Potent Nrf2-inducing, antioxidant, and anti-inflammatory effects and identification of constituents validate the anti-cancer use of Uvaria chamae and Olax subscorpioidea.

BACKGROUND: Uvaria chamae (UC) and Olax subscorpioidea (OS) roots are included in traditional anti-cancer remedies and some studies have identified their chemopreventive/chemotherapeutic potential. This study aimed to identify some cellular/molecular mechanisms underlying such potential and the associated chemical constituents. METHODS: Effect on the viability of cancer cells was assessed using the Alamar Blue assay; ability to modulate oxidative stress was assessed using the 2',7'-dichlorofluorescein diacetate (DCFDA) assay; potential to modulate Nuclear factor erythroid 2-related factor like-2 (Nrf2) activity was assessed in the AREc32 luciferase reporter cell line; and anti-inflammatory effect was assessed using lipopolysaccharide-induced nitric oxide release model in the RAW264.7 cells (Griess Assay). Chemical constituents were identified through liquid chromatography-mass spectrometry (LC-MS). RESULTS: Extracts up to 100 µg/ml were non-toxic or mildly toxic to HeLa, AREc32, PC3 and A549 cells (IC50 > 200 µg/ml). Each extract reduced basal and peroxide-induced levels of reactive oxygen species (ROS) in HeLa cells. OS and UC activated Nrf2, with UC producing nearly four-fold induction. Both extracts demonstrated anti-inflammatory effects. Chamanetin, isochamanetin, isouvaretin, uvaricin I and other compounds were found in U. chamae root extract. CONCLUSION: As Nrf-2 induction, antioxidant and anti-inflammatory activities are closely linked with chemoprevention and chemotherapy of cancers, the roles of these plants in traditional anti-cancer remedies are further highlighted, as is their potential as sources of drug leads.

Suppressive, curative, and prophylactic potentials of an antimalarial polyherbal mixture and its individual components in Plasmodium berghei-Infected mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Malaria remains one of the most prevalent infectious diseases in tropical regions of the world, particularly in sub-Saharan Africa, where it remains epidemiologically holoendemic. The absence of effective vaccines and Plasmodium resistance to antimalarial drugs have been the major challenges to malaria control measures. An alternative strategy could be the application of validated and standardized herbal formulations. AIM OF THE STUDY: To evaluate the antimalarial activity of a polyherbal mixture (APM) and compare it to those of its individual constituent plants. METHODS: APM consisted of stem barks of Mangifera indica (MI), Azadirachta indica (AI), Nauclea latifolia (and roots, NL) and roots of Morinda lucida (ML). Dihydroartemisinin-piperaquine (DHP) and pyronaridine-artesunate (PA) served as positive controls. Antimalarial activity was evaluated using suppressive, curative and prophylactic assays in mice infected with Plasmodium berghei. RESULTS: All the herbal mixtures, individually and in combination, showed significant (p < 0.05) antiplasmodial activities in the various assays. They produced considerable parasite suppression (>50%), substantial clearance (>70%), and notable prophylaxis (>60%, except for NL: 35%). APM (95.4-98.7%) and AI (92%), respectively, elicited greater and comparable suppression relative to DHP (88%) and PA (87.3%). However, all the herbal decoctions, individually (72-93.6%) and in combination (82.5-91%), showed lower parasite clearance than DHP (100%) and PA (99.5%). Meanwhile, APM showed relatively greater suppression and prophylaxis than its constituent plants, suggesting that the combination produced synergistic or additive effects. CONCLUSION: These findings could substantiate the use of these plants, singly or in combination, as traditional remedies for malaria. Further studies are recommended to evaluate their clinical usefulness.

COVID-19 Pandemic: A Case for Phytomedicines.

Coronavirus disease 2019 (COVID-19) is an infection caused by a newly discovered coronavirus which was identified in Wuhan, China. The race is on globally to repurpose drugs for COVID-19 and develop a safe and effective vaccine against the disease. There is an urgent need to search for effective remedies against COVID-19 from the rich and extensive flora of Africa and the world. A literature search was conducted to obtain information on drugs with the potential for effectiveness in the treatment of COVID-19 based mostly on outcomes of preclinical studies and a few clinical investigations. This was considered important to this perspective as some of the identified mechanisms of action may be related to potential anti-COVID-19 actions of phytomedicines. The findings from the literature search were also used to establish the need for exploration of phytomedicines in the fight against COVID-19. This perspective identifies the need to preserve the rich tradition of herbal medicine in Africa, repositioning it by inculcating all aspects of discovery, development, and chemical evaluation of pharmaceuticals from medicinal plants for effective management of prevalent diseases. The identified mechanisms of action of current drugs under consideration for the treatment of COVID-19 include preventing fusion of SARS-CoV-2 with human cells; decrease acidity in endosomes, cell membrane-derived vesicles for transportation of the virus within the host cell and within which the virus can replicate; and blockade of the production of proinflammatory cytokines. Phytomedicines may possibly elicit either one or a combination of these effects. The case for the exploration of phytomedicines against COVID-19 is strengthened by the emergence of a number of conventional drugs from medicinal plants and the emergence of botanicals with proven efficacy for some medical conditions. Caution against indiscriminate use of medicinal plants in the guise of treating COVID-19 has been highlighted and the need for reliable preclinical and clinical studies.

