The effects of Garcinia kola and curcumin on the dorsal root ganglion of the diabetic rat after peripheral nerve transection injury.

OBJECTIVE: To test the protective effects of Garcinia kola and curcumin on the ganglion tissues of diabetic rats following the use of autologous vein graft in peripheral nerve transection injury. METHODS: The sciatic nerve on the right side was transected, and anastomosis was performed between the proximal and distal ends using an autologous vein graft. Curcumin and Garcinia kola seed extract were administered daily by oral gavage. The ganglion tissues were harvested after a 90-day waiting period. Sensory neurons in the dorsal root ganglion at the L4 and L5 levels were used for stereological evaluations. Mean sensory neuron numbers were analyzed using a stereological technique. The size of the light and dark neurons was also estimated, and ultrastructural and immunohistochemical evaluations were performed. RESULTS: A statistically significant difference in sensory neuron numbers was observed between the groups with and without Garcinia kola and curcumin applications. The immunohistochemical results showed that the s-100 protein is expressed selectively between cell types. CONCLUSION: The results of this study show that curcumin and Garicinia kola prevented sensory neuron loss in diabetic rats following transection injury to the sciatic nerve.

Efficient Cr(VI) sequestration from aqueous solution by chemically modified Garcinia kola hull particles: characterization, isotherm, kinetic, and thermodynamic studies.

There is a need for the removal of hexavalent chromium from contaminated water prior to its discharge into the environment, as part of industrial effluents, due to its toxic nature. In this present study, an adsorbent prepared via chemical modification of Garcinia kola hull particles (GK-HP) using NaOH was applied for Cr(VI) sequestration from aqueous solution. Both the raw (rGK-HP) and chemically modified Garcinia kola hull particles (cMGK-HP) were characterized using BET, SEM, XRD, FTIR, TGA, and EDS. The effects of pH, contact time, adsorbent dose, adsorbate initial concentration, and temperature on Cr(VI) sequestration were examined. The adsorbent, cMGK-HP, proved to be more effective for the adsorption process than rGK-HP with 96.25% removal efficiency at a pH of 2, a contact time of 60 min, an adsorbent dose of 5 g/L, Cr(VI) initial concentration of 20 mg/L and a temperature of 40°C. Isotherm and kinetic studies showed experimental data to be well-fitted with Langmuir isotherm and follow the pseudo-second-order kinetic model. The thermodynamic study revealed adsorption nature to be feasible, occur via physisorption, spontaneous, and exothermic. Changes in morphological structure, textural property, spectral peak, phase composition, and chemical composition of adsorbents before and after Cr(VI) sequestration from solution were proved by SEM, BET, FTIR, XRD, and EDS analyses, respectively. cMGK-HP possessed excellent reusability attribute and high thermal stability as shown by TGA. In conclusion, the adsorption capacity of cMGK-HP is better than many other adsorbents generated from agrowastes used in previous studies for Cr(VI) removal.

Molecular docking, pharmacophore modelling, MD simulation and in silico ADMET study reveals bitter cola constituents as potential inhibitors of SARS-CoV-2 main protease and RNA dependent-RNA polymerase.

A mini survey was employed in the search of herbs and spices which people believe could prevent them from contracting COVID-19. Phytochemicals which have been earlier implicated for the bioactivity of the afore-mentioned herbs and spices were identified through literature search. The phytochemicals were then subjected to pharmacore modelling, molecular docking and molecular dynamics simulation in order to identify phytochemicals that could serve as inhibitors of 3-Chymotryprin-like protease and RNA dependent-RNA polymerase of SARS-CoV-2. The drug-likeness and toxicity profile of the phytochemicals were afterwards predicted via ADMET studies. The mini survey showed ginger, garlic, bitter cola, as the lead-herbs which could find application in anti- COVID-19 therapy. Literature search revealed 27 phytochemicals were implicated for bioactivity of these herbs. Of these 27 phytoconstituents that were docked with 3-chymotrypsin-like protease and RNA dependent-RNA polymerase, the constituents of bitter cola had lower docking scores than other phytochemicals. MD simulation results showed that Garcinia biflavonoid I displayed less comformational changes and the better binding free energy. Also, the garcinia biflavonoids had relatively safe ADMET predictions. Hence, Garcinia biflavonoids and some other constituents of bitter cola could be further modified so as to obtain safe pharmaceutical intervention for the COVID-19 challenge.Communicated by Ramaswamy H. Sarma.

Ninety-day oral toxicological profiling of Kolaviron (an extract of Garcinia kola) in male and female rats.

