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Breonadia salicina (Vahl) Hepper & J.R.I. Wood is widely distributed throughout Africa. It is used ethnobotanically to treat various diseases. However, the metabolic profile of the Breonadia species is not well characterized and the metabolites that are responsible for the bioactivity of this plant remain unknown. Therefore, there is a need to determine the phytochemical and bioactivity profile to identify metabolites that contribute to the antidiabetic, anti-inflammatory and antiproliferation activity, including the genotoxicity and cytotoxic effects, of Breonadia salicina. The study is aimed at exploring the metabolomic profile antidiabetic, anti-inflammatory and antiproliferation activity, as well as the genotoxicity and cytotoxicity effects, of constituents of B. salicina. The compounds in the B. salicina extract were analyzed by ultra-performance liquid chromatography with quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS), and the resultant data were further analyzed using a molecular networking approach. The crude stem bark and root extracts showed the highest antidiabetic activity against α-amylase at the lowest test concentration of 62.5 µg/mL, with 74.53 ± 0.74% and 79.1 ± 1.5% inhibition, respectively. However, the crude stem bark and root extracts showed the highest antidiabetic activity against α-glucosidase at the lowest test concentration of 31.3 µg/mL, with 98.20 ± 0.15% and 97.98 ± 0.22% inhibition, respectively. The crude methanol leaf extract showed a decrease in the nitrite concentration at the highest concentration of 200 µg/mL, with cell viability of 90.34 ± 2.21%, thus showing anti-inflammatory activity. No samples showed significant cytotoxic effects at a concentration of 10 µg/mL against HeLa cells. Furthermore, a molecular network of Breonadia species using UPLC-QTOF-MS with negative mode electrospray ionization showed the presence of organic oxygen compounds, lipids, benzenoids, phenylpropanoids and polyketides. These compound classes were differentially distributed in the three different plant parts, indicating the chemical differences between the stem bark, root and leaf extracts of B. salicina. Therefore, the identified compounds may contribute to the antidiabetic and anti-inflammatory activity of Breonadia salicina. The stem bark, root and leaf extracts of B. salicina yielded thirteen compounds identified for the first time in this plant, offering a promising avenue for the discovery of new lead drugs for the treatment of diabetes and inflammation. The use of molecular networking produced a detailed phytochemical overview of this Breonadia species. The results reported in this study show the importance of searching for bioactive compounds from Breonadia salicina and provide new insights into the phytochemical characterization and bioactivity of different plant parts of Breonadia salicina. [ABSTRACT FROM AUTHOR]

This study involves the investigation of various plant parts of Breonadia salicina (Vahl) Hepper and J.R.I. Wood across multiple consecutive seasons. It aims to delve into the phytochemistry of these different plant parts and establish connections between the findings and their biological activities. This comprehensive approach employs metabolomics techniques, with the ultimate goal of exploring the potential for drug development. Samples were collected in Fondwe, a village in Limpopo (South Africa), based on local reports of the efficacy of this plant used by traditional healers in the area. The antimalarial and antitrypanosomal activities of samples collected over the seasons were determined with the parasite lactate dehydrogenase (pLDH) and specific Trypanosoma brucei assays, respectively. Consequently, a total of 24 compounds were tentatively identified through ultra-performance liquid chromatography with quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS). Chemical profiles of the different plant parts of Breonadia salicina collected in different seasons produced contrasting metabolic profiles. Chemometric analysis of the UPLC-QTOF-MS data enabled us to determine the chemical variability of the crude stem bark, root and leaf extracts (n = 48) collected over four consecutive seasons by evaluating the metabolomics fingerprinting of the samples using an untargeted approach. Principal component analysis (PCA), hierarchical cluster analysis (HCA), and partial least squares discriminant analysis (PLS-DA) indicated the existence of two key clusters that are linked to the root, stem bark, and leaves. The stem and root chemistry differed from that of the leaves. Seasonal variations were noted in each plant part, with autumn and winter samples closely grouped compared to spring and summer samples in the methanol leaf extracts. Biochemometric analysis could not relate specific compounds to the antimalarial and antitrypanosomal activities of the active extracts, underscoring the intricate interactions among the secondary metabolites. This study further confirms the optimal plant parts to collect in each season for the most effective antimalarial and antitrypanosomal activities.

