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Although medicinal plants have been used by ethnic communities since ancient times to prevent and treat various diseases, only a few have been scientifically documented. Therefore, due to their rare availability and lack of comprehensive scientific information, we reviewed the ethnomedicinal uses, phytochemistry, and pharmacological activities of plants within the genus Sarcophyte. To do this, we used specific search terms and phrases to retrieve relevant information from online sources published in English from 2000 to July 2023. The results showed that there are only two plants in the genus Sarcophyte (Sarcophyte sanguinea Sparrm. and Sarcophyte piriei Hutch.), which are traditionally used to treat a wide range of diseases, especially cancer, and skin, gastrointestinal, and urinogenital tract ailments in humans, and to cure animals in ethnoveterinary practices. It was noted that 13 secondary metabolites have been isolated from the two plants, the most prominent of which are flavonoids (diinsininol, diinsinin, and naringenin). The antioxidant activity of S. piriei is reported based on the scavenging of 2,2-diphenyl-1-picrylhydrazyl (DPPH) (IC50: 4.26 ± 0.22 μg/mL) and 2 -2′-Azino-di-[3-ethylbenzthiazoline sulfonate (ABTS) radicals (IC50: 4.62 ± 0.14 μg/mL), chelating iron (IC50: 1.82 ± 0.01 μg/mL, 3.50 ± 0.09 μg/mL), and nitric oxide (IC50: 9.97 ± 0.88 μg/mL, 9.09 ± 0.11 μg/mL). The methanolic stem extracts of S. piriei possess antimicrobial activity against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Vibrio fluvialis, and Enterococcus avium, with minimum inhibitory concentration (MIC) values ranging from 0.16 to 0.625 mg/mL, and a minimum bactericidal concentration (MBC) of 1.25 to 5 mg/mL. Cytotoxic effects of the extracts from the two plant species were also demonstrated. Sarcophyte piriei possesses therapeutic potential as evidenced by the inhibitory effects of the aqueous rhizome extract on edema (1,000 mg/kg) and prostaglandin synthesis (IC50 = 0.2 mg/mL). In addition, diinsininol and diinsinin were isolated from S. sanguinea inhibited prostaglandin synthesis (IC50: 9.20 µM, 13.14 µM) and platelet-activating factor-induced exocytosis. Therefore, based on this review, further scientific research is needed to demystify the links between traditional medicinal uses, various secondary metabolites, and the pharmacology of the two plants.

Metformin (MET) is a preferred drug for the treatment of type 2 diabetes mellitus. Recent studies show that apart from its blood glucose‐lowering effects, it also inhibits the development of various tumours, by inducing autophagy. Various studies have confirmed the inhibitory effects of MET on cancer cell lines' propagation, migration, and invasion. The objective of the study was to comprehensively review the potential of MET as an anticancer agent, particularly focusing on its ability to induce autophagy and inhibit the development and progression of various tumors. The study aimed to explore the inhibitory effects of MET on cancer cell proliferation, migration, and invasion, and its impact on key signaling pathways such as adenosine monophosphate‐activated protein kinase (AMPK), mammalian target of rapamycin (mTOR), and PI3K. This review noted that MET exerts its anticancer effects by regulating key signalling pathways such as phosphoinositide 3‐kinase (PI3K), LC3‐I and LC3‐II, Beclin‐1, p53, and the autophagy‐related gene (ATG), inhibiting the mTOR protein, downregulating the expression of p62/SQSTM1, and blockage of the cell cycle at the G0/G1. Moreover, MET can stimulate autophagy through pathways associated with the 5′ AMPK, thereby inhibiting he development and progression of various human cancers, including hepatocellular carcinoma, prostate cancer, pancreatic cancer, osteosarcoma, myeloma, and non‐small cell lung cancer. In summary, this detailed review provides a framework for further investigations that may appraise the autophagy‐induced anticancer potential of MET and its repurposing for cancer treatment. Significance statement: This comprehensive review article explores the potential of metformin (MET) as an anticancer agent, focusing on its ability to induce autophagy and inhibit the development and progression of various tumors. MET has shown potential as an anticancer agent by regulating key signaling pathways such as PI3K, LC3‐I and LC3‐II, Beclin‐1, p53, and the autophagy‐related gene (ATG), inhibiting the mammalian target of rapamycin (mTOR) protein, downregulating the expression of p62/SQSTM1, and blocking the cell cycle at the G0/G1 phase. The ability of MET to stimulate autophagy through the AMPK pathway presents a potential strategy for inhibiting the development and progression of various human cancers, including hepatocellular carcinoma, prostate cancer, pancreatic cancer, osteosarcoma, myeloma, and non‐small cell lung cancer. The detailed review of MET's effects on cancer in experimental and clinical studies, with a focus on autophagy and the AMPK/mTOR signaling pathways, provides a framework for future investigations and the potential repurposing of MET for cancer treatment. This signifies the importance of exploring MET's role in cancer therapy and its implications for clinical practice. [ABSTRACT FROM AUTHOR]

