In the present study, aqueous leaf extract of Annona muricata was assessed for its capacity to mitigate testicular damages and sperm toxicity induced by gasoline fumes. Thirty‐two male Wistar rats were randomized into four groups of eight animals per group: the control group was given distilled water, and the PEBI group was exposed to petrol by inhalation and petrol‐exposed animals that were concomitantly treated with A. muricata at 100 and 200 mg kg−1 body weight (b.w), respectively (PEBI + AM100 and PEBI + AM200) via oral gavage. Oxidative stress markers, sperm quality variables and histological examination of the testes evaluated at the end of the 10‐week exposure period showed that coadministration of A. muricata significantly reduced thiobarbituric acid reactive substances (TBARS) and hydrogen peroxide (H2O2) concentration, elevated catalase (CAT) activity, diminished DNA fragmentation and improved sperm quality, thereby attenuating testicular and epididymal sperm toxicity in rats exposed to gasoline fumes. Interestingly, the higher dose A. muricata could also lower lipid peroxidation to below the control values, demonstrating the antilipoperoxidative and antioxidant protective effects of A. muricata in a gasoline fume model of testicular and spermatoxicity in rats.
This study investigated and compared the trace mineral profiles and antioxidant capacities of Polyherbal Ethanolic Extract (PHEE) and Soursop Leaf Ethanolic Extract (SLEE). Trace elements, including copper (Cu), zinc (Zn), manganese (Mn), iron (Fe), and selenium (Se), were quantified using Atomic Absorption Spectrophotometry. Antioxidant properties were assessed using DPPH, FRAP, Total Antioxidant Capacity (TAC), hydroxyl radical, and nitric oxide scavenging assays. Mineral analysis revealed higher concentrations of Cu, Mn, Fe, and Se in PHEE, while Zn was more abundant in SLEE. Both extracts exhibited significant antioxidant activities: SLEE showed stronger DPPH (IC₅₀ = 33.11 µg/mL), FRAP (IC₅₀ = 107.15 µg/mL), and nitric oxide scavenging (IC₅₀ = 54.95 µg/mL) capacities, whereas PHEE demonstrated superior TAC (IC₅₀ = 199.52 µg/mL) and hydroxyl radical scavenging activity (IC₅₀ = 53.70 µg/mL). These findings suggest that the antioxidant potentials of both extracts may be attributed to their phytochemical profiles and mineral contents, supporting their potential use in managing oxidative stress-related conditions.
Cancer is a complex global health challenge that requires novel and holistic approaches to treatment and prevention. Polyherbal medicines, composed of multiple plants with historical use in traditional medicine, have gained popularity due to their safety, cost-effectiveness, and accessibility. However, selecting the right plants and determining optimal combinations for enhanced biological effects remains challenging. To address this, a molecular docking study was conducted, targeting proteins implicated in cancer pathogenesis. The study identified bioactive compounds with strong binding energies, guiding the selection of polyherbal formulations for further experimentation. Using response surface methodology, various combinations of plant extracts were screened for their antioxidant properties and phytochemical content. Among the formulations tested, PHEE (Polyherbal Ethanolic Extract), comprising 70% soursop leaf, 5% jackfruit leaf, 5% orange peel, 15% citrus juice, and 5% apple fruit ethanolic extracts, exhibited the most potent biological activities, followed by SLEE (Soursop Leaf Ethanolic Extract), a 100% soursop leaf ethanolic extract. Design Expert Software predicted soursop leaf extract as a key contributor to desirable outcomes, attributed to its rich phytochemical composition. Cell-based assays revealed varying cytotoxic effects of the extracts on leukemia cells, with PHEE showing the highest potency (IC50 = 2.50 μg/mL), followed closely by SLEE (IC50 = 2.90 μg/mL). These effects are potentially due to the abundant acetogenins and flavonoids present in the extracts. However, caution is warranted regarding their cytotoxicity to normal cells. Apoptotic studies confirmed the ability of both PHEE and SLEE to induce programmed cell death, further supporting their potential as anticancer agents. This research underscores the importance of strategic plant combinations in polyherbal formulations and highlights PHEE as a promising candidate for further investigation in cancer treatment.
