XYLOPIA AETHIOPICA
BOTANICAL DESCRIPTION
Xylopia aethiopica is an evergreen fragrant tree growing up to 15-30 meters high and diameter of 60 to 70 cm. It is mainly found in West, Central and Southern Africa. This plant thrives well in lowland rainforests and wet fringe forests in savanna zones. Its leaves are oblong to elliptic, simple, and alternate. The flowers are creamy-green, bisexual, and can appear alone or in clusters of three to five, in twisted spikes or cymes up to 5.5 cm long. The dark brown fruits are cylindrical, 2.5 to 5 cm long. Each pod contains 5 to 8 kidney-shaped seeds, about 5 mm long.
TAXONOMY
Order: Magnoliales
Family: Annonaceae
Genus: Xylopia
Species: aethiopica
Name: Xylopia aethiopica
COMMON NAMES
Negro pepper, African pepper, Guinea pepper, Ethiopian pepper, Black pepper and Spice tree
LOCAL NAMES
- Hwenteaa or Hwentia (TWI OR Akans)
- Etso (Ewe)
- So (Ga)
- Samaamdabile (Waala)
- Kimba (Hausa)
ETHNOBOTANICAL USES
Xylopia aethiopica is widely used in folk medicine across Africa and in Ghana specifically to treat infections including, rheumatism, stomach issues, menstrual problems, nasopharyngeal infections, diarrhoea, dysentery, boils, wounds, uterine fibroids, cough, asthma, female infertility, haemorrhoids, malaria, syphilis, diabetes, and neuralgia. Crushed seeds are applied for headaches and consumed for epilepsy, anaemia, and aiding postpartum placental expulsion.
PHYTOCHEMICAL SCREENING
The phytochemical analysis of Xylopia aethiopica revealed a rich composition of compounds in both the ethanolic stem bark extract and the dried fruit extracts. Key findings included the presence of alkaloids, flavonoids, saponins, phenols, tannins, and steroids in the stem bark, while the dried fruits contained 28 odor-active compounds, with linalool as the most prominent. The ethanol extract showcased 52 identified compounds, including dodecanoic acid, methyl ester and oleic acid, representing 100% of the oil content. The essential oil was characterised by compounds such as terpinen-4-ol (11.88%) and α-terpineol (5.93%), with the predominant classes being oxygenated monoterpenes and sesquiterpenes. This comprehensive composition underscores the potential medicinal and aromatic uses of Xylopia aethiopica.
CHEMICAL STRUCTURE
PHARMACOLOGICAL ACTIVITY
ANTIOXIDANT ACTIVITY
The ethanolic fruit extract of Xylopia aethiopica, highlights antioxidant properties, including, the ability to scavenge free radicals. The extract's bioactive chemicals, and GC-MS analysis, suggest potential applications in feed systems, animal feed composition, and medication manufacturing. The Xylopia aethiopica fruit extract and gold nanoparticles showed concentration-dependent antioxidant activities, likely due to phytochemical components like xylonic acid, alkaloids, sterols, saponins, tannins, and diterpenes. Using the DPPH (2,2-diphenyl-1-picrylhydrazyl) test, the essential oil isolated from the seeds of Xylopia aethiopica demonstrated noteworthy antioxidant activity, with an IC50 value of (2.19 ± 0.09 mg/mL).
ANTI-CHOLINESTERASE ACTIVITY
With an IC50 value of (1.21 ± 0.06 mg/mL), the essential oil isolated from the seeds of Xylopia aethiopica demonstrated considerable anti-cholinesterase action. Xylopia aethiopica essential oil exhibits anti-cholinesterase activity, inhibiting acetylcholinesterase and butyrylcholinesterase. Eugenol, a key phytochemical, has antioxidant and neuroprotective properties, potentially boosting brain acetylcholine levels for Alzheimer's disease management. Xylopia aethiopica stem bark essential oil, at a concentration of 5 ppm, exhibits significant inhibitory activity against acetylcholinesterase, enhancing cognitive function and potentially treating memory-related conditions like Alzheimer's disease by increasing acetylcholine levels.