Prunus africana, a widely utilized medicinal plant in various African ethnic communities, continues to hold significant importance in traditional healing practices. Research has identified phytochemical compounds in this plant, exhibiting diverse pharmacological activities that offer potential for pharmaceutical development. Notably, P. africana is employed in treating various ailments such as wounds, diabetes mellitus, malaria, benign prostatic hyperplasia, chest pain, and prostate cancer. Its pharmacological properties are attributed to a spectrum of bioactive compounds, including tannins, saponins, alkaloids, flavonoids, terpenoids, phytosterols, and fatty acids. Multiple studies have documented the anti-inflammatory, antimicrobial, antiandrogenic, antiangiogenic, antioxidant, antidipeptidyl peptidase-4 activity, analgesic, and astringent properties of P. africana extracts. This review offers a comprehensive compilation of ethnomedicinal applications, phytochemical composition, pharmacological effects, and toxicity assessments of P. africana, serving as a foundation for future preclinical and clinical investigations. By understanding its traditional uses and chemical constituents, researchers can target specific medical conditions with greater precision, potentially expediting the development of safe and effective pharmaceuticals. Moreover, toxicity assessments provide crucial insights into the safety profile of P. africana extracts, ensuring the development of safe pharmaceuticals to treat various diseases. [ABSTRACT FROM AUTHOR]

Colorectal cancer (CRC) is a common and highly metastatic cancer affecting people worldwide. Drug resistance and unwanted side effects are some of the limitations of current treatments for CRC. Naringenin (NAR) is a naturally occurring compound found in abundance in various citrus fruits such as oranges, grapefruits, and tomatoes. It possesses a diverse range of pharmacological and biological properties that are beneficial for human health. Numerous studies have highlighted its antioxidant, anticancer, and anti‐inflammatory activities, making it a subject of interest in scientific research. This review provides a comprehensive overview of the effects of NAR on CRC. The study's findings indicated that NAR: (1) interacts with estrogen receptors, (2) regulates the expression of genes related to the p53 signaling pathway, (3) promotes apoptosis by increasing the expression of proapoptotic genes (Bax, caspase9, and p53) and downregulation of the antiapoptotic gene Bcl2, (4) inhibits the activity of enzymes involved in cell survival and proliferation, (5) decreases cyclin D1 levels, (6) reduces the expression of cyclin‐dependent kinases (Cdk4, Cdk6, and Cdk7) and antiapoptotic genes (Bcl2, x‐IAP, and c‐IAP‐2) in CRC cells. In vitro CDK2 binding assay was also performed, showing that the NAR derivatives had better inhibitory activities on CDK2 than NAR. Based on the findings of this study, NAR is a potential therapeutic agent for CRC. Additional pharmacology and pharmacokinetics studies are required to fully elucidate the mechanisms of action of NAR and establish the most suitable dose for subsequent clinical investigations. Significance statement: The review discusses the molecular and biochemical processes related to naringenin (NAR's) effects on colorectal cancer (CRC), emphasizing its diverse pharmacological and biological properties. NAR interacts with estrogen receptors, regulates gene expression related to the p53 signaling pathway, promotes apoptosis, inhibits enzymes involved in cell survival and proliferation, decreases cyclin D1 levels, and reduces the expression of cyclin‐dependent kinases and antiapoptotic genes in CRC cells. In vitro studies demonstrate that NAR derivatives have better inhibitory activities on CDK2 than NAR, suggesting their potential as therapeutic agents for CRC. [ABSTRACT FROM AUTHOR]