Bioactivity and modulatory functions of Napoleona vogelii on oxidative stress-induced micronuclei and apoptotic biomarkers in mice.

Napoleona vogelii is used in traditional medicine for the management of pain, inflammatory conditions and cancer. This study was conducted to investigate the modulatory mechanisms of methanol stem bark extract of N. vogelii on induction of micronuclei, apoptotic biomarkers and in vivo antioxidant enzymes in mice. Forty male albino mice were randomly divided into eight groups (n = 5) and were administered distilled water (DW, 5 mL/kg) as negative control, 100, 200 or 400 mg/kg of the extract respectively for 28 days before the injection of cyclophosphamide (CP, 40 mg/kg) i.p. on the 28th day. The remaining groups were administered 100, 200 or 400 mg/kg of the extract only for 28 days. Twenty four hours after injection of CP or administration of the last dose of extract, animals were euthanized by cervical dislocation and blood samples collected for determination of in vivo antioxidants, the spleen harvested for immunohistochemical expression of NFκB, Bcl-2, Bax and p53. Bone marrow smears were also made for the micronucleus assay. Treatment with the extract resulted in a significant (p < 0.0001) reduction in frequency of micronucleated polychromatic erythrocytes (MNPCEs) compared to CP exposed control conferring protection of 75.09, 94.74 and 96.84% at 100, 200 or 400 mg/kg respectively. In extract and CP exposed animals, there were significant (p < 0.05) increases in GSH, GST and SOD with a corresponding significant (p < 0.05) reduction in MDA. In addition, the extract significantly downregulated cytoplasmic levels of NFκB and Bcl-2 and upregulated Bax and p53. These findings demonstrate that N. vogelli may serve as an interesting lead for chemo-preventive drug development.

Antioxidative, antimitotic, and DNA-damaging activities of Garcinia kola stem bark, Uvaria chamae root, and Olax subscorpioidea root used in the ethnotherapy of cancers.

Garcinia kola (GK) stem bark, Uvaria chamae (UC) root, and Olax subscorpioidea (OS) root are components of various indigenous/traditional anticancer regimens. It is, therefore, possible that they might combat oxidative stress and impair cellular proliferation linked to carcinogenesis. In this study, we investigated the antioxidative, mito-depressive, and DNA-damaging activities of the three plant extracts in order to provide further mechanistic insights into their potential anticancer roles in documented cancer remedies that include them. Antioxidative properties were investigated in the 1,1-diphenyl-2-picrylhydrazyl (DPPH) and nitric oxide (NO) radical scavenging assays and an animal model of drug (cisplatin)-induced oxidative stress. The Allium cepa assay and the single cell gel electrophoresis (SCGE) assay were used to assess mito-depressive and DNA-damaging activities. GK and OS showed significantly higher antioxidant activities in the DPPH assay than ascorbic acid; OS had the lowest IC50 of the three plants in the NO assay, comparable to that of ascorbic acid. Pretreatment with the extracts produced an ameliorative and protective effect against the cisplatin-induced oxidative stress as shown by inhibition of lipid peroxidation and improved or restored reduced glutathione and superoxide dismutase levels. In the Allium test, the three extracts produced significant decreases in root growth and also significant cytotoxicity as evidenced by decreased mitotic index. Each of the extracts also showed significantly increased tail DNA (%) in the SCGE assay, indicating the significant DNA-damaging effect. Taken together, this study demonstrates the possible chemopreventive and chemotherapeutic potentials of the three study extracts, which may explain the roles of their source plants in traditional remedies in the therapy of cancers.

Toxicological evaluation of Picralima nitida in rodents.

