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Chemical compounds isolated and identified from Olax subscorpioidea and their reported pharmacological activities

Chemical compounds isolated and identified from Olax subscorpioidea and their reported pharmacological activities

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Background The plant Olax subscorpioidea Oliv (Olacaceae) is a shrub that is widely available in Africa. It has been used in traditional medicine to treat various diseases including asthma, pain, inflammation, gastrointestinal and central nervous system (CNS) disorders, cough, diabetes mellitus, cancer, infectious diseases, hepatic diseases, and ma...

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... santalbic acid was isolated from the methanol seed fraction of Olax subscorpioidea [45]. The phytochemical constituents identified and isolated from Olax subscorpioidea are illustrated in Table 3. The chemical structures of the major isolated compounds from Olax subscorpioidea are presented in Fig. 2. ...

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... Other tribes in Nigeria such as Edo and Igala call it Ukpakon and Ocheja respectively. [5,6]. The roots of the plant have been commonly used due to its aphrodisiac effect. ...
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One of the most common objections leveled against natural products is a lack of standardization, necessitating the exploration of various quality control approaches aimed at proving the safety and quality of crude medications. The purpose of this study was to assess the quality of Olax subscorpoidea leaves. The ethanol extract of Olax subscorpoidea leaves was obtained by the maceration process. Chemo-microscopy and physicochemical examination (moisture content, total ash value, acid insoluble ash, water soluble ash, extractive values) of the crude drug were performed using established procedures. The presence or absence of starch, mucilage, calcium oxalate, cellulose, and lignin was determined to deduce various microscopic traits with chemical reagents. The crude drugs qualitative phytochemical investigation disclosed the presence of tannins, saponins, flavonoids, alkaloids, phenols, terpenoids, steroids, and cardiac glycosides. Quantitative phytochemical analysis revealed that the plant extract had more alkaloids and saponins than the other phytoconstituents present. Chemomicroscopy of Olax subscorpoidea leaves indicated the presence of starch, mucilage, cellulose, calcium oxalate, and lignin. The physicochemical study of Olax subscorpoidea ethanol leaf extract indicated moisture content (8±0.03%) and total ash content (0.15±0.01%), respectively. The extractive value also revealed that polar solvents are most suited for extracting the crude drug. This study was able to provide useful information that aids pharmacognostic standardization, thereby building a scientific platform to buttress the quality of Olax subscorpoidea powdered leaf and its ethanol extract for ease of formulation and commercialization.
... Olax subscorpioidea, a member of the Olacaceae, is one. This plant is common in Africa and has been used to address various health concerns, including asthma, inflammation, cough, infectious diseases, diabetes, hepatitis, and cancer (12). Popoola et al found that the herb may prevent and cure cancer (13). ...
... Many medicinal plants show potential in fighting cancer, but few have been fully researched. One example is O. subscorpioidea a member of Olacaceae (12). Although the plant is known for its antioxidant and anticancer effects, its bioactive components and mechanisms of action are unknown. ...