Background. The emergence of antimicrobial resistance (AMR) and multidrug resistance (MDR) among Escherichia coli and Klebsiella pneumoniae, especially through the production of extended spectrum β-lactamases (ESBLs), limits therapeutic options and poses a significant public health threat. Objective. The aim of this study was to assess the phenotypic and genetic determinants of antimicrobial resistance of ESBL-producing Escherichia coli and Klebsiella pneumoniae isolates from patient samples in two Kenyan Hospitals. Methods. We collected 138 E. coli and 127 K. pneumoniae isolates from various clinical specimens at the two health facilities from January 2020 to February 2021. The isolates' ESBL production and antibiotic susceptibility were phenotypically confirmed using a standard procedure. Molecular analysis was done through conventional polymerase chain reaction (PCR) with appropriate primers for gadA, rpoB, blaTEM, blaSHV, blaOXA, blaCTX-M-group-1, blaCTX-M-group-2, blaCTX-M-group-9, and blaCTX-M-group-8/25 genes, sequencing and BLASTn analysis. Results. Most E. coli (82.6%) and K. pneumoniae (92.9%) isolates were ESBL producers, with the highest resistance was against ceftriaxone (69.6% among E. coli and 91.3% among K. pneumoniae) and amoxicillin/clavulanic acid (70.9% among K. pneumoniae). The frequency of MDR was 39.9% among E. coli and 13.4% among K. pneumoniae isolates. The commonest MDR phenotypes among the E. coli isolates were CRO-FEP-AZM-LVX and CRO-AZM-LVX, while the FOX-CRO-AMC-MI-TGC-FM, FOX-CRO-FEP-AMC-TZP-AZM-LVX-MI and CRO-AMC-TZP-AZM-MI were the most frequent among K. pneumoniae isolates. Notably, the FOX-CRO-FEP-AMC-TZP-AZM-LVX-MI phenotype was observed in ESBL-positive and ESBL-negative K. pneumoniae isolates. The most frequent ESBL genes were blaTEM (42%), blaSHV (40.6%), and blaOXA (36.2%) among E. coli, and blaTEM (89%), blaSHV (82.7%), blaOXA (76.4%), and blaCTX-M-group-1 (72.5%) were most frequent ESBL genes among K. pneumoniae isolates. The blaSHV and blaOXA and blaTEM genotypes were predominantly associated with FOX-CRO-FEP-MEM and CRO-FEP multidrug resistance (MDR) and CRO antimicrobial resistance (AMR) phenotypes, among E. coli isolates from Embu Level V (16.7%) and Kenyatta National Hospital (7.0%), respectively. Conclusions. The high proportion of ESBL-producing E. coli and K. pneumoniae isolates increases the utilization of last-resort antibiotics, jeopardizing antimicrobial chemotherapy. Furthermore, the antimicrobial resistance patterns exhibited towards extended-spectrum cephalosporins, beta-lactam/beta-lactamase inhibitor combinations, fluoroquinolones, and macrolides show the risk of co-resistance associated with ESBL-producing isolates responsible for MDR. Hence, there is a need for regular surveillance and implementation of infection prevention and control strategies and antimicrobial stewardship programs. [ABSTRACT FROM AUTHOR]

Although medicinal plants have been used by ethnic communities since ancient times to prevent and treat various diseases, only a few have been scientifically documented. Therefore, due to their rare availability and lack of comprehensive scientific information, we reviewed the ethnomedicinal uses, phytochemistry, and pharmacological activities of plants within the genus Sarcophyte. To do this, we used specific search terms and phrases to retrieve relevant information from online sources published in English from 2000 to July 2023. The results showed that there are only two plants in the genus Sarcophyte (Sarcophyte sanguinea Sparrm. and Sarcophyte piriei Hutch.), which are traditionally used to treat a wide range of diseases, especially cancer, and skin, gastrointestinal, and urinogenital tract ailments in humans, and to cure animals in ethnoveterinary practices. It was noted that 13 secondary metabolites have been isolated from the two plants, the most prominent of which are flavonoids (diinsininol, diinsinin, and naringenin). The antioxidant activity of S. piriei is reported based on the scavenging of 2,2-diphenyl-1-picrylhydrazyl (DPPH) (IC50: 4.26 ± 0.22 μg/mL) and 2 -2'-Azino-di-[3-ethylbenzthiazoline sulfonate (ABTS) radicals (IC50: 4.62 ± 0.14 μg/mL), chelating iron (IC50: 1.82 ± 0.01 μg/mL, 3.50 ± 0.09 μg/mL), and nitric oxide (IC50: 9.97 ± 0.88 μg/mL, 9.09 ± 0.11 μg/mL). The methanolic stem extracts of S. piriei possess antimicrobial activity against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Vibrio fluvialis, and Enterococcus avium, with minimum inhibitory concentration (MIC) values ranging from 0.16 to 0.625 mg/mL, and a minimum bactericidal concentration (MBC) of 1.25 to 5 mg/mL. Cytotoxic effects of the extracts from the two plant species were also demonstrated. Sarcophyte piriei possesses therapeutic potential as evidenced by the inhibitory effects of the aqueous rhizome extract on edema (1,000 mg/kg) and prostaglandin synthesis (IC50 = 0.2 mg/mL). In addition, diinsininol and diinsinin were isolated from S. sanguinea inhibited prostaglandin synthesis (IC50: 9.20 μM, 13.14 μM) and platelet-activating factor-induced exocytosis. Therefore, based on this review, further scientific research is needed to demystify the links between traditional medicinal uses, various secondary metabolites, and the pharmacology of the two plants. [ABSTRACT FROM AUTHOR]