There remains an insufficiency of data on the long-term toxicological profile of Garcinia kola Heckel and its extract, Kolaviron (KV), despite several studies on its pharmacological effects. This research was designed to investigate the long-term histopathological, hematological, biochemical, hormonal, reproductive, and oxidative effects of 90 days administration of KV to male and female rats, as well as additional 30 days reversibility study to assess the potential for reversal of induced effects. Fifty-six male and female Wistar rats divided into four groups were treated orally with distilled water/propylene glycol, 20 mg/kg KV, 100 mg/kg KV, and 500 mg/kg KV for 90 days. At the end of 90 days and 30 additional days of reversibility study, 5 ml blood was collected from animals for relevant analyses. Vital organs were harvested for histopathological assessments. In this study, KV did not elicit any adverse effect on histopathological presentations of vital organs which were generally non-abnormal. There was significant increase (p < 0.05) in LEU, MON, EOS%, BAS%, HCT (male animals) and LYM%, EOS%, BAS%, RBC, hemoglobin and MCH (female animals). There was significant diminution (p < 0.05) in cholesterol, triglycerides, LDL, and VLDL levels, with significant increase (p < 0.05) in HDL level in both male and female animals. KV elicited a non-significant increase in sperm count accompanied by a significant increase (p < 0.05) in levels of Follicle stimulating hormone (FSH) and testosterone in male rats. Furthermore, KV elicited significant (p < 0.001-0.05) elevation in the levels of GSH, SOD and CAT, and diminution in the level of MDA. The findings in this study suggest that long-term administration of KV is considerably safe with some variations in response between male and female animals. The possible sustenance of observed effects after cessation of KV administration, lipid lowering, erythropoiesis inducing, and immune system boosting activities of KV were confirmed in this study.

Effects of Combined Garcinia kola and Kigelia africana on Insulin and Paraoxonase 1 (PON1) Levels in Type 2 Diabetic Rats.

BACKGROUND: Individual extracts of Garcinia kola and Kigelia africana have been shown to have therapeutic effects against a variety of variables linked to the development of diabetes mellitus. However, there is still a lack of information about the combined effects of these extracts on Insulin and Paraoxonase 1 (PON-1) in Streptozotocin-Nicotinamide-induced type-2 diabetic Wistar rats. METHODS: Forty-two young male rats (180-200g) were randomly divided into six groups (n = 7/group). Diabetes was intraperitoneally induced with 110 mg/kg of nicotinamide constituted in distilled water and fifteen minutes later with 65 mg/kg of streptozocin freshly prepared in 0.1M citrate buffer (pH of 4.5) and treated for six weeks as follows: the control rats received either 0.9% normal saline (NS) or 250 mg/kg extract by gavage. The remaining animals were diabetes induced and subsequently treated with either NS, graded doses of the extract (250 mg/kg and 500 mg/kg), or 5 mg/kg Glibenclamide + 100mg/kg Metformin. Gas chromatography-mass spectrometry (GCMS) of the combined extracts was also analyzed to identify the bioactive compounds present in it. Insulin, PON-1 levels, lipid profiles, and atherogenic index were assessed. RESULTS: Our findings show that Insulin and PON-1 levels in the plasma of diabetic rats treated with the combined extracts were significantly increased when compared to the control rats. Moreover, the GCMS of the extract shows the presence of both monounsaturated (oleic acid) and polyunsaturated (linoleic acid) fatty acids. CONCLUSION: The current findings suggest that the extract may help improve glucose homeostasis and prevent atherosclerosis through the established mechanism of the identified bioactive compounds.

Kolaviron, a flavonoid-rich extract ameliorates busulfan-induced chemo-brain and testicular damage in male rats through inhibition of oxidative stress, inflammatory, and apoptotic pathways.