ANALGESIC ACTIVITY
Xylopia aethiopica's analgesic properties in Wistar rats revealed strong effects, particularly at a higher dose of 50 mg/kg. Molecular docking studies suggest potential interactions between the plant's bioactive compounds and opioid receptors. The methanolic fruit extract of Xylopia aethiopica demonstrated significant analgesic effects in a formalin-induced nociception model in rats, evidenced by decreased paw licking in both early and late test phases. The ethanol extract of Xylopia aethiopica fruits and its active ingredient, xylopic acid, demonstrated significant pain-relieving properties in mouse models, likely due to its phytochemicals. Xylopic acid and its ethanol extract, Xylopia aethiopica, demonstrated significant analgesic benefits in mouse models of musculoskeletal pain, including hyperalgesia caused by carrageenan. These results validate the traditional use of X. aethiopica fruits.
ANTI-INFLAMMATORY ACTIVITY
Xylopia aethiopica fruit hydro-ethanol extract (XAE) inhibits acute inflammation by decreasing paw oedema caused by bradykinin, histamine, serotonin, and prostaglandin E2, possibly due to its anti-inflammatory properties. Xylopia aethiopica leaves' hydroethanolic extract exhibits strong anti-inflammatory effects, reducing pro-inflammatory cytokine production and 5-lipoxygenase activity, primarily due to phenolic compounds like kaempferol-3-O-rutinoside.
ANTI-ALLERGIC ACTIVITY
Xylopia aethiopica 70% ethanol extract exhibits strong anti-inflammatory and anti-allergic properties, stabilizing mast cell membranes preventing histamine release, and regulating the arachidonic acid pathway, likely due to its bioactive diterpenes, including xylopic acid. Xylopic acid, a component of Xylopia aethiopica, exhibits strong anti-allergic properties by opposing histamine H1 receptors, reducing mast cell degradation and anaphylactic reactions in mouse models, supporting its traditional use in treating allergic diseases.
ANTI-DIABETIC ACTIVITY
The acetone and ethanolic extracts of Xylopia aethiopica showed significant anti-diabetic effects in a type 2 diabetes (T2D) rat model, improving lipid profile, pancreatic histology, and glucose homeostasis. Treatment with 150 mg/kg (DXAL) and 300 mg/kg (DXAH) of the acetone fraction returned diabetic rats to near-normal conditions, with the DXAH group showing effects comparable to metformin. The anti-diabetic action is attributed to bioactive phytochemicals, including aporphine alkaloids, which inhibit pancreatic lipase and α-glucosidase, promoting glucose uptake and reducing lipid formation. No significant changes were observed in non-diabetic rats treated with 300 mg/kg XAAF.
HYPOLIPIDEMIC ACTIVITY
In Wistar rats, Xylopia aethiopica demonstrates the hypolipidemic effects of the fruit extract. The results of the study showed that the extract increased HDL cholesterol and the HDL/LDL ratio while lowering total cholesterol, triglycerides, LDL cholesterol, and VLDL cholesterol. These findings may have implications for obesity and cardiovascular disease.
ANTIMICROBIAL ACTIVITY
Xylopia aethiopica fruit extracts showed antibacterial efficacy against Candida albicans, Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa. Pseudomonas aeruginosa and Candida albicans were especially susceptible to the effects of the n-hexane and ethyl acetate fractions. In vitro, the aqueous co-extract combination of Xylopia aethiopica and Combretum molle demonstrated synergistic suppression of fungal cell growth (two times stronger inhibition than separate extracts) against Tinea corporis and Candida albicans. The extract exhibited minimum bactericidal concentrations (MBCs) of 50–100 μg/mL and minimum inhibitory concentrations (MICs) of 25–50 μg/m.
ANTIPLASMODIAL ACTIVITY AND ANTI-MALARIAL ACTIVITY
Xylopic acid, a component of Xylopia aethiopica fruit, demonstrated significant (P < 0.05) antimalarial efficacy in Plasmodium berghei -infected ICR mice, comparable to the standard drug artemether/lumefantrine, confirming both its prophylactic and curative properties. While it showed limited efficacy against chloroquine-resistant Plasmodium falciparum Dd2 strain, X. Aethiopica extract improved packed cell volume (PCV) in infected mice, highlighting its potential antimalarial benefits without causing anaemia.