Plant-based medicines have effectively managed several ailments in humans and animals since prehistoric times. However, the pharmacologic efficacy and safety of many plants currently used in traditional medicine have not been explored empirically, which raises serious public health concerns, derailing further research and their integration into the conventional healthcare system. Despite the longstanding ethnomedicinal usage of Yushania alpina shoot extract to treat inflammation, microbial infections, and diarrhoea, among other diseases, there is insufficient scientific data to appraise its toxicity profile and safety. Accordingly, we investigated the subacute toxicity of the aqueous shoot extract of Y. alpina in Sprague Dawley rats (both sexes) for 28 days based on the Organisation for Economic Cooperation and Development guideline 407. In this study, all the experimental rats treated orally with 40 mg/Kg BW, 200 mg/Kg BW, and 1000 mg/Kg BW of the aqueous shoot extract of Y. alpina remained normal, like the control group rats, and did not show any clinical signs of subacute toxicity, and no morbidity or mortality was recorded. Besides, the weekly body weight gains and the haematological and biochemical parameters of experimental rats orally administered with the studied plant extract at the tested doses and in the control group were comparable (P > 0.05). No pathologic alterations in internal organs were observed following necroscopy. Further, the differences in weights of the liver, kidney, and spleen of experimental rats which were subacutely treated with the studied plant extract and the control rats were insignificant (P > 0.05). Moreover, no histopathological changes were observed in tissue sections of the liver, kidney, and spleen obtained from all the experimental rats. Our findings demonstrate that the aqueous shoot extract of Y. alpina may be safe as it does not elicit subacute toxicity in Sprague Dawley rats. Further toxicological and pharmacological studies using other model animals and in clinical setups are encouraged to fully appraise the efficacy and safety of the studied plant extract. [ABSTRACT FROM AUTHOR]

The Phytexponent is used to treat pain and inflammation in complementary and alternative medicine practices; however, empirical data supporting its pharmacological efficacy and safety is scanty, hence the present study. We used the carrageenan-induced paw oedema and the acetic acid-induced writhing techniques to determine the anti-inflammatory and analgesic efficacies, respectively, of the Phytexponent in Swiss albino mice models. The 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay technique was used to investigate the in vitro cytotoxic effects of the Phytexponent in the Vero E6 cell line. The Phytexponent exerted significant (P <.05) anti-inflammatory effects in the carrageenan-induced paw oedema mouse model in a dose- and time-dependent manner, with significantly higher efficacy at 250 mg/Kg BW, than indomethacin (4 mg/Kg BW), in the first, second, and third hour (P <.05). Besides, the Phytexponent significantly reduced the acetic acid-induced writhing frequency in mice (P <.05), in a dose-dependent manner, depicting its analgesic efficacy. Notably, the Phytexponent (at doses: 125 mg/Kg BW and 250 mg/Kg BW) exhibited significantly higher analgesic efficacy than the Indomethacin (P<. 05). Moreover, the Phytexponent was not cytotoxic to Vero E6 cells (CC50 >1000 µg/ml) compared to cyclophosphamide (CC50 = 2.48 µg/ml). Thus, the Phytexponent has significant in vivo anti-inflammatory and analgesic efficacy in mice models and is not cytotoxic to Vero E6 cell line, depicting its therapeutic potential upon further empirical investigation. [ABSTRACT FROM AUTHOR]