Previous reports revealed that increased oxidative stress with up-regulated inflammatory proteins and apoptotic factors have serious implications in busulfan-induced chemo-brain and testicular damages. Hence, we investigated the potential reversal effects of kolaviron (KV), a neuro-active extract rich in flavonoids with proven anti-oxido-inflammatory and anti-apoptotic properties, on busulfan-induced oxidative damage, inflammatory proteins, and apoptosis in the brains and testes of male rats. In the treatment-regimen, animals in groups 1 and 2 had saline (10 ml/kg/p.o./day) and dimethyl sulfoxide (DMSO; 10 ml/kg/p.o./day), group 3 received KV extract (200 mg/kg/p.o./day), group 4 was given busulfan (50 mg/kg/p.o./day) and animals in group 5 were pretreated with busulfan (50 mg/kg/p.o./day) successively for 56 days in addition to KV extract (200 mg/kg/p.o./day) from days 29-56. Non-spatial memory function was valuated with a novel-object recognition memory test. Thereafter, testicular and brain oxidative/antioxidant status, proinflammatory- and apoptotic-related proteins, testicular enzymatic markers were evaluated respectively. Kolaviron extract improved cognitive function by increasing exploration of novel-object of busulfan-treated rats. Kolaviron extract reversed busulfan-mediated increased malondialdehyde, 8-hydroxy-2'-deoxyguanosine, and decreased superoxide dismutase, catalase, glutathione, and glutathione-peroxidase in brains and testes as well as the testicular enzyme markers. Increased brain and testicular weights, and TNF-α, IL-1ß, and NF-κß productions due to busulfan administration were also reduced by the extract. The reduced testicular B-cell lymphoma-2, sperm mitochondrial cytochrome-C, and membrane potential, increased DNA fragmentation, caspases -3 and -9 levels were also profoundly reversed by KV. Additionally, KV extract ameliorated busulfan-induced testicular histopathological changes in rats. Conclusively, KV extract reverses busulfan-induced neuroendopathobiological derangements via oxidative stress inhibition, down-regulation of inflammatory and apoptotic mediators in rats' brains and testes. PRACTICAL APPLICATIONS: Busulfan is an orally effective chemotherapy drug widely used for cancer treatment. It has been reported that chronic usage of busulfan increases the tendency for carcinogenic and teratogenic activities with severe side effects on the functions of the gonads and other body organs such as brain, popularly regarded as chemo-brain. When taken over a prolonged period of time, busulfan causes sterility in animals and destroyed spermatogonial stem cells along with the seminiferous tubules and sperm morphology of animals as well as memory impairments. The findings from the study revealed that KV extract prevent busulfan-induced cognitive and testicular impairments following kolaviron supplementation. Thus, the findings from this scientific investigation suggest that KV extract could improve the quality of reproductive life and cognitive functions of male patients during busulfan chemotherapy, particularly during prolonged therapy.

The effects of Gum Arabic, curcumin (Curcuma longa) and Garcinia kola on the rat hippocampus after electromagnetic field exposure: A stereological and histological study.

The present study was designed to focus on the potential effects of the electromagnetic field (EMF) emitted by mobile phones on hippocampal pyramidal neurons and to investigate the role of curcumin (Cur), Garcinia kola (GK) and Gum Arabic (GA) in reducing these adverse effects. Fifty-four 12-week-old male Wistar albino rats were used. These were randomly divided into nine groups of six rats each. The control, Cur, GK and GA groups were not exposed to EMF, while the sham group was kept in the EMF exposure system without being exposed to EMF. The EMF+Cur, EMF+GK, EMF+GA and EMF groups were exposed to 900 MHz EMF for one hour a day for 28 days. The number of the pyramidal neurons in the cornu ammonis (CA) of the hippocampus was estimated using the optical fractionator technique. Histopathological changes were evaluated under light and electron microscopes. The activities of the superoxide dismutase (SOD) and catalase (CAT) enzymes were also evaluated from serum samples. Significant levels of CAT and SOD activities were observed in the EMF group compared to the control group (p = 0.000; p = 0.001) respectively. Microscopic observations showed that dark-coloured nuclei with unclear neuron boundaries were frequently observed in the EMF group. Stereological data analysis revealed a significant decrease in the CA's total number of pyramidal neurons in the EMF group compared to the control and sham groups (p = 0.000; p = 0.000) respectively. Cur and GK were observed to provide significant protection in the EMF+Cur and EMF+GK groups compared to the EMF group (p = 0.000; p = 0.000) respectively. No significant difference was observed between the EMF+GA group and EMF group (p = 0.989). Exposure to 900 MHz EMF causes severe alterations in the number and structure of hippocampal pyramidal neurons. Cur and GK exhibit a protective effect against these deleterious effects, but GA showed no protective effect.

A review on garcinia kola heckel: traditional uses, phytochemistry, pharmacological activities, and toxicology.