Background and Objective: Beer clarity remains a significant factor influencing consumer choice and preferences.Clarifying agents (gelatin, chill guard, isinglass, polyclar, Irish moss and activated charcoal) were deployed for clarification of produced beer and their influence on the lipid profiles of rats was investigated.The interrelationship between the consumption of study beers and obesity was also measured using physical parameters such as weight loss and gain.Materials and Methods: Sorghum beer was home-brewed using white maize and sweet potato as adjuncts while spicing with grains of selim and ginger.Seventy male Wister rats (150-170 g) were grouped into binge, moderate and mild alcohol drinkers using standard doses of administration for 21 days.Results: Filtered but not clarified beer served as the positive control group while unclarified beer served as the negative control.Beer clarified with isinglass gave the highest clarity while those of activated charcoal, Irish moss, polyclar, chill guard, gelatin and filtered beer gave lesser clarity in decreasing order.At p#0.05, significant weight gain was obtained for all groups.Clarified beers under study showed a decrease in high-density lipoprotein activity but an increase in the levels of triglyceride, total cholesterol, very low-density lipoprotein and non-high-density lipoprotein.Conclusion: This study suggested that daily consumption of beer clarified with these findings even at moderate dosages, increases bad cholesterol and the likelihood of developing obesity which potentiates the development of type 2 diabetes hypertension, coronary heart diseases and stroke.
Dichlorvos (DDVP) is an organophosphate insecticide known to cause oxidative stress, which can have a number of negative public health consequences. Harungana madagascariensis (HM), also known as dragon blood tree/amuje, is a plant with antioxidant and anti-inflammatory properties found to reduce oxidative stress in a variety of scenarios. In this study, we looked at the ability of HM stem bark extract to reduce subchronic DDVP induced oxidative stress in rats. Forty (40) Wistar albino rats were randomly assigned into polyphenylene cages Eight (8) per cage in five groups namely; control (group 1), group 2 (DDVP exposed), and treatment groups (groups 3, 4, 5 ‘DDVP exposed’ + 50 mg/kg, 100 mg/kg, 150 mg/kg extract, respectively). Male rats were treated with DDVP (10 mg/kg b.w) except for the control. Both the stressor/toxicant and extract were administered orally throughout the study duration of 28 days. At the end of the study, rats were sedated with chloroform, and blood and organ samples were collected for biochemical analysis. Biomarkers of oxidative stress, such as SOD, CAT, GPx, MDA, and NO, were meticulously evaluated in liver, kidney, and serum. Hormonal indicators, such as FSH, LH, and TES, were assessed in serum too. The result revealed that HM stem bark extract has antioxidant and anti-inflammatory properties that can protect against subchronic DDVP-induced oxidative stress. The extract also influences increased SOD, CAT, and GPx activity and decreased MDA and NO levels in DDVP exposed rats’ liver, kidney, and serum. Additionally, it decreased FSH, LH, and TES levels in DDVP-exposed rats suggesting a potential hormonal protective property. The results are indicative that HM stem bark extract has potential as a therapeutic agent for treatment of subchronic DDVP-induced oxidative stress and its related adverse health conditions. Advance studies are required to elucidate the mechanisms of action of HM stem bark extract and to determine its efficacy in human populations.
Annona muricata (soursop) leaves have been traditionally used for medicinal purposes due to its potential antioxidant, anti-inflammatory, anticancer, antimicrobial, and analgesic properties. This study quantitatively determined the phytochemical composition of soursop leaf. Using a BUCK M910 Gas Chromatography with a flame ionization detector, the analysis of phytochemicals was carried out. A 15 m x 250 0.15 RESTEK MXT-1 column was used. Helium 5.0pa.s was used as the carrier gas, flowing at a rate of 40 ml/min, with a splitless injection of 2ul of sample at a linear velocity of 30cm/s. The injector temperature was 280⁰C. At first, operating at 200⁰C, the oven was then increased to 330⁰C at a rate of 3⁰C per minute, and this temperature was maintained for 5min. An operating temperature of 320⁰C was used by the detector. The result shows that soursop ethanolic extract contains phytochemicals that belong to the broad class flavonoids (a class of polyphenolic compounds). They include naringenin (5.92 ug/ml), flavan-3 ol (5.70 mg/l), rutin (2.79 ug/ml), flavanones (3.28 ug/ml), kaempferol (6.15 ug/ml), flavone (1.99 ug/ml), proanthocyanin (2.36 ug/ml). Other polyphenols (not flavonoids) present include resveratrol (7.03 ug/ml), tannin (2.90 ug/ml), catechin (2.49 ug/ml), and epicatechin (7.67 ug/g). The alkaloids found include lunamarin (4.72 ug/ml) and spartein (2.07 ug/ml) while saponins found include sapogernin (16.07 ug/ml) and sapogenin (3.08 ug/ml). Other classes of phytochemicals found include steroids, cyanogenic glycoside, anti-nutrient, and cardiac glycosides. Soursop leaf contains bioactive compounds such as flavonoids, polyphenols, alkaloids, steroids, cyanogenic glycoside and other phytochemicals with medicinal potentials.