The root and leaf extracts of Launaea cornuta have been locally used in traditional medicine for decades to manage inflammatory conditions and other oxidative-stress-related syndromes; however, their pharmacologic efficacy has not been scientifically investigated and validated. Accordingly, we investigated the in vitro antioxidant activity, anti-inflammatory (in vitro, ex vivo, and in vivo) efficacy, acute oral toxicity, and qualitative phytochemical composition of the aqueous root extract of L. cornuta. The ferric-reducing antioxidant power (FRAP) and the 2,2-diphenyl-2-pycrylhydrazyl (DPPH) radical scavenging test methods were used to determine the studied plant extract's antioxidant activity. Besides, the anti-inflammatory efficacy of the studied plant extract was investigated using in vitro (anti-proteinase and protein denaturation), ex vivo (membrane stabilization), and in vivo (carrageenan-induced paw oedema in Swiss albino mice) methods. The studied plant extract demonstrated significant in vitro antioxidant effects, which were evidenced by higher DPPH radical scavenging and FRAP activities, in a concentration-dependent manner (p < 0.05). Generally, the studied plant extract exhibited significant in vitro, ex vivo, and in vivo anti-inflammatory efficacy, respectively, and in a concentration/dose-dependent manner compared with respective controls (p < 0.05). Moreover, the studied plant extract did not cause any observable signs of acute oral toxicity, even at the cut-off dose of 2000 mg/Kg BW (LD50 > 2000 mg/Kg BW), and was thus considered safe. Additionally, qualitative phytochemistry revealed the presence of various antioxidant- and anti-inflammatory-associated phytochemicals, which were deemed responsible for the reported pharmacologic efficacy. Further studies to characterise bioactive molecules and their mode(s) of pharmacologic efficacy are encouraged. [ABSTRACT FROM AUTHOR]

Snakebite envenomation (SBE) is a life-threatening global public health problem affecting over 2.7 million persons annually, with a bigger burden lying in the developing world. Despite the successful management of SBE by antivenom therapy in conventional medicine, it is of low efficacy due to the diverse venom composition across snake types, which limits its usefulness. As a result, inhabitants of the sub-Sahara region, where SBE incidence is high, utilise medicinal plants as an alternative remedy for SBE. However, most plants have not been ethnobotanically documented and validated empirically and hence this study is needed. An ethnobotanical survey to document medicinal plants used to manage SBE in Migwani ward, Mwingi West Subcounty, Kitui County, was conducted between January and February, 2021. Ethnobotanical data were collected from 45 purposefully sampled respondents from Migwani ward using semistructured questionnaires, field walks, and oral interviews. In this study, 14 medicinal plants which are used to manage SBE were documented. Four plants with the highest Relative Frequency of Citation (RFC) (Entada leptostachya Harms-stem bark (0.58), Senna singueana-roots (0.53), Securidaca longipendunculata-roots (0.36), and Strychnos henningsii-stem bark (0.46)) were selected and extracted using water, methanol, and dichloromethane according to the standard procedures. Qualitative phytochemical analysis of the plant extracts and their cytotoxic effects on brine shrimp nauplii (brine shrimp lethality assay) was conducted according to the standard techniques. Qualitative phytochemical screening revealed the presence of anti-SBE-associated phytochemicals, such as alkaloids, saponins, tannins, phenols, and flavonoids, in the aqueous and methanolic extracts of the studied plant extracts. However, the tested phytochemicals were not detected in dichloromethane extracts of all the studied extracts. The anti-SBE effects of the documented plants could be attributable to these associated bioactive phytocompounds, which are synthesized by the studied plants and transfered to humans when consumed. Furthermore, the aqueous and methanolic extracts of Entada leptostachya and Senna singueana had high LC50 of >1000 µg/ml and were considered noncytotoxic. However, Securidaca longipendunculata had an LC50 of <1000 µg/ml and was considered slightly cytotoxic. Further empirical investigations to characterise the bioactive phytochemicals and their safety should be done. [ABSTRACT FROM AUTHOR]