Picralima nitida (Stapf) T. Durand and H. Durand (Apocynaceae), over the years has shown wide range of usage in African folk medicine and its safety profile in instances of prolonged use and pregnancy are major concerns. The study aimed to extensively investigate the toxicological effects of Picralima nitida in albino rodents and make appropriate extrapolations to humans. In the first phase of the experiment which evaluated the genotoxicity and subchronic toxicity of P. nitida, a total of 40 albino rats (male and female) were randomized into 4 groups of 10 animals per group. Group 1 (control group) was orally administered with 10 ml/kg of distilled water. Animals in Groups 2 to 4 were administered with aqueous seed extract of the plant at 100, 200, 400 mg/kg body weight/day, respectively. Oral administration at the designated doses was continued for 90 days after which they were sacrificed by cervical dislocation for subchronic toxicological assessment. In the genotoxicity phase, 30 female mice were randomized into 5 groups, the control group was treated with 10 ml/kg of distilled water, groups 2 to 4, treated with 100 mg/kg, 200 mg/kg and 400 mg/kg doses of extract, and the 5th group had cyclophosphamide (0.1 mg/kg). The mice were sacrificed on the 28th day for bone marrow sampling for genotoxicity testing. In the second phase of the experiment which evaluated the teratogenicity of P. nitida, graded doses of the extract were administered to pregnant rats from day 1-19. Three groups of 6 female rats per group were administered 75, 150 and 300 mg/kg aqueous extract of P. nitida and a fourth group of 6 rats used as control was administered distilled water at 10 ml/kg. On day 20, 3 dams from each group were sacrificed and the foetuses were harvested through abdominal incision for physical examination. The 3 remaining dams were allowed to litter. The litters were sacrificed at 6 weeks for biochemical, haematological and histological analyses. The LD50 determined was 707.107 mg/kg. The aqueous seed extract of P. nitida was found to be genotoxic at all the test doses. There were no significant alterations in haematologic and renal parameters following subchronic administration. Notable dynamics were observed in hormonal characteristics: there was a significant dose-dependent reduction in FSH while oestradiol and progesterone showed dose-dependent increase. Furthermore, P. nitida may cause hepatopathy as shown by hepatic venous and sinusoidal congestion on hepatic histology. Also, there is non-significant reduction in total cholesterol and LDL. No significant alteration in glucose level. Furthermore, the extract produced a statistically significant decrease in birth weight (p < 0.0001). The extract induced a significant (p < 0.05) increase in creatinine and transaminase levels in the first filial of group 150 mg/kg. The platelet count was increased in all treated group (p < 0.005). All the histology of kidney in 150 mg/kg group showed vascular congestion. In conclusion, the aqueous seed extract of P. nitida has teratogenic effects and should not be used in pregnant women. Also, P. nitida is highly genotoxic and may cause hepatic damage and depletion of glutathione pool on chronic use, thereby causing oxidative stress and its potential sequelae.

Biochemical, hematological, and hormonal profile of rats orally administered methanol stem bark extract of Napoleona vogelii Hook and Planch (Lecythidaceae).

Napoleona vogelii is used in traditional medicine for the management of stomach aches, ulcer, and cancers. This study was conducted to investigate the subchronic toxicological effect of methanol stem bark extract of N. vogelii on biochemical, hematological, and hormonal profile of male and female rats. Forty rats of both sexes were randomly divided into four groups of 10 rats each and were administered 100, 200, and 400 mg/kg of the extract p.o. for 90 d. Ten milliliter per kilogram of distilled water p.o. was administered to control rats. On hematological assessment, mean corpuscular hemoglobin concentration was significantly (p < 0.01) increased at 400 mg/kg compared to control. Biochemical assessment showed a significant increase (p < 0.05) in levels of alanine aminotransferase and aspartate aminotransferase at 200 and 400 mg/kg, respectively, compared to control. Hormonal assessment of male rats revealed a significantly (p < 0.0001) reduced level of testosterone at all treatment doses compared to control while estradiol was significantly (p < 0.05) reduced at 100 mg/kg, but significantly (p < 0.0001) increased at 200 and 400 mg/kg respectively compared to control in female rats. Findings from this study demonstrate that N. vogelli is relatively safe on oral acute exposure but may possess the potential to cause hepatic dysfunction and infertility in male rats by perturbations of the hypothalamic-pituitary axis while conversely enhancing fertility in female rats on subchronic administration.

Antigenotoxic and Antioxidant Activity of Methanol Stem Bark Extract of Napoleona Vogelii Hook & Planch (Lecythidaceae) In Cyclophosphamide-Induced Genotoxicity.