Background and Objective. Rice husk remains a key by-product of rice milling generated in significant amount. Accumulated evidence indicates that rice husk contains numerous bioactive compounds; however, its application is limited. This study was designed to introduce an in vivo application of rice husk extract, against opioid-induced liver and kidney injuries. Codeine was considered a psychotic inducer in this study due to its global alarming misuse recently. The hepatorenal ameliorative proclivity of rice husk extract against codeine-induced toxicity on the liver and kidney in male albino Wistar rats was examined. To this effect, thirty-six (36) albino Wistar rats of weight 100-110 g were utilized and weight-matched animals placed in 6 groups of 6 rats each. After 30 days of the combined administration of codeine and the rice husk extract, the experimental animals were assayed for basic liver and renal markers such as AST, ALP, ALT, total protein, albumin, conjugated and total bilirubin, urea, creatinine, and electrolytes (sodium, potassium, chloride, and bicarbonate). Rice husks were collected from a local rice mill, and the extraction was done with methanol. Findings. Rice husk extract (RHE) significantly ameliorated the recorded hepatic damage. More so, the extract showed a significant action on the renal markers as well. A histopathology examination of the liver and kidney tissues revealed that RHE showed a hepatorenal ameliorative potential in a dose-dependent manner. Conclusion. Phytonutrient from RH possesses a healing ability against opioid-induced hepatorenal toxicity. Thus, RH is safe for human and may be adopted to obviate and manage codeine-induced hepatorenal damage or injury. Significance and Novelty. Data on the application of RHE as a phytonutrient to combat liver and kidney injuries were demonstrated. Future studies should evaluate its potential on other organs.
Background: The Janus kinase 2-Signal Transducer and Activator of the Transcription 5 pathway (JAK2-STAT5 pathway) is a signaling pathway that plays a role in a variety of cellular processes, including cell growth, proliferation, and survival. Dysregulation of the JAK2-STAT5 pathway has been linked to several diseases, including cancer and its relapse. This study performed molecular docking simulation and Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) investigations on selected bioactive compounds against JAK2-STAT5 proteins for cancer drug discovery. Methods: JAK2 protein (Protein Data Bank (PDB) ID: 3Q32), STAT5 protein (PDB ID: 1Y1U), and 313 bioactive compounds, including standard anticancer drugs, were used for molecular docking simulation. The proteins' crystal structures were retrieved from PDB and prepared using BIOVIA Discovery Studio. The chemical structures of the compounds were retrieved from the National Center for Biotechnology Information (NCBI) PubChem database and prepared using the Open Babel and VConf software. PyRx equipped with AutoDock vina was used to perform molecular docking. The ADMET parameters for the top-performing compounds were determined using the SwissADME and pkCMS web servers. Results: The result from this study suggests that the following top-performing compounds, hypericin, withanolide, tomatidine, silymarin, baicalin, and diosmin, had the best binding energies with the potentials to serve as scaffolds or leads for new drug discovery against cancer. The ADMET study revealed that hypericin, baicalin, and diosmin violated more than one Lipinski's rule of 5 (RO5), which implies poor oral bioavailability, while withanolide, tomatidine, silymarin, ailanthone, elliptinium, ellipticine, etc. did not violate the rule which implies that they would be the best oral drug candidates based on the RO5 rules. Conclusions: The top-performing compounds, hypericin, withanolide, tomatidine, silymarin, baicalin, and diosmin, could serve as potential inhibitors/therapeutics against cancer caused by JAK2-STAT5 dysregulation.