CYTOTOXIC ACTIVITY
The brine shrimp lethality test revealed strong cytotoxic action in the methanolic extract of Xylopia aethiopica fruits, likely due to bioactive phytochemicals with anticancer capabilities, potentially paving the way for further exploration. Gold nanoparticles (AEXAf-AuNPs) from Xylopia aethiopica fruit extract showed cytotoxic efficacy against colorectal and breast cancer cells, but not human fibroblast cells. Their antioxidant properties may be due to phytochemicals found in the fruit. Compounds 3 and compound 5 from Xylopia aethiopica's methanol extract exhibit cytotoxic action against various cancer cell lines, likely due to the antioxidant properties of the flavonoids and alkaloids.
HEPATOPROTECTIVE ACTIVITY
The leaf extract of Xylopia aethiopica in albino rats at 200 mg/kg and 250 mg/kg significantly reduced the levels of liver enzymes (AST and ALT), suggesting a hepatoprotective action. Xylopia aethiopica extracts reduced alcohol-induced hepatotoxicity in albino rats by increasing their total antioxidant capacity, reducing malondialdehyde levels, and scavenging free radicals and reactive oxygen species produced during alcohol metabolism and oxidative stress. The Xylopia aethiopica stem bark extract prevents liver damage in Sprague Dawley rats by enhancing antioxidant enzyme activities and lowering malondialdehyde levels in the liver, likely due to its antioxidant capacity.
NEPHROPROTECTIVE ACTIVITY
Rats treated with Xylopia aethiopica fruit extract showed protection against kidney damage from carbon tetrachloride (CCl4). The ethanolic extract of Xylopia aethiopica fruits did not negatively impact the kidneys of experimental albino rats, indicating potential nephroprotective efficacy. In male rats, the aqueous extract of Xylopia aethiopica fruits showed protection against the hepatic and renal damage caused by panadol.
NEUROPROTECTIVE PROPERTY
Male Wistar rats exposed to lead-induced neurotoxicity showed neuroprotective benefits from Xylopia aethiopica extract, attributed to its antioxidant properties. This was demonstrated by reduced malondialdehyde levels, reduced antioxidant enzyme activities, and improved altered cerebral cortex histology. Animal studies show Xylopia aethiopica fruit extract and xylopic acid improve learning and memory, possibly due to their kaurene diterpenoid composition, which is a crucial phytochemical characteristic. Pretreatment with diazepam abolishes these effects. The ethanolic extract of Xylopia aethiopica fruit (XAE) and xylopic acid (XA), a neuroprotective molecule, has been found to enhance mice's learning and memory, possibly due to their anti-inflammatory and antioxidant properties.
HEMATOLOGICAL ACTIVITY
The study found that Xylopia aethiopica aqueous extract, when administered in large doses over four weeks, significantly increased platelet counts in female Wistar rats, suggesting that the fruit may have been used to stop bleeding in traditional medicine. No significant changes were observed in other haematological markers. The ethanolic extract of Xylopia aethiopica's dried fruit improved haematological parameters in Wistar rats due to its antioxidant capacity. Further research is needed to understand how these bioactive ingredients affect haematopoiesis.
DRUG-DRUG INTERACTION
SYNERGISTIC EFFECTS
The aqueous co-extract mixture of Combretum molle (stem bark) and Xylopia aethiopica (fruit) showed synergistic inhibition of fungal cell growth (2-fold higher inhibition over individual extracts) against Candida albicans and Tinea corporis in vitro. A synergistic anti-malarial effect was noted when it was coupled with the iodoquinoline alkaloid cryptolepine from Cryptolepis sanguinolenta.
TOXIC PROFILE
The aqueous fruit extract of Xylopia aethiopica exhibited acute toxicity in albino rats, with clinical symptoms such as nausea and diarrhoea observed at doses of 1000 mg/kg and above, leading to death at 2900 and 5000 mg/kg, while the calculated LD50 of 2154 mg/kg indicates that although generally safe, excessive dosages can be harmful. The hydroethanolic leaf extract of Xylopia aethiopica demonstrated low toxicity in female Wistar rats during acute and 28-day sub-chronic toxicity studies, with no observed mortality or behavioural abnormalities, and no significant effects on body weight, organ weights, or haematological and biochemical markers, as well as no cytotoxicity in the Artemia salina assay, even at doses up to 1000 mg/kg.
CLINICAL VALIDATED USES
Not reported
REFERENCES
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