BACKGROUND: Napoleona vogelii is used in traditional medicine for cancer management. AIM: The study was conducted to evaluate the antigenotoxic and antioxidant activities of methanol stem bark extract of N. vogelii in male Sprague Dawley rats. MATERIALS AND METHOD: Thirty male Sprague Dawley rats were randomly divided into group 1 (control) administered 10 mL/kg distilled water, groups 2 and 3 were co-administered 100 mg/kg, 200 mg/kg of N. vogelli and 5 mg/kg cyclophosphamide (CPA) respectively for 7 days p.o. Groups 4 and 5 were administered only 5 mg/kg CPA and 200 mg/kg NV respectively. RESULTS: The LD50 oral was greater than 4 g/kg. There were significant (p < 0.0001) increases in plasma enzymatic and non-enzymatic antioxidant enzymes and significant (p < 0.0001) decrease in percentage micronuclei in bone marrow of extract treated rats compared to rats administered 5 mg/kg CPA alone. There was steatosis pointing to cytotoxic injury in the liver of rats co-administered 200 mg/kg NV and 5 mg/kg CPA. Gas chromatography-mass spectrometry analysis of the extract showed the presence of phytol and unsaturated fatty acids. CONCLUSION: N. vogelii possesses antigenotoxic and antioxidant activities associated with the presence of phytochemicals, phytol and unsaturated fatty acids.

Three indigenous plants used in anti-cancer remedies, Garcinia kola Heckel (stem bark), Uvaria chamae P. Beauv. (root) and Olax subscorpioidea Oliv. (root) show analgesic and anti-inflammatory activities in animal models.

ETHNOPHARMACOLOGICAL RELEVANCE: Phytochemicals with anti-oxidative and anti-inflammatory properties are known to inhibit tumour initiation, promotion and progression. Hence, there is an increasingly-convincing rationale for employing remedies containing those phytochemicals in the treatment of cancers and also as analgesic and anti-inflammatory adjuvants in therapy. The plants Garcinia kola Heckel (Clusiaceae), stem bark; Uvaria chamae P. Beauv. (Annonaceae), root; and Olax subscorpioidea Oliv. (Olacaceae), root, have been documented to be part of various indigenous anti-cancer regimens. AIM OF THE STUDY: To determine if the three plants exhibit significant anti-oxidative and anti-inflammatory properties. MATERIALS AND METHODS: Using established models, the analgesic and anti-inflammatory activities of the three plants were investigated. RESULTS: Pre-treatment with the plant extracts at 100, 200 and 400mg/kg produced inhibition of writhes; G. kola and U. chamae showed no significant effect on formalin-induced pain, but O. subscorpioidea produced inhibition in both phases of the formalin test. Similarly, while G. kola and U. chamae did not produce any significant inhibitory effect in the xylene-induced ear oedema model, the oedema was significantly reduced by O. subscorpioidea pre-treatment. However, all the three plants significantly inhibited the time-dependent increase in paw circumference in the carrageenan- and formaldehyde-induced rat paw oedema tests, with peak effects observed at 400mg/kg, 6h after the induction of oedema, comparable in some cases to the effects of two standard drugs, the non-steroidal anti-inflammatory drug diclofenac and the anti-inflammatory antibiotic doxycycline. CONCLUSION: We conclude that the three plant extracts possess analgesic and anti-inflammatory properties, thus providing a scientific rationale for their inclusion in some traditional anti-cancer regimens.

Potentials of Mangifera indica in the treatment of depressive-anxiety disorders: possible mechanisms of action.

BACKGROUND: Mangifera indica (Anacardiaceae) is an important herb in the traditional African and Ayurvedic medicines. The stem barks are used in the treatment of hypertension, insomnia, tumour, depression, rheumatism and as a tonic. This study was carried out to investigate antidepressant- and anxiolytic-like effect of the hydroethanol stem bark extract of M. indica (HeMI) in mice. METHODS: HeMI (12.5-100 mg/kg, p.o.) was administered 1 h before subjecting the animal to the forced swim test (FST), tail suspension test (TST) and elevated plus maze tests (EPM). RESULTS: HeMI (12.5-100 mg/kg, p.o.) treatment produced significant reduction in immobility time [F(6.56)=8.35, p<0.001], [F(6,56)=7.55, p<0.001] in the FST and TST, respectively. Moreover, co-administration of sub-therapeutic doses of imipramine or fluoxetine with HeMI (3.125 mg/kg) elicited significant reduction in time spent immobile in the FST. However, pretreatment of mice with parachlorophenylalanine, metergoline, yohimbine or sulpiride abolished the antidepressant-like effect elicited by HeMI. In the EPM, HeMI produced significant [F(5,42)=8.91, p<0.001] increase in open arms exploration by 75.55 % and this effect was blocked by pretreatment of mice with flumazenil or metergoline. CONCLUSIONS: Findings from this study showed antidepressant-like effect of M. indica through interaction with 5-HT2 receptor, α2-adrenoceptor and dopamine D2-receptors. Also, an anxiolytic-like effect through its affinity for 5-HT2 and benzodiazepine receptors. Hence, M. indica could be a potential phytotherapeutic agent in the treatment of mixed anxiety-depressive illness.