Introduction: Microbial infections cause high morbidity and mortality in humans globally. Antimicrobial resistance, emergence of new strains, high costs of antibiotics, inaccessibility-especially in remote areas, and adverse effects, impede successful eradications of pathogens, hence the need for novel strategies. Bridellia micrantha is used in traditional medicine to treat microbial infections; however, it has not been empirically validated. Methods: Antimicrobial activity of the aqueous and methanolic stem bark extracts of Bridellia micrantha was investigated using the disk diffusion and broth microdilution techniques, described by the Clinical Laboratory Standards Institute (CLSI) guidelines. The brine shrimp lethality assay technique was used to investigate the cytotoxic effects of the studied plant extracts in exposed nauplii. Acute oral toxicity effects of the studied plant extracts in Winstar rats were investigated following the up-and-down procedure described by the Organisation for Economic Development and Co-operation (OECD). Qualitative phytochemical screening was performed following standard procedures. Results: The aqueous and methanolic extract of B. micrantha indicated varied antimicrobial activities against E. coli, S. typhimurium, S. aureus, and C. albicans, with inhibition zones ranging from 6.00mm to 19.00mm. Furthermore, the studied plant extracts exhibited low MIC values (=100 µg/ml) on selected microbes. Since the MIC values were much lower than 1000µg/ml (the cutoff for antimicrobial efficacy appraisal), it is anticipated that, the studied plant extracts can be strong antibiotics. The aqueous and methanolic stem bark extracts of B. micrantha were cytotoxic to brine shrimp nauplii, with LC50 values of 486.67±3.15 µg/ml and 458.33±2.87 µg/ml, respectively; however, these extracts did not elicit any observable signs of toxicity in rat models. Pharmacologically active phytochemicals, including flavonoids, alkaloids, saponins, tannins, phenols, and anthraquinones were detected in the two studied extracts. Conclusions: The aqueous and methanolic stem bark extracts of B. micrantha have appreciable antimicrobial activity against E. coli, S. typhimurium, S. aureus and C. albicans. Besides, the studied plant extracts are cytotoxic to brine shrimp nauplii; but they do not cause acute oral toxicity effects in rat models. Additionally, the studied plant extracts contain bioactive phytochemicals, with antimicrobial activity. [ABSTRACT FROM AUTHOR]

Over 50 million persons are living with cognitive deficits worldwide, with over 80% of these individuals living in the developing world. The number of affected persons is projected to go over 152 million by the year 2050. Current drugs used for cognitive impairment are debatably ineffective, costly, inaccessible, and associated with undesirable events that call for the search for alternative and complementary approaches. Plants are arguably affordable, accessible, and efficacious. However, despite the reported healing claims, scientific data validating these claims are lacking. L. eriocalyx is traditionally used for the management of various conditions, including cognitive impairment but has not been scientifically explored. In this study, the Morris Water Maze (MWM) method was used to evaluate in vivo cognitive-enhancing effects of studied extracts of L. eriocalyx. Furthermore, following MWM experiments, brains were dissected and processed, and malondialdehyde profiles were determined. Qualitative phytochemical profiles of the studied plant extracts were also determined. The results showed that mice that were treated with the studied plant extracts took significantly shorter transfer latencies, navigation distances, and significantly longer latencies in the target quadrant (NW) (p < 0.05) compared with the negative control mice, indicating cognitive-enhancing activities. Furthermore, cognitively impaired mice that received the studied plant extracts had significantly lower MDA profiles compared with the MDA profile of the negative control group mice (p < 0.05). The cognitive-enhancing and MDA profile lowering effects were attributed to the presence of antioxidant phytoconstituents that ought to have modulated the redox state, thereby attenuating brain damage. These extracts can be, therefore, used for the management of cognitive deficits. Further studies leading to isolation and characterization of active molecules for cognitive impairment are recommended. Furthermore, the precise mechanism(s) through which these extracts exert their pharmacologic activity should be established. [ABSTRACT FROM AUTHOR]