PURPOSE: Garcinia kola is a medicinal plant commonly known as bitter kola. It is utilised in ethnomedicine for the treatment of diarrhoea, bronchitis, bacterial infection, cough, hepatitis, gonorrhoea, laryngitis, food poison, liver and gastric diseases. OBJECTIVE: This study reviewed the phytochemistry, pharmacological activities, and ethnomedicinal potentials of G. kola. MATERIALS AND METHODS: An extensive review was performed using electronic literature collated from ScienceDirect, Springer, Wiley, and PubMed databases. RESULTS: Phytochemical analysis revealed the isolation of several chemical compounds including 9-octadecenoic acid, linoleic acid, 14-methylpentadecanoic acid, 1-butanol, hexadecanamide, I-4',II-4',I-5,II-5,I-7,II-7-hexahydroxy-I-3,II-8-biflavanone, lanost-7-en-3-one, kolaflavanone (8E)-4-geranyl-3,5-dihydroxybenzophenone, glutinol, Garcinia biflavonoid (GB-2a-II-4'-OMe), 9,19-cyclolanost-24-en-3-ol, 24-methylene, tirucallol, lupeol, ß-amyrin, obtusifoliol and Kolaviron. Diverse pharmacological in-vivo and in vitro investigations revealed that G. kola has anti-inflammatory, antimalarial, hepatoprotective, cardioprotective, anti-asthmatic, neuroprotective, antioxidant, and antidiabetic activities. CONCLUSION: The present study revealed that G. kola has preventive and therapeutic potentials against various diseases in both in vivo and in vitro studies and therefore can be utilised as a raw material in the pharmaceutical industries for the development of therapeutic products. However, there is a need for clinical trial experiments to validate and provide accurate and substantial information on the required safe dosage and efficacy for the treatment of several diseases.

Ameliorative effects of hexane extract of Garcinia kola seeds Heckel (Clusiaceae) in cisplatin-induced hepatorenal toxicity in mice.

Garcinia kola seed is used to manage liver diseases in ethnomedicine. However, there is limited information on its role in Cisplatin (CIS)-induced toxicity. Here, we investigated the potential of hexane extract of Garcinia kola (HEGK) in lessening CIS-induced hepatorenal- and gene- toxicity. Male mice (22 ± 3 g) randomly assigned into groups (n = 5) were treated for five days: Corn oil only, HEGK (200 mg/kg), CIS (20 mg/kg; i.p; 48-hours), CIS + HEGK (100 mg/kg), CIS + HEGK (200 mg/kg), CIS + Quercetin (25 mg/kg), and Quercetin(25 mg/kg). Corn oil, HEGK, and Quercetin were administered daily by gavage. GC-MS revealed the presence of 9,19-Cyclolanost-24-en-3-ol as the most abundant component in HEGK, with an LC50 of 1023 µg/mL. HEGK significantly (p < 0.05) scavenged DPPH, inhibited lipid peroxidation and exhibited reducing activity dose-dependently. CIS treatment increased (p < 0.05) urinary albumin and creatinine by 18 and 56%, respectively, serum levels of total bilirubin, creatinine, and hepatic transaminases, while albumin decreased (p < 0.05) by 57%. CIS treatment increased renal and hepatic malondialdehyde (MDA) levels by 67 and 70% individually, while the activities of glutathione peroxidase (GPx), superoxide dismutase (SOD), catalase (CAT) and reduced glutathione (GSH) levels were decreased (p < 0.05). Furthermore CIS-induced the formation of mononucleated polychromatic erythrocytes (mnPCEs) 150% in the bone marrow of mice. Histology revealed necrosis of hepatocytes, congestion of renal interstitial vessel, and hyperplasia of the Kupffer cells. Pretreatment with HEGK reduced the levels of MDA, mnPCEs, and increased the activities of antioxidant enzymes and restored GSH to levels comparable in control mice. Taken together, HEGK ameliorated CIS-toxicity via the activation of the antioxidative pathways and mitigated genotoxicity by mitigating mnPCEs formation in mice.

Aqueous Extract of Cola nitida and Garcinia kola Synergistically Enhances Hippocampal-hypothalamic Glutamate and Na+ /K+ -ATPase Activity in Male Wistar Rats.