Modulatory potentials of aqueous leaf and unripe fruit extracts of Carica papaya Linn. (Caricaceae) against carbon tetrachloride and acetaminophen-induced hepatotoxicity in rats.

INTRODUCTION: Carica papaya Linn is used in a traditional medicine for hepatobiliary disorders. This study investigated the hepatomodulatory effects of aqueous extracts of C. papaya leaf (CPL) and unripe fruit (CPF) at doses of 100 and 300 mg/kg on carbon tetrachloride (CCl4) and acetaminophen (ACM)-induced liver toxicities in rats. MATERIALS AND METHODS: Rats were administered CCl4 (3 ml/kg in olive oil, i.p.) followed by oral administration of CPL and CPF at 2, 6 and 10 h intervals. The ACM model proceeded with the same method but inclusive of animals treated with N-acetyl cysteine (3 ml/kg i.p). At the end of the study, serum levels of liver biomarkers and antioxidant enzymes were assessed and histology of the liver tissues determined. RESULTS: There was a significant (P < 0.05) reduction in CCl4 and ACM-induced increases in serum levels of alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase and direct bilirubin at 100 and 300 mg/kg, respectively. The levels of catalase (CAT), superoxide dismutase and reduced GSH were decreased in both models with corresponding significantly (P < 0.05) elevated level of malondialdehyde. However, these antioxidant enzymes were significantly (P < 0.05) increased in CPL and CPF-treated rats. Histopathological assessment of the liver confirmed the protective effects of CPL and CPF on CCl4 and ACM-induced hepatic damage evidenced by the normal presentation of liver tissue architecture. CONCLUSION: These results indicate that aqueous extracts of C. papaya may be useful in preventing CCl4 and ACM-induced liver toxicities.

Modulatory potentials of the aqueous stem bark extract of Mangifera indica on carbon tetrachloride-induced hepatotoxicity in rats.

Among Yoruba herbalists (Southwest Nigeria), hot water infusion of Mangifera indica L. ( Máng Guǒ) stem bark is reputedly used for the treatment of fever, jaundice and liver disorders. The present study, therefore, investigates the protective effects and mechanism(s) of chemopreventive and curative effects of 125-500 mg/kg/day of Mangifera indica aqueous stem bark extract (MIASE) in acute CCl4-induced liver damage in rats. Rats were treated intragastrically with 125, 250 and 500 mg/kg/day of MIASE for 7 days before and after the administration of CCl4 (3 ml/kg of 20% CCl4, i.p.). The serum levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), total protein (TP), albumin (ALB), triglyceride (TG), total cholesterol (TC), high density lipoprotein cholesterol (HDL-c), low density lipoprotein cholesterol (LDL-c), total bilirubin (TB), conjugated bilirubin (CB) and fasting blood glucose (FBG) levels were estimated. In addition, hepatic tissue reduced glutathione (GSH) and the malondialdehyde (MDA) concentrations, catalase (CAT), superoxide (SOD) activities in the hepatic homogenate, and histopathological changes in the rat liver sections were determined. Preliminary qualitative phytochemical screening for bioactive compounds in MIASE was also conducted. Results showed that oral treatment with 125-500 mg/kg/day of MIASE significantly attenuated the increase in serum ALT, AST, ALP, FBG, TB, CB and LDL-c levels in acute liver injury induced by CCl4 treatment. Findings also revealed significant elevations in the serum TC, TG, HDL-c, TP and ALB levels. There was marked architectural remodeling in the hepatic lesions of hepatocyte vacuolation and centrilobular necrosis induced by CCl4 treatment, coupled with significant weight loss. MIASE also markedly enhanced SOD and CAT activities while reducing MAD formation; and increased GSH concentration in the hepatic homogenate compared with untreated CCl4-intoxicated group, with more protection offered in the curative than the chemopreventive models of CCl4 hepatotoxicity. Thus, these results indicate that MIASE has a profound protective effect against acute CCl4-induced hepatotoxicity in rats, which may be due to its free radicals scavenging effect, inhibition of lipid peroxidation, and its ability to increase antioxidant activity.

