condensate (EBC). The MOF nanoprobe consisted of Tb3+ ions as metal part and dimethylformamide (DMF) and 1,10-phenanthroline (Phen) as organic parts of nanoprobe.

The used probe shows a weak fluorescence in alkaline media owing to an energy transfer from nitrogen groups of DMF and Phen on carbonyl group of DMF as an antenna for Tb3+ luminescence. However, its fluorescence is enhanced in acidic conditions by protonation of DMF nitrogen atoms and Phen and deactivation of energy transfer pathways of nitrogen groups to carbonyl group. Lamotrigine addition to this fluorescent system leads to quenching in the fluorescence intensity due to reactivation of the above mentioned energy transfer pathways resulting in competitive interaction with H+ ions. Moreover, the inner filter effect (IFE) of lamotrigine on DMF–Tb–Phen MOF NPs is considered as another reason for the observed quenching in the fluorescence of DMF–Tb–Phen MOF NPs. The intensity of the fluorescence was recorded at λem = 545 nm and the difference between fluorescence signal in the absence and presence of lamotrigine was the analytical response. The factors affected on experimental conditions were optimized utilizing a multivariate optimization technique. The validation of nanoprobe response to lamotrigine gives a linear relationship in the range of 0.05 to 2.0 µg⋅mL‒1 with a detection limit of 11.0 ng⋅mL‒1 for lamotrigine.

The developed method reveals good repeatability and selectivity for lamotrigine in real samples.

Taxane-induced pain is a disabling condition. This trial was conducted to assess the effects of melatonin on preventing paclitaxel-associated acute and chronic pain or decreasing its severity in patients with breast cancer.

This randomized, double-blind, placebo-controlled clinical trial was conducted on breast cancer women who received weekly paclitaxel (80 mg/m2) with or without trastuzumab after using doxorubicin + cyclophosphamide. The intervention group randomly received oral melatonin (10 mg/day) or placebo, which started from the first night of chemotherapy and continued through the planned 12 weeks of chemotherapy. The level of arthralgia-myalgia as acute pain was assessed every day in both groups using the Brief Pain Inventory (BPI). The Douleur Neuropathique 4 questionnaire (DN4) and National Cancer Institute Common Terminology Criteria for Adverse Events (NCI-CTCAE) version 5.0 were used to measure chemotherapy-induced peripheral neuropathy as chronic pain.

Seventeen patients were enrolled in each group randomly. The incidence of neuropathy according to a DN4 score ≥ 4 was significantly lower in the melatonin group versus the placebo group at week 12 compared to baseline (5 vs 11, P-value= 0.039). In addition, the mean neuropathy severity was significantly lower in the melatonin group over time (β= -0.051, P-value= 0.01). However, there were no significant differences in the mean worst and least pain scores over the twelve cycles of treatment between arms (P-value= 0.633 and 0.34, respectively).

Co-administration of melatonin in women with breast cancer decreased the incidence of severe paclitaxel-associated neuropathy but melatonin was not effective against acute pain.

Spirulina is an interesting nutritional supplement that has attracted a lot of attention. The aim of the present study was to examine the effect of spirulina supplementation on oxidative stress, inflammatory factors and plasma markers of exercise-induced muscle damage in male taekwondo athletes.

A total of 18 trained taekwondo male athletes took part in a double-blind, placebo-controlled crossover study. Each subject received either spirulina (8 g/day) or placebo for 3 weeks. The study had two periods separated by a 14-day washout. Blood samples were taken after finishing a training checklist program (4 times in total).

There were no significant carryover effects; therefore, the two-week washout period was adequate. Compared to the placebo, a dose of 8 g / d of spirulina supplement over 21 days resulted in a significant decrease in plasma levels of lactate dehydrogenase (LDH), creatine kinase (CK) and interleukin 6 (IL6) and a significant increase in plasma levels of total antioxidant capacity (TAC), superoxide dismutase (SOD) and glutathione peroxidase (GPX) (p<0.05). There was not any statistically significant change in the plasma malondialdehyde (MDA) (p>0.05).

Due to the improvement of antioxidant and anti-inflammatory conditions as well as appropriate protein content, spirulina supplementation can produce a preventive effect on exercise-induced muscle damage in taekwondo athletes.

Considering the potential benefits of colchicine in coronary artery diseases, we aimed to carry out the present study to assess the impact of colchicine in the prevention of myocardial injury following elective percutaneous coronary intervention (PCI).

A randomized, single-blinded, clinical trial was carried out on 102 patients undergoing elective PCI. All patients received the standard treatment prior to performing PCI. Moreover, the intervention group received 1, 0.5, 0.5 mg colchicine 12 to 18 hours before, 30-60 min before, and 12 hours after PCI, respectively. Serum concentrations of cardiac troponin I (cTnI) were measured before, 8, and 24 hours after the procedure to assess myocardial damage during PCI.

There were no significant differences in cTnI levels at baseline (P = 0.839), 8 (P = 0.729), and 24 hours (P = 0.398) after PCI between the intervention and the control groups. Likewise, no significant differences were seen regarding the mean differences of cTnI at baseline and 8 hours (P =0.190), at baseline and 24 hours (P = 0.780), and 8 and 24 hours after PCI (P = 0.680) in both groups.