BACKGROUND: The incidence of cognitive decline has been proposed to rise exponentially in the coming years. Therapies targeting molecular pathways involved in the enhancement of memory and energy regulation could be a major breakthrough in the prevention or management of dementia in susceptible populations. OBJECTIVES: This study investigated the effects of aqueous extracts of Cola nitida (AECONS) and Garcinia kola (AEGAK) on glutamate level and Na+/K+-ATPase activity in the hippocampus and hypothalamus of male Wistar rats. METHODS: Adult male Wistar rats (170-200) were randomly allotted into groups (n=5/group); control (distilled water p.o.), AECONS1 (200 mg/kg), AECONS2 (400 mg/kg), AEGAK1 (200 mg/kg), AEGAK2 (400 mg/kg), AECONS1+AEGAK1 and AECONS2+AEGAK2. The extract was prepared and the administration was done daily for 6 weeks. RESULTS AND DISCUSSION: Administration of AECONS or AEGAK increased plasma, hippocampal and hypothalamic glutamate, Na+/K+-ATPase activity, NO, SOD except hippocampal glutamate in AECONS1/AEGAK1, Na+/K+-ATPase activity and SOD in AEGAK1, hypothalamic glutamate and SOD in AECONS1 when compared with control. Besides, MDA level decreased in AEGAK2 and hippocampal but not hypothalamic MDA decreased in AEGAK1 compared with control. However, concomitant administration of AECONS and AEGAK enhanced plasma, hippocampal and hypothalamic biomarkers except hypothalamic MDA level. The present study demonstrates that AECONS and AEGAK synergistically enhance hippocampal and hypothalamic glutamate and Na+/K+- ATPase activity, which are accompanied by NO and SOD-dependent antioxidant enrichment. CONCLUSION: These findings, therefore, suggest that AECONS+AEGAK could be a better therapeutic candidate in hippocampal-hypothalamic-related neurodegenerative diseases.

Comparative influence of kolaviron and coenzyme Q10 on complex I activity, glutamate clearance, 3,4-dihydroxyphenethylamine metabolism, and redox stress in rotenone-induced neurotoxicity.

3,4-dihydroxyphenethylamine (dopamine) depletion, inhibition of complex I activity, oxidative stress, and glutamate excitotoxicity are cardinal biochemical features of neurotoxicity induced by systemic unilateral infusion of rotenone. Kolaviron (KV), a biflavonoid from Garcinia kola seeds, has been proven to have pharmacological effects against neurotoxicity. Coenzyme Q10 plays an essential role in mitochondrial oxidative phosphorylation and as an antioxidant. This study examined the comparative influence of kolaviron and coenzyme Q10 on complex I activity, dopamine metabolism, glutamate clearance, and redox stress in rotenone-induced neurotoxicity in the cortex, hippocampus, and striatum of the brain of rats. Adult Male Wistar rats were pretreated with 200 mg/kg KV or 100 mg/kg coenzyme Q10 for 7 days followed by administration of a progressive six doses of 1.5 mg/kg rotenone within the next 48 h after which the animals were euthanized and the brain excised. On the cortical, hippocampal, and striatal regions of the brain, complex I activity, dopamine metabolism, oxidative stress markers, as well as glutamate metabolism were carried out and analyzed. In all brain regions examined, KV and coenzyme Q10 pretreatment modulated complex I activity, ameliorated redox imbalance, and enhanced dopamine metabolism via increasing the activity of tyrosine hydroxylase and decreasing monoamine oxidase activity. KV facilitated glutamate clearance through augmentation of glutamate dehydrogenase and glutamine synthetase activities.  The activity of KV was comparable to that of the mitochondrial membrane antioxidant compound, coenzyme Q10, this indicates that KV is a promising therapeutic agent in the treatment of Parkinson's disease and its activity compares well with coenzyme Q10.

Bitter kola and kola nut use and their effect on treatment outcome on People Living with HIV at a Military Hospital in Benue state Nigeria: Bitter kola (Garcinia) and Cola nut (Cola nitida among PLWHIV

Introduction Bitter Kola (Garcinia Kola) and kola nut, contains substances attributed to numerous effects on humans including anti-inflammatory, anti-allergic properties, anti-infective and caffeinism. This study explores Bitter kola and kola nut use and its impact on treatment outcome on People Living with HIV (PLWHIV). Methods: The study was conducted at a Military Hospital in Nigeria. An analytical cross-sectional study was done using questionnaire among 700 HIV-positive clients selected using simple random sampling. Data were collected by researcher and three trained assistants. Chi-square test and binary logistic regression were used for identifying associations and predictors, respectively. The level of significance was set at p < 0.05. Results: Findings show that 260 (63.6%) and 179 (25.6%) have ever and currently used Bitter kola/Kola nut, respectively. Also, 14 (7.8%) used Bitter kola/Kola nut alone while 165 (92.2%) used it in addition to other substances, especially with alcohol 123 (68.7%). Bitter kola use was associated with age (p = 0.037), gender (p < 0.001), occupation (p = 0.001), and number of children (p < 0.011). Identified predictors were being a female (AOR 0.79; 95% CI 0.08-0.92) and earning <18,000 Naira (AOR 2.91; 95% CI 2.03-21.54). There was no association of Bitter kola/kola nut use with CD4 count and viral load suppression. Conclusion: Though Kola nut and Bitter kola use was high as in the general population we have not found any effect on treatment outcome among PLWHIV. This calls for more research to ascertain if there are other possible beneficial effects on PLWHIV.