Rice husks (RHs) is an agro waste generated from rice production with limited application. Codeine belongs to the numerous drugs of abuse worldwide and its impact on reproductive injury has been reported. This study was designed to establish the ameliorative potential of brown rice husk extract (RHE) against reproductive damage induced by codeine misuse. Experimental rats were grouped into six groups with six rats per group: Group I received only rat chow and clean water for 30 days. Group II received only codeine 10 mg/kg body weight (b.w) of rats. Group III received only RHE 500 mg/kg b.w of rats. The 4th, 5th and 6th groups received codeine 10 mg/kg/b.w alongside 250 mg, 500 mg and 1000 mg RHE, respectively. Treatments (RHE and codeine) were administered once during the early hours between 9-10 am daily for 30 days, the animals were sacrificed, and blood and tissue samples were harvested. Male reproductive hormones such as testosterone, Follicle stimulating hormone (FSH) and luteinizing hormone (LH), and sperm quality parameters were assayed. The testis tissues were excised and examined for histopathological changes. The result revealed that high dose codeine administration significantly decreased epidermal morphology, motility, and sperm count as well as testosterone, FSH, and LH concentrations, respectively. The histopathological examination revealed distinct abnormal changes in the codeine control group when compared with the other experimental groups. RHE administration significantly improved the altered assayed parameters.
Volatile organic compounds found in petrol include benzene, toluene, ethylbenzene, and xylene (BTEX). Extract of Camellia sinensis (tea plant) leaf contains some secondary metabolites such as flavonoids, alkaloids, terpenoids saponins, anthraquinones, and tannins. Polyphenols in Camellia sinensis possess anti-atherosclerosis and cardioprotective, neuroprotective, anti-inflammatory, anti-carcinogenic, antibacterial, anti-diabetic, anti-tumor, anti-hypertensive, and hepato-protective effects. The study aimed to investigate the potential of Camellia sinensis in ameliorating lung damage, oxidative stress, and inflammation caused by petrol fumes. Forty-eight Wistar albino rats weighing between 140g-230g were randomized into 8 groups of 6 rats each consisting of control, petrol fumes only group, three aqueous drink groups of different doses, and three methanol extract groups of different doses respectively. The oxido-inflammatory responses and histopathological alterations in rat lungs following 6 hours of daily exposure for 30 and 60 days were recorded. Oxidative stress (superoxide dismutase (SOD), reduced glutathione (GSH), catalase (CAT)) and inflammatory biomarkers namely: Tumor necrosis factor alpha (TNF-α), interleukin 6 (IL-6) were evaluated. The biochemical analyses showed that petrol fumes exposure resulted in significant (P<.05) increases in biomarkers of oxidative stress, pro-inflammation cytokines, and reduced GSH levels in rats as well histopathological alteration in lungs. The treated groups showed anti-oxidant properties by the elevation of antioxidant enzymes (CAT, SOD) and non-enzymatic antioxidant (gluthathione) and reduction of MDA levels as well as reversal of alterations in the lungs after histopathological analysis. This study showed that Camellia sinensis leaf aqueous and methanol extract have the potential to attenuate petrol fumes-induced oxidative stress due to its natural bioactive constituents.
Wnt/beta-catenin signaling pathway plays a role in cancer development, organogenesis, and embryogenesis. The abnormal activation promotes cancer stem cell renewal, proliferation, and differentiation. In the present study, molecular docking simulation and ADMET studies were carried out on selected bioactive compounds in search of beta-catenin protein inhibitors for drug discovery against cancer. Blind docking simulation was performed using PyRx software on Autodock Vina. beta-catenin protein (PDB ID: 1jdh) and 313 bioactive compounds (from PubChem database) with selected standard anticancer drugs were used for molecular docking. The ADMET properties of the best-performing compounds were calculated using SwissADME and pkCMS web servers. The results obtained from the molecular docking study showed that glycyrrhizic acid, solanine, polyphyllin I, crocin, hypericin, tubeimoside-1, diosmin, and rutin had the best binding interactions with beta-catenin protein based on their binding affinities. Glycyrrhizic acid and solanine had the same and lowest binding energy of -8.5 kcal/mol. This was followed by polyphyllin I with -8.4 kcal/mol, and crocin, hypericin, and tubeimoside-1 which all had a binding energy of 8.1 kcal/mol. Other top-performing compounds include diosmin and rutin with binding energy of -8.0 kcal/mol. The ADMET study revealed that the following compounds glycyrrhizic acid, solanine, polyphyllin I, crocin, hypericin, tubeimoside-1, diosmin, rutin, and baicalin all violated Lipinski's rule of 5 which implies poor oral bioavailability. However, based on the binding energy score, it was suggested that these pharmacologically active compounds are potential molecules to be tested against cancer.