The study did not support the potential benefit of colchicine in the prevention of myocardial injury following elective PCI. Conducting well-designed randomized clinical trials with adequate sample size is recommended.

Instant disintegration of oral disintegrating tablets (ODTs) provides a greater chance for buccal absorption, avoiding presystemic metabolism of nimodipine. In addition, ODT can be easily dispersed in suitable liquid before delivery via nasogastric tube in critical care setting.

Drop assisted co-grinding of nimodipine with glycine (at molar ratios 1:1, 1:2 and 1:3) or tartaric acid (at molar ratios 1:0.5, 1:1, 1:2, 1:3, and 1:4) was performed. Solid state characterization and in vitro dissolution studies were employed. The optimized formulations were employed to prepare ODTs using suitable excipients.

The prepared formulations improved drug dissolution compared to unprocessed and wet ground nimodipine. Fourier–transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffraction and scanning electron microscopy suggested transformation of the crystalline structure after co-processing. This was due to salt formation in case of tartaric acid and the formation of new crystalline species/ size reduction in case of glycine. These changes were associated with dissolution enhancement. Formulations with highest release efficiency (nimodipine and glycine with a molar ratio of 1:1 or nimodipine and tartaric acid at a molar ratio of 1:3) were successively incorporated in ODTs which showed fast liberation of nimodipine and dissolution efficiency values of 76 + 0.6% and 73.3 + 1.7% for the tablets containing glycine or tartaric acid respectively.

The study introduced a simple co-grinding approach for dissolution enhancement of nimodipine with high scaling up potential. The developed tablets will increase patient compliance with expected improved bioavailability.

New compounds called choline-based ionic liquids (ILs) that are environmentally friendly have become more attractive. In this study, some choline-based ILs (choline lactate (ChLa) and choline propionate (ChPro)) have been used to increase the aqueous solubility of lamotrigine (LTG) and piroxicam (PXM) at T = 298.15 to 313.15 K.

ILs were prepared and purified. The solubility of drugs in the aqueous ILs solutions was measured at different temperatures with shake flask method.

The solubility of the investigated drugs increased with increasing the weight fraction of ILs. The solubility data were correlated by e-NRTL, Wilson, Apelblat and λh (Buchowski) models.

The aqueous solubility of drugs depends on both the weight fraction of co-solvents and the solution temperature. These two essential parameters were analyzed through some semi-empirical and activity coefficient models getting the average relative deviation percent as e-NRTL (3.09%) < Wilson (3.92%) (for full range concentration of co-solvent) and Apelblat (3.52%) < λh (Buchowski) (5.11%) (for the dilute region of co-solvent). In addition, the results show that the aqueous solubility increases with rising temperature and there are strong interactions between the drug and the ILs.

Regardless of the availability of all novel and earlier treatments, seizure control is notoriously complicated. In the hopes of discovering the latest and ultimate therapy, medicinal chemists will keep on to hunt for new antiepileptic compounds with high specificity and low CNS toxicity. The biological effects of benzodiazepine compounds have been examined. Benzene and a diazepine ring are fused together to form the chemical structure. Diverse combinations of moieties attached to the innermost structure in positions 1, 2, 5, and 7 the pharmacological qualities, effect potency, and pharmacokinetic conditions are all influenced by the various side groups.

This paper describes the synthesis of several 1H-benzo[b][1,5]diazepin-2(3H)-one derivatives. The substituents at N1 are benzoyl, 5-substituted-1,3,4-thiadiazoles-2-yl-aminoacetyl. Condensation of orthophenylene diamine with ethyl acetoacetate gave 7-substituted-4-methyl-1H-benzo[b][1,5]diazepin-2(3H)-ones, which were then linked to benzoyl chloride and chloroacetyl chloride to yield N1-benzoyl and N1-chloroacetyl derivatives. N1- chloroacetyl derivatives were further linked with 5-substituted-1,3,4-thiadiazoles amines using microwave irradiation.

FTIR, 1H-NMR, and mass spectroscopy were used to authenticate the synthesized compounds. The PTZ produced convulsions method was used to test the compounds for anticonvulsant activity. When compared to the control group; Compounds 4a and 4c gave 80% protection at 0.4 mg/kg, whereas Compounds 2a and 2c offered 80% protection at 20 and 30 mg/kg, respectively.

When compared to a control, the experimental synthesis and pharmacological assessment of the 1,5-benzodiazepin-2-one moiety replaced with 1,3,4-thiadiazole yields a potentially active anticonvulsant drug.

Quality and quantity assurance of herbs are global concerns. This study aimed to classify and compare the monographs and test procedures of Senna parts and preparations according to two editions of BP and USP-NF. The monographs and specifications were compared to suggest a practical approach to extract relevant data.

BP 2015 and 2020, USP-NF 39-34 and 43-38, and scientific databases were used for literature review.

In both editions of USP-NF, determination of heavy metals was solely included for the powder and tablet of sennosides. In both editions of BP, assessment of microbial contamination was merely included in the monograph of dry extract of Senna, not for the rest of the monographs. Comparing two editions of BP indicated that in BP 2020, LC and HPTLC methods were added to assure the quality of pods and leaflets of Senna species.

Preparation of tabular data will assist analysts in extracting desired information and guidelines to prepare licensed herbal products. This approach could be applicable to select relevant tests according to the facilities and equipment of laboratories.