Garcinia kola and garcinoic acid suppress SARS-CoV-2 spike glycoprotein S1-induced hyper-inflammation in human PBMCs through inhibition of NF-κB activation.

Symptoms and complications associated with severe SARS-CoV-2 infection such as acute respiratory distress syndrome (ARDS) and organ damage have been linked to SARS-CoV-2 spike protein S1-induced increased production of pro-inflammatory cytokines by immune cells. In this study, the effects of an extract of Garcinia kola seeds and garcinoic acid were investigated in SARS-CoV-2 spike protein S1-stimulated human PBMCs. Results of ELISA experiments revealed that Garcinia kola extract (6.25, 12.5, and 25 µg/ml) and garcinoic acid (1.25, 2.5, and 5 µM) significantly reduced SARS-CoV-2 spike protein S1-induced secretion of TNFα, IL-6, IL-1ß, and IL-8 in PBMCs. In-cell western assays showed that pre-treatment with Garcinia kola extract and garcinoic acid reduced expressions of both phospho-p65 and phospho-IκBα proteins, as well as NF-κB DNA binding capacity and NF-κB-driven luciferase expression following stimulation of PBMCs with spike protein S1. Furthermore, pre-treatment of PBMCs with Garcinia kola extract prior to stimulation with SARS-CoV-2 spike protein S1 resulted in reduced damage to adjacent A549 lung epithelial cells. These results suggest that the seed of Garcinia kola and garcinoic acid are natural products which may possess pharmacological/therapeutic benefits in reducing cytokine storm in severe SARS-CoV-2 and other coronavirus infections.

Kolaviron abates busulfan-induced episodic memory deficit and testicular dysfunction in rats: The implications for neuroendopathobiological changes during chemotherapy.

Busulfan is a popular antileukemia chemotherapeutic alkylating agent widely known to induce variety of serious adverse effects including chemobrain-related cognitive impairments and dysfunction in male reproductive system. Whether kolaviron, a neuro- and repro-active compound obtained from Garcinia kola, with neuroprotective and reproductive-promoting activities, mitigates busulfan-induced cognitive and male reproductive impairments remain unknown. Hence, we investigated the reversal effects of kolaviron on busulfan-induced episodic memory deficit and testicular dysfunction, and its underlying mechanisms in male rats. In the treatment-protocol, rats in groups 1 and 2 received saline (10 mL/kg/p.o./day) and DMSO (10 mL/kg/p.o./day) respectively, group 3 was given kolaviron (200 mg/kg/p.o./day), group 4 received busulfan (50 mg/kg/p.o./day) and group 5 was pretreated with busulfan (50 mg/kg/p.o./day) consecutively for 56 days prior to kolaviron treatment (200 mg/kg/p.o./day) from days 29-56. Episodic memory deficit was assessed using passive avoidance task (PAT). Following euthanization, blood samples, epididymal sperm, testes and brain were harvested and hormonal and neurochemical contents and their metabolizing enzymes were assayed. Kolaviron reversed busulfan-induced episodic cognitive deficit in the PAT. The reduced serotonin, dopamine, noradrenaline concentrations, elevated glutamate levels, acetylcholinesterase, monoamine oxidase-A and B activities were normalized by kolaviron. Kolaviron also reversed the busulfan-induced decreased testicular/body weights and spermatogenesis. Kolaviron abated busulfan-induced changes in androgenic hormones (testosterone, FSH, LH), dehydrogenase enzymes (3ß-HSD and 17ß-HSD), altered sperm-chromatin, sperm-membrane integrity and sperm-acrosomal reaction and capacitation impairments. Our findings suggest that kolaviron could mitigate busulfan-induced episodic memory deficit and dysfunction in male reproductive system via neurochemical modulations and increase testicular androgenic hormones/enzymes in rats.

Exploring the potentials of some compounds from Garcinia kola seeds towards identification of novel PDE-5 inhibitors in erectile dysfunction therapy.

Erectile dysfunction (ED) is one of the main challenges occurring among men worldwide, and is characterised by trouble getting or keeping steady erection during sexual intercourse. Various drugs like sildenafil, a phosphodiesterase-5 inhibitor (PDE-5) are freely available in the pharmacies, though normally associated with several adverse. This study was designed to assess the molecular relations obtainable between catechin, garcinal, garcinoic acid and d-tocotrienol compounds isolated from Garcinia kola and targeted receptor linked to ED. These processes include the molecular docking of catechin, garcinal, garcinoic acid, d-tocotrienol, and sildenafil to receptor: PDE-5 via AutoDock Vina. Following the docking of catechin, garcinal, garcinoic acid and d-tocotrienol with the PDE-5-receptor protein, we observed that all are protein inhibitors with garcinoic acid showing better binding affinity -10.0 kcal/mol with PDE-5 receptor relevant to ED. Hence, the results provided insights into the development of garcinoic acid as a replacement for present ED management, with further analysis worth considering.