Inflammation and pain are devastating conditions characterizing many diseases. Their manifestation ranges from mild body discomfort, to a debilitating experience, which may culminate in organ failure or death. In conventional medicine, corticosteroids, nonsteroidal anti-inflammatory drugs, opioids, and adjuvants are utilized to manage symptoms related to pain and inflammation. Despite their reported successes, these agents are only palliative, debatably inaccessible, unaffordable, and cause many undesirable side effects. As a result, the search for alternative and complementary therapies is warranted. Medicinal plants have been intensively utilized by humans for a long time to treat various ailments. In spite of their reported efficacies, empirical scientific data supporting their healing claims is scanty. P. thonningii (Schumach.) has been used in African traditional medicine, especially by traditional herbalists in Nigeria and Kenya, to treat conditions associated with inflammation. Even though analgesic, anti-inflammatory, and toxicity studies have been performed on leaf extracts, and some of their isolated compounds in Nigeria, there is scanty data supporting the use of stem bark extracts, which are commonly utilized in Kenya for pain, and inflammation management. Moreover, scientific data regarding safety and toxicity of the stem bark extracts of P. thonningii utilized in Kenya by traditional herbalists are inadequate. Based on this background, acute oral toxicity evaluation of the aqueous and methanolic stem bark extracts of P. thonningii, in Swiss albino mice, was performed according to the OECD/OCDE (2008) guidelines. Anti-inflammatory activities were investigated using the xylene-induced ear oedema in mice, whereas analgesic activities were examined following the acetic acid-induced writhing technique. The acute oral toxicity data was analyzed, and interpreted according to the OECDE (2008) guidelines. Anti-inflammatory and analgesic activities data were tabulated on MS Excel, and exported to GraphPad Prism (v8.3). Descriptive statistics were computed, and expressed as mean ± SEM. Thereafter, One-Way ANOVA followed by Tukey's test was performed. p < 0.05 was considered statistically significant. All the studied plant extracts had LD50 values > 2000 mg/kg bw, and were hence deemed to be nontoxic according to OECD/OCDE document no. 425. The results showed that the acetic acid-induced writhing frequency in mice administered the aqueous stem bark extract of P. thonningii, at a dose of 500 mg/kg bw, was not significantly different from that recorded for mice which received the reference drug (acetylsalicylic acid 75 mg) (p > 0.05). Additionally, at all the studied extract doses, significantly lower acetic acid-induced writhing frequencies were recorded in mice that received the aqueous stem bark extract of P. thonningii, compared with the writhing frequencies in mice that received the methanolic extract of the same plant (p < 0.05). On the other hand, the aqueous stem bark extract of P. thonningii, at doses of 100 mg/kg bw and 500 mg/kg bw, and the methanolic stem bark extract of the same plant, at a dose level of 500 mg/kg bw, exhibited significantly higher percentage inhibitions of xylene-induced oedema than the percentage inhibitions shown by the reference drug (dexamethasone 1 mg/kg bw) (p < 0.05). Generally, the aqueous stem bark extract of P. thonningii, at all the studied dose levels, caused significantly higher inhibitions of xylene-induced ear oedema in mice, compared with the percentage inhibitions shown by methanolic stem bark (p < 0.05). Therefore, the aqueous, and methanolic stem bark extracts of P. thonningii, grown in Kenya, possess peripheral analgesic and anti-inflammatory activities in Swiss albino mice. Hence, they have a potential of offering safe analgesic, and anti-inflammatory compounds. Further studies aimed at isolating, elucidating, and characterizing bioactive components from the studied extracts are recommended. Moreover, specific mode(s) through which these extracts exert the reported bioactivities should be established. Further toxicological investigations involving the studied plant extracts are encouraged to fully establish their safety. [ABSTRACT FROM AUTHOR]

Oxidative stress has been recognized as a key driver of many ailments affecting humankind. Free radicals attack biologically important biomolecules, impairing their functioning, thereby initiating and exacerbating diseases. As a comeback, antioxidant therapies have been proposed as novel approaches to ameliorating oxidative stress–associated diseases including chronic ones. Antioxidants are thought to employ multifaceted and multitargeted mechanisms that either restore oxidative homeostasis or prevent free radical buildup in the body, which overwhelm the endogenous defenses. Plants have been used for many ages across time to manage human diseases, and have a host of antioxidant phytocompounds. Piliostigma thonningii is traditionally used for the management of inflammation, malaria fever, rheumatism, and insanity, among other diseases caused by a disturbed redox state in the body. In this study, in vitro antioxidant activities of the methanolic and aqueous stem bark extracts of P. thonningii were evaluated using the in vitro antilipid peroxidation, the 1,1-diphenyl-2-picryhydrazyl (DPPH) free radical scavenging, and the ferric reducing antioxidant power assay methods. The obtained results revealed remarkable antioxidant activities of the studied plant extracts as evidenced by the low IC50 and EC50 values. These antioxidant activities could be due to the presence of antioxidant phytochemicals like flavonoids, carotenoids, tannins, and phenols, among others. Therefore, the therapeutic potency of this plant could be due to its antioxidant properties. This study recommends in vivo antioxidant efficacy testing of the studied plant extracts, as well as isolation and characterization of bioactive antioxidant compounds that are potent against oxidative stress. [ABSTRACT FROM AUTHOR]