Breonadia salicina (Vahl) Hepper & J.R.I. Wood is widely distributed throughout Africa. It is used ethnobotanically to treat various diseases. However, the metabolic profile of the Breonadia species is not well characterized and the metabolites that are responsible for the bioactivity of this plant remain unknown. Therefore, there is a need to determine the phytochemical and bioactivity profile to identify metabolites that contribute to the antidiabetic, anti-inflammatory and antiproliferation activity, including the genotoxicity and cytotoxic effects, of Breonadia salicina. The study is aimed at exploring the metabolomic profile antidiabetic, anti-inflammatory and antiproliferation activity, as well as the genotoxicity and cytotoxicity effects, of constituents of B. salicina. The compounds in the B. salicina extract were analyzed by ultra-performance liquid chromatography with quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS), and the resultant data were further analyzed using a molecular networking approach. The crude stem bark and root extracts showed the highest antidiabetic activity against α-amylase at the lowest test concentration of 62.5 µg/mL, with 74.53 ± 0.74% and 79.1 ± 1.5% inhibition, respectively. However, the crude stem bark and root extracts showed the highest antidiabetic activity against α-glucosidase at the lowest test concentration of 31.3 µg/mL, with 98.20 ± 0.15% and 97.98 ± 0.22% inhibition, respectively. The crude methanol leaf extract showed a decrease in the nitrite concentration at the highest concentration of 200 µg/mL, with cell viability of 90.34 ± 2.21%, thus showing anti-inflammatory activity. No samples showed significant cytotoxic effects at a concentration of 10 µg/mL against HeLa cells. Furthermore, a molecular network of Breonadia species using UPLC-QTOF-MS with negative mode electrospray ionization showed the presence of organic oxygen compounds, lipids, benzenoids, phenylpropanoids and polyketides. These compound classes were differentially distributed in the three different plant parts, indicating the chemical differences between the stem bark, root and leaf extracts of B. salicina. Therefore, the identified compounds may contribute to the antidiabetic and anti-inflammatory activity of Breonadia salicina. The stem bark, root and leaf extracts of B. salicina yielded thirteen compounds identified for the first time in this plant, offering a promising avenue for the discovery of new lead drugs for the treatment of diabetes and inflammation. The use of molecular networking produced a detailed phytochemical overview of this Breonadia species. The results reported in this study show the importance of searching for bioactive compounds from Breonadia salicina and provide new insights into the phytochemical characterization and bioactivity of different plant parts of Breonadia salicina.

This study evaluated the antioxidant properties of the leaves of Breonardia salicina and the profiling of its chemicals. The leaves of the plant are widely used ethnobotanically for the treatment of cancer, gastrointestinal diseases, fevers, headaches, arthritis, diabetes, inflamed wounds, and ulcers. The plant is an evergreen growing along riverbanks, streams, and river tributaries, belonging to the family Rubiaceae. The plant was collected and identified, samples and fractions of the samples were then evaluated for antioxidant activity using DPPH and ABTS and chemical profiling of the sample was performed using LC-ESI-MS/MS. Antioxidant equivalence of the leaf extracts/fractions of the plant at R² value of 0.9938 and standard equation (y = 0.9891x - 1.996) was found to be highest at 281.7 ±0.8 mg Trolox Equivalent and lowest at 118.7 ±2.7 mg Trolox Equivalent. The LC-ESI-MS/MS of the sample identified 22 compounds with their structures, belonging to different classes including flavonoids, glycosides, phenolic acids, triterpenoids, amides, and sulphonamides. The identified compounds are of medicinal importance, which is undoubtedly responsible for the antioxidant and anticancer properties of the plant. The good antioxidant values obtained revealed the possible use of the plant in the treatment of many diseases that are known to respond to antioxidation. [ABSTRACT FROM AUTHOR]