Ameliorative effect of Kolaviron, an extract of Garcinia kola seeds, on induced hypertension.

OBJECTIVES: Early diagnosis and management of known cardiovascular disease risk attributes such as hypertension lessens morbidity and mortality as well as increase quality of life of patients. This present study was modelled to investigate the ameliorative effect of Kolaviron, an extract of Garcinia kola Heckel seeds, in ethanol- and sucrose-induced hypertension. METHODS: Test animals were divided into six groups of six animals each for each hypertensive model. Animals were treated daily with distilled water (10 ml/kg); 35% ethanol (3 g/kg) or sucrose (5-7%); Kolaviron (50, 100 and 200 mg/kg) separately plus ethanol or sucrose and Amlodipine (0.14 mg/kg) separately plus ethanol or sucrose for 8 weeks. Systolic, diastolic and mean arterial pressures were determined using non-invasive BP system after 8 weeks. Blood was obtained for the assessment of biochemical parameters, lipid profile and antioxidant indices. Vital organs were collected for approximation of tissue antioxidant levels. RESULTS: Results show that Kolaviron at various doses and Amlodipine significantly reduced (p<0.05-0.001) the elevated systolic, diastolic, and mean arterial pressures produced by ethanol and sucrose administration. Additionally, Kolaviron and Amlodipine significantly overturned (p<0.05-0.001) the reduction in GSH, SOD and CAT, and elevation in MDA levels elicited by ethanol and sucrose. Furthermore, Kolaviron and Amlodipine produced significant reduction (p<0.001) in levels of cholesterol, triglycerides and low-density lipoproteins, as well as significant increase (p<0.01-0.001) in levels of high-density lipoproteins. CONCLUSIONS: Results from this study demonstrate that Kolaviron possibly possesses significant antihypertensive effect which may possibly be attributed to its antioxidant effects and relative improvement of lipid profile.

In Vitro Anticoccidial Activities of the Extract and Fractions of Garcinia kola (Heckel h.) Against Eimeria tenella Oocyst.

BACKGROUND: Commercial poultry farming is expanding every day and contributing to the provision of affordable and high-quality protein. However, this sector is confronted with many diseases of which coccidiosis is among the most important. There are many registered patents affirming the health benefits of Garcinia kola in poultry. OBJECTIVE: Evaluation of in vitro anticoccidial activities of the extracts and fractions of Garcinia kola against Eimeria tenella oocyst was carried out. METHODS: Fresh seeds of G. kola were collected, dried under shade at room temperature, and pulverized using a mortar and a pestle. The powder was exhaustively extracted with a soxhlet apparatus using 70% methanol, and the crude methanol extract (CME) was concentrated to dryness using a rotary evaporator. The CME was further partitioned using butanol, ethylacetate, and n-hexane. The CME, butanol fraction (BTF), ethylacetate fraction (EAF), and hexane fraction (HXF) were concentrated in vacuo and tested for the presence of phytochemical constituents using standard procedures. Similarly, the CME, butanol, ethyl acetate, and hexane fractions were evaluated in vitro for oocyst sporulation inhibition. RESULTS: Phytochemical analysis revealed the presence of cardiac glycosides, saponins, carbohydrates, steroids/triterpenes, tannins, flavonoids, and alkaloids in the CME and BTF. The EAF contains all the metabolites mentioned except saponins. Similarly, HXF contains only cardiac glycosides, tannins, and steroids/ triterpenes. The CME and BTF caused a concentration-dependent increase in the inhibition of sporulation of unsporulated oocysts of E. tenella. In the acute toxicity studies, the CME did not produce any toxic effect or mortality at doses between 10 and 5000 mg/kg. The CME was then considered safe, and the LD50 was assumed to be >5000 mg/kg. CONCLUSION: The data obtained in this study suggested that the crude methanol extract (CME) of G. kola could be an appreciable beneficial effect as an anticoccidial agent against Eimeria tenella oocyst.

Kolaviron suppresses dysfunctional reproductive axis associated with multi-walled carbon nanotubes exposure in male rats.