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Introduction: Olax subscorpioidea is a medicinal plant that Africans use to treat numerous ailments, including cancer. This research examines the antioxidant, anticancer, and in-silico properties of ethyl acetate fraction of Olax subscorpioidea’s (OSEA) on 7,12-Dimethylbenz(α) anthracene (DMBA)-induced cell proliferation in female rats. Methods: Forty female Sprague Dawley rats averaging 110 ± 20 g were induced proliferation with DMBA (80 mg/kg) and treated with ethyl acetate fraction (250 mg/kg BW) of O. subscorpioidea or tamoxifen (6.6 mg/kg BW) before and after induction. The trial lasted 22 weeks. In-vivo antioxidant parameters such as superoxide dismutase (SOD), malondialdehyde (MDA), and reduced glutathione (GSH) were examined. Likewise, carcinoma antigen marker (CA153), and DNA methyltransferase 3-like (DNMT3L) activity were measured. Gas chromatography-mass spectrometry (GC-MS) detected the bioactive compounds, and molecular docking studies predicted the mechanism of action of OSEA against DNA methyltransferase. Results: Treatment with OSEA significantly increased the SOD activity, enhanced GSH levels, and lowered the levels of MDA, CA-153, and DNMT3L in DMBA-exposed rats. The GC-MS analysis of OSEA revealed the presence of 40 bioactive compounds. The molecular docking revealed that 4-cyclopentene-1,3-dione (-6.407 kcal/mol), 2-(2-hydroxyethylthio) (-4.926 kcal/mol) and 3,4,5,6-tetrahydrophthalic anhydride (-6.16 kcal/mol) had the lowest binding energies against DNMT1, DNMT3A, and DNMT3B, respectively. 2-(2-hydroxyethylthio) was the least toxic. The molecular dynamic simulation revealed that the interaction between DNMT3A and 2-(2-hydroxyethylthio) propionic was stable to an extent. : The in-silico and biochemical analysis of the ethyl acetate fraction of O. subscorpioidea showed that it can protect against lipid peroxidation and oxidative stress and may be a potent source of drug that serves as an effective therapeutic in the future.
... In pharmacological research, it was found that Olax subscorpioidea fractions and extracts exhibited analgesic, anti-inflammatory, antibacterial, antidiabetic, antimalarial, and antioxidant properties. 16 Unfortunately, there is still a limited understanding of the breast cancer anticancer mechanisms of Olax subscorpioidea. Thus, the study evaluated the anticancer properties of the ethyl acetate fraction and ethanol leaf extract of Olax subscorpioidea can help fight cancer. ...
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Breast cancer continues to be a major contributor to cancer-related deaths in developing nations. Olax subscorpioideais used in Nigerian traditional medicine as a treatment for cancer. The study examined the effects of Olax subscorpioidea'sethyl acetate fraction (OSEA) and ethanol leaf extract (OSE) on 7,12-Dimethylbenz(α)anthracene (DMBA)-induced breast cancer in female Sprague-Dawley rats. The anticancer, antioxidant and anti-inflammatory activities of the extracts were evaluated using established procedures. The study involved 40 female Sprague-Dawley rats with an average weight of 110 ± 20 g. The rats were given a dose of 80 mg/kg of DMBA to stimulate proliferation. Subsequently, OSEA, OSE (250 mg/kg BW), and tamoxifen (6.6 mg/kg BW) were administered.The trial spanned a duration of 22 weeks. The study evaluated the impact of the treatment on various aspects such as body weight, organ weight, liver and kidney function, oxidative stress indicators, oestrogen levels, Interleukin 6 (IL-6), Cancer antigen 153 (CA-153), and mammary tissue histology. It was found that body weight, Superoxide dismutase (SOD), Reduced glutathione (GSH), liver enzymes, and renal function increased significantly with OSEA and OSE therapy. The levels of oestrogen, IL-6, CA-153, and Malondialdehyde (MDA) decreased significantly. The histological study revealed that OSEA and OSE had a positive impact on acini normalisation and the inhibition of breast ductal cell growth. The study found that OSEA and OSE demonstrated promising effects against cancer, as well as antioxidant and anti-inflammatory properties, in rats with DMBA-induced breast cancer. The results offer scientific support for the traditional use of Olax subscorpioideaas a potential natural remedy for breast cancer.
... [15] Hexane, ethyl acetate and acetone fractions of leaf extract of Olax subscorpioidea were reported to show remarkable inhibition of α-amylase and α-glucosidase which are the carbohydrate digesting enzymes. [16] There are many reports available on various species of genus Olax for their antihyperglycemic activity but similar reports on O. scandens are not available and scientifically not evaluated. To provide scientific evidence to traditional claim of O. scandens bark being used as a supporting drug to treat diabetes. ...