AbstractThis systematic review identified various bioactive compounds which have the potential to serve as novel drugs or leads against acute myeloid leukemia. Acute myeloid leukemia (AML) is a heterogeneous hematopoietic malignancy that arises from the dysregulation of cell differentiation, proliferation, and cell death. The risk factors associated with the onset of AML include long‐term exposure to radiation and chemicals such as benzene, smoking, genetic disorders, blood disorders, advancement in age, and others. Although novel strategies to manage AML, including a refinement of the conventional chemotherapy regimens, hypomethylating agents, and molecular targeted drugs, have been developed in recent years, resistance and relapse remain the main clinical problems. In this study, three databases, PubMed/MEDLINE, ScienceDirect, and Google Scholar, were systematically searched to identify various bioactive compounds with antileukemic properties. A total of 518 articles were identified, out of which 59 were viewed as eligible for the current report. From the data extracted, over 60 bioactive compounds were identified and divided into five major groups: flavonoids, alkaloids, organosulfur compounds, terpenes, and terpenoids, and other known and emerging bioactive compounds. The mechanism of actions of the analyzed individual bioactive molecules differs remarkably and includes disrupting chromatin structure, upregulating the synthesis of certain DNA repair proteins, inducing cell cycle arrest and apoptosis, and inhibiting/regulating Hsp90 activities, DNA methyltransferase 1, and histone deacetylase 1.
This study deals with the determination of possible phytocompounds, minerals, vitamins and nutritional constituents present in Rice husk (RH). Dried rice husk samples were collected from a local rice mill at Awgu Town in Enugu, South-East Nigeria. The proximate, phytochemical, vitamin and mineral composition of the ground sample were investigated using standard methods of analysis, while a Gas chromatography-mass spectrometry (GC-MS) device was employed for the characterization of bioactive components of the sample. The proximate analysis revealed the presence of carbohydrate (37.04%), crude protein (1.85%), moisture (7.93%), crude fat (3.76%), fibre (25.74%), and ash content (23.39%). The phytochemical screening high amount of flavonoids, carotenoid, and glycosides in the RH sample. Vitamins such as A, C, D, E, K and B complexes (B1, B2, B3, B5, B6, B7, B9, and B12) as well as minerals (calcium, magnesium, potassium, sodium, zinc, iron, selenium, cobalt, manganese, copper and phosphorus) were also identified in the sample. Meanwhile, the GC-MS analysis of the sample revealed the presence of cynarin, demecolcine, penta-triacontene, hyoscyamine, kheltin, acetyldigoxin, quinoline-3- methyl, coumaric acid, copaene, benzyl benzoate, caryophyllene, danthron, lupenon, beta-amyrin, ephedrine, alpha-ergosterol, galanthamine, kawain, agrimophol, eugenol, anabasine, benzylisoquinoline, carpaine, phytol, phytic acid, myrcene, lobeline, beta-caryophyllene, sparteine, and emetine. This study established that the high nutritional value and bioactive composition of rice husk indicates the rice milling by-product to be a promising food formulate with numerous health benefits.