Reproductive toxicity associated with excessive exposure to multi-walled carbon nanotubes (MWCNTs), which are commonly used in medicine as valuable drug delivery systems, is well documented. Kolaviron, a bioflavonoid isolated from Garcinia kola seeds, elicits numerous health beneficial effects related to its anti-inflammatory, anti-genotoxic activities, anti-apoptotic, and antioxidant properties. However, information on the role of kolaviron in MWCNTs-induced reproductive toxicity is not available in the literature. Herein, we assessed the protective effects of kolaviron on MWCNTs-induced dysfunctional reproductive axis in rats following exposure to MWCNTs (1 mg/kg) and concurrent treatment with kolaviron (50 or 100 mg/kg body weight) for 15 successive days. Results showed that MWCNTs-induced dysfunctional reproductive axis as evidenced by deficits in pituitary and testicular hormones, marker enzymes of testicular function, and sperm functional characteristics were abrogated in rats co-administered with kolaviron. Moreover, co-administration of kolaviron-abated MWCNTs-induced inhibition of antioxidant enzyme activities increases in oxidative stress and inflammatory indices. This is evidenced by diminished levels of tumor necrosis factor-alpha, nitric oxide, lipid peroxidation, reactive oxygen, and nitrogen species as well as reduced activity of myeloperoxidase in testes, epididymis, and hypothalamus of the rats. Biochemical data on the chemoprotection of MWCNTs-induced reproductive toxicity were corroborated by histological findings. Taken together, kolaviron suppressed dysfunctional reproductive axis associated with MWCNTs exposure via abrogation of oxidative stress and inflammation in male rats.

Genome-wide genetic diversity and population structure of Garcinia kola (Heckel) in Benin using DArT-Seq technology.

Garcinia kola (Heckel) is a versatile tree indigenous to West and Central Africa. All parts of the tree have value in traditional medicine. Natural populations of the species have declined over the years due to overexploitation. Assessment of genetic diversity and population structure of G. kola is important for its management and conservation. The present study investigates the genetic diversity and population structure of G. kola populations in Benin using ultra-high-throughput diversity array technology (DArT) single nucleotide polymorphism (SNP) markers. From the 102 accessions sampled, two were excluded from the final dataset owing to poor genotyping coverage. A total of 43,736 SNPs were reported, of which 12,585 were used for analyses after screening with quality control parameters including Minor allele frequency (≥ 0.05), call rate (≥ 80%), reproducibility (≥ 95%), and polymorphic information content (≥ 1%). Analysis revealed low genetic diversity with expected heterozygosity per population ranging from 0.196 to 0.228. Pairwise F-statistics (FST) revealed low levels of genetic differentiation between populations while an Analysis of molecular variance (AMOVA) indicated that the majority of variation (97.86%) was within populations. Population structure analysis through clustering and discriminant analysis on principal component revealed two admixed clusters, implying little genetic structure. However, the model-based maximum likelihood in Admixture indicated only one genetic cluster. The present study indicated low genetic diversity of G. kola, and interventions are needed to be tailored towards its conservation.

Study on characteristics of biflavanones distribution in Garcinia kola seeds and identification of compounds in gum resin exuded from fresh slices.

Garcinia kola seeds play an important role in African traditional medicine, which are widely used to treat stomachache, gastritis, malaria, venereal diseases and laryngitis. The habitats, specification, different parts of seeds and slicing process are important factors that affect the quality of Garcinia kola seeds. Interestingly, brownish yellow or brownish red spots were derived from gum resin exuded during slicing, whose chemical constituents have not been elucidated. A rapid high performance liquid chromatography method was established for quantitative study of four main biflavanones (GB-2, GB-1, kolaflavanone and GB-1a) in Garcinia kola seeds. We found that the content of the tested biflavanones was slightly different in Garcinia kola seeds from different habitats, while the seeds weight showed no obvious influence on the biflavanones content from the same habitat. With the aid of "spider-web" mode, we unveiled that the accumulation of biflavanones mainly occurred in seed kernels. Furthermore, slices thickness (1-2 mm) was optimized by comprehensive evaluation of biflavanones' content, moisture, cutting-time and drying-time to efficiently dry the slices. By employing of ultra-high performance liquid chromatography coupled with electrospray ionization quadrupole Orbitrap high resolution mass spectrometry (UHPLC/ESI Q-Orbitrap MS), garcinoic acid and its derivatives were successfully identified in gum resin, conducing to the interesting finding about the distribution of biflavanones and derivatives of garcinoic acid in Garcinia kola seeds. Generally, our findings in this research could contribute to standardizing the process of harvesting, processing and quality control for Garcinia kola seeds, and help better development and utilization of this important medicinal plant.