Malaria is a deadly disease caused by a protozoan parasite whose mode of transmission is through a female Anopheles mosquito. It affects persons of all ages; however, pregnant mothers, young children, and the elderly suffer the most due to their dwindled immune state. The currently prescribed antimalarial drugs have been associated with adverse side effects ranging from intolerance to toxicity. Furthermore, the costs associated with conventional approach of managing malaria are arguably high especially for persons living in low-income countries, hence the need for alternative and complementary approaches. Medicinal plants offer a viable alternative because of their few associated side effects, are arguably cheaper, and are easily accessible. Based on the fact that studies involving antimalarial medicinal plants as potential sources of efficacious and cost-effective pharmacotherapies are far between, this research was designed to investigate antiplasmodial and cytotoxic activities of organic and aqueous extracts of selected plants used by Embu traditional medicine practitioners to treat malaria. The studied plants included Erythrina abyssinica (stem bark), Schkuhria pinnata (whole plant), Sterculia africana (stem bark), Terminalia brownii (leaves), Zanthoxylum chalybeum (leaves), Leonotis mollissima (leaves), Carissa edulis (leaves), Tithonia diversifolia (leaves and flowers), and Senna didymobotrya (leaves and pods). In vitro antiplasmodial activity studies of organic and water extracts were carried out against chloroquine-sensitive (D6) and chloroquine-resistance (W2) strains of Plasmodium falciparum. In vivo antiplasmodial studies were done by Peter's four-day suppression test to test for their in vivo antimalarial activity against P. berghei. Finally, cytotoxic effects and safety of the studied plant extracts were evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) rapid calorimetric assay technique. The water and methanolic extracts of T. brownii and S. africana and dichloromethane extracts of E. abyssinica, S. pinnata, and T. diversifolia leaves revealed high in vitro antiplasmodial activities (I C 50 ≤ 10 μ g / ml). Further, moderate in vivo antimalarial activities were observed for water and methanolic extracts of L. mollissima and S. africana and for dichloromethane extracts of E. abyssinica and T. diversifolia leaves. In this study, aqueous extracts of T. brownii and S. africana demonstrated high antiplasmodial activity and high selectivity indices values (SI ≥ 10) and were found to be safe. It was concluded that T. brownii and S. africana aqueous extracts were potent antiplasmodial agents. Further focused studies geared towards isolation of active constituents and determination of in vivo toxicities to ascertain their safety are warranted. [ABSTRACT FROM AUTHOR]

Cognitive impairment (CI) is among the leading causes of disability in humans. It is estimated that over 35.6 million people are suffering from Alzheimer's disease- (AD-) associated cognitive deficits globally with these statistics projected to rise over 115.4 million by the year 2050. There is no specific etiology for this cognitive impairment; however, various contributing factors including advancing age (>60 years old), oxidative stress, cerebral injuries, infections, neurologic disorders, and cancer have been implicated. Despite various attempts to manage CI, no curative medicines are yet available. The current drugs used to manage symptoms of AD-associated CI including Donepezil and Rivastigmine among others are only palliative rather than therapeutic. Furthermore, these agents have been associated with undesirable side effects. This calls for alternative and complementary approaches aimed at either preventing or reverting AD-related CI in a curative way without causing adverse events. It is estimated that over 80% of the world's population utilize herbal medicines for basic healthcare as it is considered safe, affordable, and easily accessible as opposed to conventional healthcare. Various parts of P. thonningii are used in traditional medicine to manage various conditions including CI. However, empirical and scientific data to validate these uses is lacking. In this study, the Morris water maze (MWM) experiment was adopted to evaluate the cognitive-enhancing effects of the studied plant extracts. The malondialdehyde (MDA) profiles in the brains of experimental mice were determined using the thiobarbituric acid reactive substances (TBARS) test. Moreover, qualitative phytochemical profiling of the studied plant extracts was performed using standard procedures. The results showed remarkable cognitive-enhancing activities which were reflected in significantly shorter transfer latencies, navigation distances, longer time spent in platform quadrant, and lower MDA levels compared with those recorded for the negative control mice (p < 0.05). Phytochemical screening of the studied plant extracts revealed the presence of antioxidant phytocompounds, which may have played key roles in the extracts' potency. Based on the findings herein, P. thonningii extracts, especially the aqueous ones have a promising potential for the management of AD-associated CI. Further studies aimed at isolating and characterizing specific active compounds for CI from P. thonningii are recommended. Additionally, specific mode(s) of action of active principles should be elucidated. Moreover, toxicity studies should be done on the studied plant extracts to ascertain their safety. [ABSTRACT FROM AUTHOR]