Oryza sativa (rice) is a widely consumed staple grain with significant amount of fibre, carbohydrate, and trace amount of other biomolecules such as minerals and vitamins. Thus, it’s a good energy source. The pre-clinical and clinical investigations of rice hull has revealed its numerous health benefits. Utilization of rice products as dietary supplements, additives and pharmacological adjuvants has become a global trend. Rice husk (RH), is a by-product of rice milling generated in tremendous quantity. Considering the global trend in codeine consumption especially by the youths, this study adopted codeine as a drug of abuse as against its therapeutic use as an analgesic. The study explored the haematopoietic potential of rice husk methanol extract (RHME) in codeine-administered male Wistar rats. A total of thirty-six (36) rats weighing between 100-110g were procured and assembled into 6 groups of 6 rats. Group I was the negative control (NC), Group II received codeine at 10mg/kg body weight, Group III received 10mg/kg body weight of RHME, while Groups IV, V, and VI received codeine with RHME concurrently but at three different concentrations of 250, 500, and 1000mg/kg respectively. After 30 days of treatment, blood samples of the specimens were subjected to haematological assay. From the assessment, codeine administration significantly decreased the haematological indices (PCV, haemoglobin, RBC, WBC, platelets, neutrophil, eosinophil, lymphocyte and monocyte), while RHME administration significantly upregulated the altered blood parameters concentration. Thus, RH showed haematopoietic efficacy and should be considered a possible therapeutic for prevention and/or management of anaemia as well as boosting of key haematology indices.
Clinical studies have shown the benefits that plant products can offer to health by recognizing the specific nutrients and chemicals in the plants linked with these benefits hence the bioactive and nutritional composition of Camellia sinensis leaves were evaluated in this study. The result of the phytochemical content of the aqueous extract and methanol extract showed the presence of flavonoids, alkaloids, steroids, other phenolic compounds and anti-nutrients. Only the aqueous extract had tannins as part of its composition.The proximate analysis showed that fibre had the lowest concentration and carbohydrate had the highest concentration. The most abundant vitamin and element are vitamin C and potassium respectively. The most abundant essential and non-essential amino acids are threonine and arginine respectively. The limiting amino acid is tryptophan. Camellia sinensis can be explored to be both a food and a medicinal plant.
Toxicological indices of wistar rats fed formulated chaw of Telfairia occidentalis planted on crude oil contaminated and bioremediated soil was studied. Farmland, measuring 18 m2 was divided into three lots of 4 m2 and 2 m space was allowed between each lot (A, B and C). Two lots were polluted, subjected to 16 weeks of bioremediation and viable seeds of T. occidentalis were planted and grown for 28 days. The harvested vegetable leaves were analyzed. Leaves from natural attenuated soil showed high concentration of both aliphatic and polycyclic aromatic hydrocarbons with values of 9.34+0.03 mg/kg and 9.18+0.05 mg/kg for C36 and Fluoranthene respectively, while the bioaugmented soil had Lead as the highest heavy metal with a value of 0.10+0.02 g/100g. Four groups, of 9 rats each (totalling 36 rats) of adult males and females, wealing males and females were subsequently sub-grouped into 3 and allowed to acclimatize for a period of 1 week. These animals were fed formulated rat chaw of 50% dry weight of T. occidentalis, from the three lots (control, bioaugmented and natural attenuated soil) for a period of 28 days. Assay of animals’ toxicological index showed elevated concentrations of alkaline phosphatase, alanine and aspartate aminotransferases, urea and creatinine in their sera. A slight increase in serum amylase activity was recorded, while concentrations of their haemoglobin and Packed Cell Volume (PCV) reduced. The obtained results from these biomarkers were confirmed by the histopathological sections of the animal organs.
Doxorubicin is an effective and still-used antineoplastic agent. However, the clinical use of doxorubicin is marred by life-threatening cardiotoxicity and nephrotoxicity. Free radicals have been implicated in the toxicity of doxorubicin. The aim of this study was to determine the phytochemical contents and protective effects of methanol extract of Ficus sur (MEFS) in doxorubicin-induced oxidative damage in Wistar albino rats, using biomarkers of cardiac, renal functions and oxidative stress as indicators. Phytochemical analyses revealed that MEFS is rich in tannins, alkaloid, saponins, flavonoids, but low in steroids. Acute toxicity studies show that MEFS was non-toxic up to 5000mg/kg b.w of Wistar rats. Administration of doxorubicin led to a significant (P< 0.05) increase in Creatine kinase (CK-MB), troponin, creatinine, urea and MDA concentrations. Sodium and potassium concentrations were not significantly (P>0.05) affected. Cardiac and renal superoxide dismutase (SOD), catalase and glutathione (GSH) were also significantly reduced. Results also show that pre-administration of MEFS was cardio- and nephroprotective in doxorubicin oxidative damage as evidenced by significant (P<0.05) reduction of elevated troponin, CK-MB, creatinine and urea concentrations. Concentrations of renal and cardiac SOD, catalase and GSH were also significantly (p<0.05) increased by MEFS compared to doxorubicin-treated group. Cardiac and renal MDA concentrations were significantly reduced. It may be concluded that protective effects of MEFS on doxorubicin toxicity may be due to the antioxidant properties of MEFS.