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Background: Olax scandens Roxb. (Olacaceae) is a scandent thorny shrub used by many ethnic tribes of Asia to cure stomach ache, diarrhoea, fever, cough, mouth ulcers, anaemia, filaria, joint pains, intestinal and liver diseases and diabetes. Objectives: The present study was undertaken to investigate the in vitro hypoglycemic activity and mechanism of action of O. scandens stem bark extracts in five different in vitro models at different glucose concentrations. Materials and Methods: Various extracts of O. scandens stem bark was studied for their effect on glucose adsorption, glucose diffusion, glucose uptake by yeast cells, alpha glucosidase and alpha amylase inhibition at different glucose concentrations. Results: In the glucose adsorption method, the butanolic extract showed statistically significant increase in glucose bound concentration of 7.35 mM/L at 100 mM glucose concentration used. All extracts showed a significant retardation in glucose diffusion across a dialysis membrane into the external medium, at different time intervals. GDRI of ethyl acetate extract was 84.471 at 30 min whereas the butanolic extract and aqueous ethanolic extract showed highest GDRI of 80.267 and 70.386 at 120 min respectively. In the method of glucose uptake by yeast cells, aqueous ethanolic and butanolic extracts both showed significantly higher uptake of glucose of 65% at 5 mg/mL concentration. The ethyl acetate extract and standard acarbose showed 26.25% and 35% inhibition of alpha glucosidase respectively at 100 µg/mL concentration. Whereas at the same concentration, ethyl acetate extract and acarbose showed 48.922% and 63.093% inhibition of alpha amylase. Conclusion: Significant in vitro hypoglycemic activity was seen in glucose diffusion method suggesting a possible role of fibre which may retard glucose release across the dialysis membrane. This mechanism can be correlated with retardation in the transport of glucose across the intestinal lumen thus causing a reduction in post prandial hyperglycemia.
... O. subscorpioidea can grow up to 30 feet. The plant has been given different names by different groups of people (tribes), including Ifon by the Yorubas, Ukpakon by the Edos, Igbulu by the Igbos, Gwaanon kurmii by the Hausas, Ocheja by the Igalas and Aziza in Nsukka, Nigeria (Ukwe et al., 2010;Odoma et al., 2017;Ahmad et al., 2021). ...
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Olax subscorpioidea Oliv. is an important medicinal plant included in African traditional anticancer medicines. Little information about its safety and toxicity appears in the literature. This study thus aimed at evaluating the safety of its methanol root extract orally administered in laboratory animals. Fourier Transform Infrared (FTIR) spectrophotomet-ric analysis of O. subscorpioidea extract was conducted. For acute toxicity, methods within the Organization for Economic Cooperation and Development (OECD) guidelines were used, with slight modifications. A single female mouse was orally administered a dose of 2,000 mg/kg body weight of O. subscorpioidea methanol root extract and was monitored for at least 24 h for any signs of toxicity or death. An additional four mice (n = 4, 2/sex) were similarly treated. Another female mouse was orally administered 5,000 mg/kg body weight and observed for at least 24 h. Additional four mice were similarly treated. For sub-acute toxicity, the extract was administered daily to Wistar rats for 21 days at 250 mg/kg, 500 mg/kg, and 1,000 mg/kg. General behaviours changes, haematological, biochemical, and histological examinations on rats' organs were performed. The FTIR spectrum showed no peaks in the 2220À2260 cm À1 region, suggesting that no cyanide groups were present in the extract. A single oral dose at both 2000 mg/kg and 5000 mg/kg did not induce any signs of toxicity or mortality, indicating an oral median lethal dose (LD 50) >5000 mg/kg. When compared to the controls, dose-dependent changes were observed in the red blood cells, haemoglobin and haematocrit levels at 500 mg/kg and 1000 mg/kg (p<0.05). Histopathological examinations showed severe vascular congestion in the liver, and interstitial congestion and haemorrhage with moderate glomer-ular damage in the kidney. This study showed O. subscorpioidea root's methanol extract as non-toxic in acute administration , but with potential for toxicity in sub-acute oral administration.