Abstract Background Medicinal plants have been the mainstay for the treatment of various diseases since antiquity. The importance of ethnomedicinal plants in drug discovery and development can never be overemphasized. Breonadia salicina (Vahl) Hepper and J.R.I.Wood (Rubiaceae) is a medium to a large plant that is widely distributed in the tropical and subtropical regions; the leaf, stem bark, and the root have been used in folk medicine for the treatment of cancer, arthritis, inflammation, wound infections, fever, diarrhoea, and vomiting. Studies showed that the plant contains several phytochemical compounds, some of which were isolated in their pure form from various parts of the plant. The compounds isolated include ursolic acid, α-amyrin, stigmasterol, and sitosterol. Other essential compounds isolated were 7-(β-d-apiofuranosyl-(1 → 6)-β-d-glucopyranosyl) umbelliferone (Adicardin), 7-hydroxycoumarin, and 6-hydroxy-7-methoxycoumarin. Literature works on B. salicina are limited, and information regarding its nutritional value is lacking. However, the leaf of the plant is used as food preservative. Main body This review is a compilation of information obtained from scholarly databases including ScienceDirect, ResearchGate, Sci-Hub, Wiley Online Library, and Google Scholar using search keywords related to the topic of the review. The articles were selected based on the year of publication, which was from 2010 to 2021, but some older references were still be included in this review because some data in recent articles were cited from older sources. This review focuses on the ethnomedicinal uses of this plant as well as the underpinning experimental evidence of its pharmacological activities such as antibacterial, antifungal, and anti-trypanasomal activities. Conclusion There is a need to explore the potentials of this plant by initially isolating and characterizing the bioactive compounds and then subsequently evaluating its various pharmacological activities and be considered for further development to a novel therapeutic compound.

Background: Medicinal plants have been the mainstay for the treatment of various diseases since antiquity. The importance of ethnomedicinal plants in drug discovery and development can never be overemphasized. Breonadia salicina (Vahl) Hepper and J.R.I.Wood (Rubiaceae) is a medium to a large plant that is widely distributed in the tropical and subtropical regions; the leaf, stem bark, and the root have been used in folk medicine for the treatment of cancer, arthritis, inflammation, wound infections, fever, diarrhoea, and vomiting. Studies showed that the plant contains several phytochemical compounds, some of which were isolated in their pure form from various parts of the plant. The compounds isolated include ursolic acid, α-amyrin, stigmasterol, and sitosterol. Other essential compounds isolated were 7-(β-d-apiofuranosyl-(1 → 6)-β-d-glucopyranosyl) umbelliferone (Adicardin), 7-hydroxycoumarin, and 6-hydroxy-7-methoxycoumarin. Literature works on B. salicina are limited, and information regarding its nutritional value is lacking. However, the leaf of the plant is used as food preservative. Main body: This review is a compilation of information obtained from scholarly databases including ScienceDirect, ResearchGate, Sci-Hub, Wiley Online Library, and Google Scholar using search keywords related to the topic of the review. The articles were selected based on the year of publication, which was from 2010 to 2021, but some older references were still be included in this review because some data in recent articles were cited from older sources. This review focuses on the ethnomedicinal uses of this plant as well as the underpinning experimental evidence of its pharmacological activities such as antibacterial, antifungal, and anti-trypanasomal activities. Conclusion: There is a need to explore the potentials of this plant by initially isolating and characterizing the bioactive compounds and then subsequently evaluating its various pharmacological activities and be considered for further development to a novel therapeutic compound. [ABSTRACT FROM AUTHOR]

Breonadia salicina (Vahl) Hepper and J.R.I. Wood is widely used in South Africa and some other African countries for treatment of various infectious diseases such as diarrhea, fevers, cancer, diabetes and malaria. However, little is known about the active constituents associated with the biological activities. This study is aimed at exploring the metabolomics profile and antioxidant constituents of B. salicina. The chemical profiles of the leaf, stem bark and root of B. salicina were comprehensively characterized using proton nuclear magnetic resonance (1H-NMR) spectroscopy and ultra-performance liquid chromatography with quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS). The antioxidant activities of the crude extracts, fractions and pure compounds were determined using the DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging and reducing power assays. A total of 25 compounds were tentatively identified using the UPLC-QTOF-MS. Furthermore, the 1H-NMR fingerprint revealed that the different parts of plant had differences and similarities among the different crude extracts and fractions. The crude extracts and fractions of the root, stem bark and leaf showed the presence of α-glucose, β-glucose, glucose and fructose. However, catechin was not found in the stem bark crude extracts but was found in the fractions of the stem bark. Lupeol was present only in the root crude extract and fractions of the stem bark. Furthermore, 5-O-caffeoylquinic acid was identified in the methanol leaf extract and its respective fractions, while the crude extracts and fractions from the root and dichloromethane leaf revealed the presence of hexadecane. Column chromatography and preparative thin-layer chromatography were used to isolate kaempferol 3-O-(2″-O-galloyl)-glucuronide, lupeol, d-galactopyranose, bodinioside Q, 5-O-caffeoylquinic acid, sucrose, hexadecane and palmitic acid. The crude methanol stem bark showed the highest antioxidant activity in the DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging activity with an IC50 value of 41.7263 ± 7.6401 μg/mL, whereas the root crude extract had the highest reducing power activity with an IC0.5 value of 0.1481 ± 0.1441 μg/mL. Furthermore, the 1H-NMR and UPLC-QTOF-MS profiles showed the presence of hydroxycinnamic acids, polyphenols and flavonoids. According to a literature survey, these phytochemicals have been reported to display antioxidant activities. Therefore, the identified hydroxycinnamic acid (caffeic acid), polyphenol (ellagic acid) and flavonoids (catechin and (epi) gallocatechin) significantly contribute to the antioxidant activity of the different parts of plant of B. salicina. The results obtained in this study provides information about the phytochemistry and phytochemical compositions of Breonadia salicina, confirming that the species is promising in obtaining constituents with medicinal potential primarily antioxidant potential.