Mechanisms of analgesic and anti-inflammatory properties of Annona muricata Linn. (Annonaceae) fruit extract in rodents.

Unripe fruit of Annona muricata Linn. (Annonaceae) (soursop) is used in traditional African medicine for the treatment of neuralgia, rheumatism, and arthritic pain. This study sought to investigate the analgesic and anti-inflammatory effects of lyophilized fruit extract of Annona muricata (AM) in rodents. The analgesic activity was evaluated using the mouse writhing, formalin, and hot-plate tests while the anti-inflammatory action was investigated using the carrageenan-induced rat paw edema and xylene-induced ear edema tests. Pretreatment with AM (50, 100, and 200 mg/kg, p.o.) produced dose-dependent (P<.001) inhibition of writhes and formalin-induced pain in the late phase. AM and morphine produced time-course increase in pain threshold in hot-plate test. However, the analgesic effect elicited by AM was reversed (P<.05) by naloxone pretreatment. Similarly, the time-dependent increase in paw circumference induced by carrageenan was inhibited by AM treatment with peak effect (0.23±0.10 cm; P<.001, 200 mg/kg; 6 h), which was comparatively similar to that of diclofenac treated. Further, the xylene-induced ear edema was significantly reduced by AM (50 or 100 mg/kg) pretreatment; however, the anti-inflammatory effect elicited by AM was prevented by pretreatment of mice with N(G)-nitro-l-arginine (20 mg/kg, i.p., nitric-oxide synthase inhibitor) 15 min before AM (200 mg/kg, p.o.). The in vitro cyclooxygenase assay also showed that AM produced concentration-dependent inhibition of both cyclooxygenase (COX)-1 and COX-2 activity by 39.44%±0.05% and 55.71%±0.12%, respectively, at 100 µg/mL. In conclusion, A. muricata possesses analgesic effect through interaction with opioidergic pathway and anti-inflammatory property through inhibition of chemical mediators of inflammation.

Safety of herbal medicines use: case study of ikorodu residents in Lagos, Nigeria.

BACKGROUND: Despite the reported widespread use of herbal medicines globally and their benefits, they are not completely without potential to cause harm. The haphazard, irresponsible or non-regulated use of several herbal medicines may put the health of their users at risk of toxicity. OBJECTIVE: This study aimed to assess the general perception of the safety and occurrence of adverse effects of herbal medicines among residents of Ikorodu in Lagos, Nigeria. METHODS: The study population included 400 randomly selected and consented residents in Ikorodu. Data was collected using a standard closed and open-ended structured questionnaire with three (3) sections on socio-demography, safety and adverse effects of herbal medicines. Associations between the variables were determined using Chi square analysis. RESULTS: The results showed that 333 respondents (82.4%) believed that herbal medicines are safe for use and only 39 (9.7%) held the view that they may not be safe. RESULTS also show that 51 (12.6%) of respondents had experienced adverse effects while 250 (61.9%) said they had never experienced adverse effects from the use of herbal medicines. CONCLUSION: Herbal medicine is popular among the respondents but they appear to be ignorant of its potential toxicities. It may be necessary to educate the consumers of herbal medicines on the potentials for herbs-drugs interaction and adverse effects specially as a result of indiscriminate and unguided use of herbal medicines.

Traditional medicine policy and regulation in Nigeria: an index of herbal medicine safety.

BACKGROUND: The requirements and methods for research and evaluation of the safety and efficacy of herbal medicines are more complex than those for conventional pharmaceuticals. In addition to the aforementioned and contrary to the general belief that herbal medicines are safe and despite the profound therapeutic advantages possessed by medicinal plants, some of their constituents have been shown to be potentially toxic, carcinogenic, mutagenic, and teratogenic. Thus, traditional medicine policy and regulation have been made an integral part of the WHO proposed critical determinants of herbal medicine safety. OBJECTIVE: Therefore, this study is designed to assess the policy and regulation guiding herbal medicine in Nigeria as this information may form a safety index of herbal medicine use in Nigeria. METHODOLOGY: Structured questionnaire adopted from WHO was used to obtain the opinions of relevant stakeholders in the field of herbal medicine on the policy and regulation of herbal medicine in Nigeria. RESULTS: The results show that 68.8% of respondents agreed that there is a national policy on TM with 31.2% disagreeing on this issue. 75% of respondents agreed that implementation of the manufacturing requirements of herbal medicines is ensured by control mechanisms while 25% disagreed. Only 25% said herbal medicines are sold by licensed practitioners, with 75% believing that herbal medicines are sold by non-licensed practitioners. 87.5% said support from the WHO is needed and should be in the form of workshops on national capacity building on safety monitoring of herbal medicines. CONCLUSION: There is need for the Federal Ministry of Health to harmonize the varying opinions on traditional medicine and policy as documented in this study through collaboration and workshops on traditional medicine. These proposed approaches may guarantee the safety and regulation of herbal medicine use in Nigeria.