This study investigated the effect of aqueous extract of the aerial parts of Leonurus cardiaca on cisplatin-induced hepato-renal damage in male Wistar albino rats. Sixty male wistar albino rats weighing between 180 and 220g were used for this study. The rats were grouped into 12 groups, five rats per group. Group 1 served as normal control, group 2 received 5mg/kg weight of cisplatin, serving as negative control while group 3 received 5mg/kg b.w of cisplatin and treated with 25mg/kg weight of hydrochlorothiazide and served as positive control. Group 4-12 rats were cisplatin-induced cardiovascular damage treated with Leonurus cardiaca extract at 166, 250, and 500mg/kg for 7, 14, and 21 days. Biochemical assays were determined using standard methods and procedures. The Na+, Cl-, HCO3-, creatinine, and urea levels of kidney homogenate of group 7 treated rats with the extract at 250mg/kg b.w for 7 days were 123.05±0.01mmol/l, 1.07±0.01mmol/l, 27.27±0.01mmol/l, 13.63±0.01mmol/l, 0.68±0.02mmol/l, and 1.14±0.01mmol/l respectively and were significantly increased when compared to the negative and normal control groups. Similar increases occurred for 14 and 21 days treatments. The kidney homogenate Na+, Cl-, HCO3, creatinine, and urea of group 7 treated rats with the extract at 500mg/kg b.w for 7 days were 158.05±0.01mmol/l, 3.03±0.01mmol/l, 31.13±0.01mmol/l, 19.46±0.01mmol/l, 2.06±0.00mmol/l, and 2.03±0.01mmol/l respectively. Values were significantly increased (p<0.05) in comparison to the normal and negative control groups. Similar increases were observed for 14 and 21 days treatments. The plasma ALT, ALP, and AST activities were 187.35±0.00U/L, 98.03±0.01U/L, 185.64±40.81U/L respectively, were significantly decreased (p<0.05) in comparison to negative control treated with the extract at 250mg/kg b.w for 14 days. The plasma ALT, ALP, and AST activities of group 10 rats treated with the extract at 500mg/kg b.w for 7 days were 164.24±0.01U/L, 87.02±0.01U/L, and 183.74±0.01U/L respectively and were significantly decreased (p<0.05) in comparison to negative control. The hepato-renal curative potential of Leonurus cardiaca could be attributed in part to its ability in enhancing liver and kidney regeneration.
Over 30-35% of patients down with AML are caused by mutations of FLT3-ITD and FLT3-TKD which keeps the protein activated while it activates other signaling proteins downstream that are involved in cell proliferation, differentiation, and survival. As drug targets, many inhibitors are already in clinical practice. Unfortunately, the average overall survival rate for patients on medication suffering from AML is 5 years despite the huge efforts in this field. To perform docking simulation and ADMET studies on selected phytochemicals against FLT3 protein receptor for drug discovery against FLT3 induced AML, molecular docking simulation was performed using human FLT3 protein target (PDB ID: 6JQR) and 313 phytochemicals with standard anticancer drugs (Sorafenib and Gilteritinib in addition to other anticancer drugs). The crystal structure of the protein was downloaded from the protein data bank and prepared using Biovia Discovery Studio. The chemical structures of the phytochemicals were downloaded from the NCBI PubChem database and prepared using Open Babel and VConf softwares. Molecular docking was performed using PyRx on Autodock Vina. The ADMET properties of the best performing compounds were calculated using SwissADME and pkCMS web servers. The results obtained showed that glabridin, ellipticine and derivatives (elliptinium and 9-methoxyellipticine), mezerein, ursolic acid, formononetin, cycloartocarpesin, hypericin, silymarin, and indirubin are the best performing compounds better than sorafenib and gilteritinib based on their binding affinities. The top-performing compounds which had better binding and ADMET properties than sorafenib and gilteritinib could serve as scaffolds or leads for new drug discovery against FLT3 induced AML.