This study involves the investigation of various plant parts of Breonadia salicina (Vahl) Hepper and J.R.I. Wood across multiple consecutive seasons. It aims to delve into the phytochemistry of these different plant parts and establish connections between the findings and their biological activities. This comprehensive approach employs metabolomics techniques, with the ultimate goal of exploring the potential for drug development. Samples were collected in Fondwe, a village in Limpopo (South Africa), based on local reports of the efficacy of this plant used by traditional healers in the area. The antimalarial and antitrypanosomal activities of samples collected over the seasons were determined with the parasite lactate dehydrogenase (pLDH) and specific Trypanosoma brucei assays, respectively. Consequently, a total of 24 compounds were tentatively identified through ultra-performance liquid chromatography with quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS). Chemical profiles of the different plant parts of Breonadia salicina collected in different seasons produced contrasting metabolic profiles. Chemometric analysis of the UPLC-QTOF-MS data enabled us to determine the chemical variability of the crude stem bark, root and leaf extracts (n = 48) collected over four consecutive seasons by evaluating the metabolomics fingerprinting of the samples using an untargeted approach. Principal component analysis (PCA), hierarchical cluster analysis (HCA), and partial least squares discriminant analysis (PLS-DA) indicated the existence of two key clusters that are linked to the root, stem bark, and leaves. The stem and root chemistry differed from that of the leaves. Seasonal variations were noted in each plant part, with autumn and winter samples closely grouped compared to spring and summer samples in the methanol leaf extracts. Biochemometric analysis could not relate specific compounds to the antimalarial and antitrypanosomal activities of the active extracts, underscoring the intricate interactions among the secondary metabolites. This study further confirms the optimal plant parts to collect in each season for the most effective antimalarial and antitrypanosomal activities., Competing Interests: The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (© 2024 The Authors.)

Background Breonadia salicina (Rubiaceae) is a critically endangered plant at the local scale native to southwestern Saudi Arabia. To understand the levels and partitioning of genetic variation across populations and geographical regions of this species, we assessed its genetic diversity using inter-simple sequence repeat (ISSR) markers. Results Fourteen ISSR primers selected from 43 primers gave rise to 211 amplified loci, of which 68 were polymorphic. The percentage of polymorphic loci (PPL) at the population level ranged from 17.1 to 23.7%, with an average of 21.3%. Nei's gene diversity (h) and Shannon's information index (I) were 0.086 and 0.125, respectively. At the species level, PPL was 32.2%, while h and I were 0.116 and 0.172, respectively. A hierarchical analysis of molecular variance revealed a high level of genetic differentiation among populations (17% of total variance, P = 0.001), consistent with the gene differentiation coefficient (GST = 0.256). Nevertheless, the evaluated genetic diversity was very low within populations; while relatively high among populations, levels were insufficient for long-term survival. Saudi Arabian accessions were also compared to accessions of a population from Yemen, where the species is more widespread. The Yemeni population also showed low genetic diversity but clustered separately. Conclusions Breonadia salicina in Saudi Arabia is characterized by low within-population genetic diversity and high among-population genetic differentiation. Based on our findings, this locally endangered species is on the verge of local extinction. The species' survival depends on successful implementation of suggested strategies for its long-term conservation. [ABSTRACT FROM AUTHOR]