Evaluation of haematological, hepatic and renal functions of petroleum tanker drivers in Lagos, Nigeria.

BACKGROUND: Hydrocarbons which are among the major components of petroleum products are considered toxic and have been implicated in a number of human diseases. Tanker drivers are continuously exposed to hydrocarbons by inhalation and most of these drivers do not use protective devices to prevent inhalation of petroleum products; nor do they visit hospital regularly for routine check-up. OBJECTIVE: In view of this occupational hazard, we investigated the haematological, renal and hepatic functions of workers of petroleum tankers drivers in Lagos, Nigeria. METHOD: Twenty-five tanker drivers' and fifteen control subjects were randomly selected based on the selection criteria of not smoking and working for minimum of 5 years as petroleum tanker driver. The liver, renal and haematological parameters were analyzed using automated clinical and haematological analyzers while the lipid peroxidation and antioxidant level tests were assayed using standard methods. RESULTS: There were significant (p ≤ 0.05) increases in the levels of serum alanine amino transferase (31.14±13.72; 22.38±9.89), albumin (42.50±4.69; 45.36±1.74) and alkaline phosphatase (84.04±21.89; 62.04±23.33) of petroleum tanker drivers compared with the controls. A significant (p≤0.05) increase in the levels of creatinine, urea and white blood cells of the tanker drivers, compared with the controls, were also obtained. CONCLUSION: The results have enormous health implications of continuous exposure to petroleum products reflected hepatic and renal damage of petroleum tanker drivers. Therefore, there is need for this group of workers to be sensitized on the importance of protective devises, regular medical checkup and management.

Antinociceptive, anti-inflammatory and antiulcerogenic activities of ethanol root extract of Strophanthus hispidus DC (Apocynaceae).

BACKGROUND: Strophanthus hispidus DC (Apocynaceae) is a medicinal plant widely used in traditional African medicine in the treatment of rheumatic afflictions, ulcer, conjunctivitis, leprosy and skin diseases. This study sought to investigate the antinociceptive, anti-inflammatory and antiulcer properties of the ethanol root extract of S. hispidus. METHODS: Antinociceptive activity was evaluated using acetic acid-induced writhing and formalin tests in mice. The carrageenan- and egg albumin-induced rat paw edema tests were used to investigate the anti-inflammatory actions, whereas the antiulcer activity was investigated using ethanol-, HCl- and pyloric ligation-induced gastric ulcer models in rats. RESULTS: S. hispidus [100-800 mg/kg orally (po)] produced significant (p<0.05) inhibition of writhing reflex with peak effect of 74.13% inhibition observed at 800 mg/kg. Similarly, S. hispidus significantly (p<0.05) attenuated formalin-induced early and late phase of nociception with peak effect of 61.84% and 89.43%, respectively, at 200 mg/kg. S. hispidus (25-800 mg/kg po) caused significant (p<0.05) inhibition of edema development in the carrageenan and egg albumin models with peak effect (93.40% and 90.10% inhibition of edema formation) observed at 50 mg/kg. With respect to antiulcer activity, S. hispidus (100-800 mg/kg) showed potent antiulcer activity with respective peak effects of 96% (ethanol-induced), 99% (HCl-induced) and 70.60% inhibition of ulcer. CONCLUSIONS: The findings in this study suggest that the ethanol root extract of S. hispidus possesses antinociceptive, anti-inflammatory and antiulcerogenic activities. This justifies the use of the extract in folklore medicine for the treatment of ulcer and inflammatory disorders.

A 90 day chronic toxicity study of Nigerian herbal preparation DAS-77 in rats.