Abstract: The activity of acetone leaf extracts of Breonadia salicina and the main antifungal compound isolated from the extract, ursolic acid, was determined against three important plant fungal pathogens (Penicillium expansum, P. janthinellum and P. digitatum) to evaluate their potential use in combating post-harvest infections of oranges. In an in vitro assay, acetone extracts had good antifungal activity against P. janthinellum with an MIC (minimum inhibitory concentration) of 0.08mg/ml. P. digitatum and P. expansum were more resistant both with MICs of 1.25mg/ml. We evaluated the potential use of an acetone extract and ursolic acid against these fungal pathogens in artificially infected oranges. A crude leaf extract at a concentration of 1mg/ml gave the same level of protection as 1mg/ml ursolic acid indicating synergistic activities within the crude extract. The acetone extract had an MIC of 0.16mg/ml compared to the MIC of 0.08mg/ml of amphotericin B against P. digitatum. Cytotoxicity of the crude extract and ursolic acid was determined using a tetrazolium-based colorimetric assay (3-(4,5-dimethylthiazol)-2,5-diphenyl tetrazolium bromide (MTT)) against Vero monkey kidney cells. The acetone extract had sufficient antifungal activity in vitro against these organisms to consider its use in the citrus industry after it has been tested under production and natural infection conditions and if it does not affect the fruit quality. The extracts were however more toxic to the kidney cells than to the fungi. The results show the potential use of plant extracts to combat plant fungal infections if extracts with lower cellular toxicity can be found or if the toxicity of the extract can be decreased without changing the antifungal activity. [Copyright &y& Elsevier]

Breonadia salicina (Vahl) Hepper and J.R.I. Wood is widely used in South Africa and some other African countries for treatment of various infectious diseases such as diarrhea, fevers, cancer, diabetes and malaria. However, little is known about the active constituents associated with the biological activities. This study is aimed at exploring the metabolomics profile and antioxidant constituents of B. salicina. The chemical profiles of the leaf, stem bark and root of B. salicina were comprehensively characterized using proton nuclear magnetic resonance (1H-NMR) spectroscopy and ultra-performance liquid chromatography with quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS). The antioxidant activities of the crude extracts, fractions and pure compounds were determined using the DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging and reducing power assays. A total of 25 compounds were tentatively identified using the UPLC-QTOF-MS. Furthermore, the 1H-NMR fingerprint revealed that the different parts of plant had differences and similarities among the different crude extracts and fractions. The crude extracts and fractions of the root, stem bark and leaf showed the presence of α-glucose, β-glucose, glucose and fructose. However, catechin was not found in the stem bark crude extracts but was found in the fractions of the stem bark. Lupeol was present only in the root crude extract and fractions of the stem bark. Furthermore, 5-O-caffeoylquinic acid was identified in the methanol leaf extract and its respective fractions, while the crude extracts and fractions from the root and dichloromethane leaf revealed the presence of hexadecane. Column chromatography and preparative thin-layer chromatography were used to isolate kaempferol 3-O-(2″-O-galloyl)-glucuronide, lupeol, d-galactopyranose, bodinioside Q, 5-O-caffeoylquinic acid, sucrose, hexadecane and palmitic acid. The crude methanol stem bark showed the highest antioxidant activity in the DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging activity with an IC50 value of 41.7263 ± 7.6401 μg/mL, whereas the root crude extract had the highest reducing power activity with an IC0.5 value of 0.1481 ± 0.1441 μg/mL. Furthermore, the 1H-NMR and UPLC-QTOF-MS profiles showed the presence of hydroxycinnamic acids, polyphenols and flavonoids. According to a literature survey, these phytochemicals have been reported to display antioxidant activities. Therefore, the identified hydroxycinnamic acid (caffeic acid), polyphenol (ellagic acid) and flavonoids (catechin and (epi) gallocatechin) significantly contribute to the antioxidant activity of the different parts of plant of B. salicina. The results obtained in this study provides information about the phytochemistry and phytochemical compositions of Breonadia salicina, confirming that the species is promising in obtaining constituents with medicinal potential primarily antioxidant potential. [ABSTRACT FROM AUTHOR]