BACKGROUND: The herbal preparation DAS-77, used for the treatment of various ailments in Nigeria, contains the milled bark of Mangifera indica L. and root of Carica papaya L. Toxicological assessment of the preparation was carried out in this study. METHODS: In the acute toxicity study, DAS-77 was administered to mice p.o. up to 20 g/kg in divided doses and i.p. at 250-3000 mg/kg. Mortality within 24 h was recorded. In the chronic toxicity study, rats were treated p.o. for 90 days at doses of 80, 400 (therapeutic dose, TD) and 2000 mg/kg. By 90 days, animals were sacrificed and blood samples collected for hematological and biochemical analysis. Organs were harvested for weight determination, antioxidants and histopathological assessments. RESULTS: DAS-77 did not produce any lethality administered p.o. up to 20 g/kg in divided doses but the i.p. LD50 was 1122.0 mg/kg. At TD, DAS-77 produced significant (p < 0.05) reductions in body weight, food intake and K+, and increases in ovary weight, neutrophils and HDL, which were reversible. Histopathological presentations were generally normal. Effects at the other doses were comparable to those at TD except for reversible increases in antioxidants in the liver, kidney and testes, and sperm abnormality, and reductions in liver enzymes, sperm motility and count. CONCLUSIONS: Findings in this study revealed that DAS-77 is relatively safe with the potential for enhancing in vivo antioxidant activity. However, possibly reversible side-effects include electrolyte imbalance and sterility in males.

Use of complementary medicine amongst patients on antiretroviral drugs in an HIV treatment centre in Lagos, Nigeria.

Traditional herbal remedies have been used to treat many ailments in Nigeria but the safety of herbal remedies has been the major concerns to many people especially when the chemical constituents of the products are not known. This study is therefore designed to evaluate the prevalence of use of complementary drugs with antiretroviral (ARV) therapy and possible treatment outcome of the concurrent utilization of these therapeutic agents. A descriptive cross-sectional survey of 354 HIV patients attending APIN clinics in LUTH using a consecutive sampling technique was used. There was also correlation of the data obtained from the patients with their clinical case notes. Results showed that only 8.2 % of the respondents' used herbal medicine concurrently with ARV therapy. Ninety percent of the participants were on a two nucleoside and one non-nucleoside based ARV therapy. The most common regimen (55%) was Zidovudine/lamivudine/Nevirapine fixed dose combination while 10% use a protease inhibitor based regimen. The commonly herbal drugs used ranges from Jobelyn [Sorghum bicolor plant leaves (13.8%)], Garlic [Allicin, γ-glutamyl- (s)-ally-L-Cysteine] (10.3%), Ginger [Essential oil] (17.2%) and Aloe vera [Hydroxyanthracene derivatives expressed as Barbaloin] (10.3%). The major reason for the commencement of herbal medicine is the perception that the medicine will boost their immunity (65.5%). However, there was a marginal improvement though not significant (p ≥ 0.05) in the CD4 counts (489.8 ± 195.2; 419.1 ± 236.2) and viral load (5117.8 ± 26092.0; 31136.7 ± 197954.6) of HIV patients on herbal drugs compared to those who are not on herbal drugs. Herbal medicines have potentials to interact with ARVs and thus result in adverse reactions and possibly therapeutic failure. There is need for thorough investigation of the pharmacological action of these herbal medicines in HIV treatment taking into consideration their pharmacokinetic and toxicological profile.

Toxicological evaluation of the aqueous leaf extract of Moringa oleifera Lam. (Moringaceae).

ETHNOPHARMACOLOGICAL RELEVANCE: The rapid increase in consumption of herbal remedies worldwide has been stimulated by several factors, including the notion that all herbal products are safe and effective. However, over the past decade, several news-catching episodes in developed communities indicated adverse effects, sometimes life-threatening, allegedly arising as a consequence to taking herbal products or traditional medicines from various ethnic groups. Despite the popular use of Moringa oleifera for treating various disorders, there is limited or no scientific data available regarding safety aspects of this remedy, nor are there any documented toxicological studies that can be used to ascertain the safety index of its herbal preparation. Therefore, this present study aimed to carry out extensive toxicological evaluation of the aqueous leaf extract of Moringa oleifera. MATERIALS AND METHODS: In an acute toxicity test, male Wistar albino mice were orally administered an aqueous extract up to 6400 mg/kg and intraperitoneally up to 2000 mg/kg. A sub-chronic toxicity test was performed by daily administration with the extract at 250, 500 and 1500 mg/kg orally for 60 days. Control rats received distilled water. Sperm quality was analyzed, haematological and biochemical (liver enzymes, urea and creatinine) parameters were determined and a histopathological examination was carried out. RESULTS: The LD(50) was estimated to be 1585 mg/kg. The extract did not elicit any significant difference (P≥0.05) in sperm quality, haematological and biochemical parameters in the treated rats compared to the control. Moreover, there was no significant difference in weight gain of the control and treated animals although there was a dose-dependent reduction in food consumption of the animals treated with 250 to 1500 mg/kg extract. CONCLUSIONS: Results obtained in this study suggest that the aqueous leaf extract of Moringa oleifera is relatively safe when administered orally.