... Although several scientific reports are available on the numerous pharmacological activities of O. subscorpioidea including its anticancer potentials, there is a dearth scarcity of information on isolated cytotoxic compounds from the plant (Agbabiaka and Adebayo, 2021;Ahmad et al., 2021;Adekunle et al., 2022b). Forgacs and Provost (1981) isolated an oleanane-type triterpene glycoside, olaxoside, from the leaves, root, and bark extracts of some Olax species including O. andronensis Baker, O. glabriflora P. Danguy and O. psittacorum (Lamk) Vahl. ...
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Bioactivity-guided phytochemical fractionation of the methanol extract of Olax subscorpioidea root has led to the isolation of six triterpenes. Three of these compounds are previously undescribed triterpenoid saponins: oleanolic acid 3-O-[α-L-rhamnopyranosyl-(1→3)-β-D-glucopyranosyl-(1 → 2)-6-O-methyl-β-D-glucuronopyranoside]-28-O-β-D-glucopyranosyl ester (2), oleanolic acid 3-O-[β-D-glucopyranosyl-(1 → 4)-β-D-glucopyranosyl-(1 → 3)-β-D-glucopyranoside] (3), and oleanolic acid 3-O-[β-D-glucopyranosyl-(1 → 4)-6-O-methyl-β-D-glucuronopyranoside] ester (5). Other reported known compounds include two triterpene glycosides: oleanolic acid 3-O-[β-D-glucopyranosyl-(1 → 4)-6-O-methyl-β-D-glucuronopyranoside]-28-O-β-D-glucopyranosyl ester (1) and oleanolic acid 3-O-[β-D-glucopyranosyl-(1 → 4)-β-D-glucuronopyranoside] (4); and a triterpene acid, oleanolic acid (6). The structures of these compounds were elucidated by spectroscopic means. The isolated compounds were tested against human cervical cancer (HeLa), colorectal cancer (Caco-2) and breast cancer (MCF-7) cell lines using the in vitro 3-[4,5-dimethylthiazole-2-yl] 3,5-diphenyltetrazolium bromide (MTT) assay, with vincristine as positive control. The cytotoxicity assay showed that compounds 3 and 5 exhibited significant inhibitory effects on the HeLa cell line, with IC50 values of 7.42 ± 0.34 μM and 10.27 ± 1.26 μM; and moderate effects on MCF-7 (IC50 values, 36.67 ± 1.23 μM and 43.83 ± 0.65 μM) and Caco-2 (IC50 values, 35.83 ± 0.55 μM and 39.03 ± 4.38 μM, respectively) cell lines. They were also more selectively cytotoxic than vincristine against the cancer cell lines, when compared with cytotoxicity against the normal lung cell line MRC5.
... Many scientific studies have provided preliminary evidence for some of the ethnobotanical information on O. subscorpioidea and suggested that this plant could be a good source of new drug candidates (Table 3). Some of the pharmacological activities that have been established in the literature include anti-arthritics, anticonvulsive, antidepressant, antidiabetic, anti-inflammatory, antimicrobial, antinociceptive, antioxidant, antiproliferative, anti-ulcer, cytotoxic, and hepatoprotective effects, among others (Agbabiaka & Adebayo, 2021;Ahmad et al., 2021). ...
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Background: Olax subscorpioidea Oliv. (Olacaceae) is a woody shrub that is widely distributed in Africa. It has trado-medicinal importance and is used in the treatment of asthma, cancer, convulsion, diabetes, intestinal worm infections, jaundice, mental illnesses, neurodegenerative disorders, sexually transmitted infections, swellings and rheumatism, and yellow fever. Aims: To review available literature on the phytochemistry, ethnobotany, pharmacology and toxicity of Olax subscorpioidea Oliv. Method: Published findings were searched in online databases such as Web of Science, Scopus, Pubmed, Google Scholar and other relevant sources, and the data were sorted by relevance. Combinations of keywords used in the search include Olax subscorpioidea, Olacaceae, Olax, Ewe Ifon, and African medicinal plants. Results: The presence of alkaloids, anthraquinones, cardiac glycosides, flavonoids, phenolic compounds, proanthocyanidins, saponins, tannins and triterpenes has been reported from O. subscorpioidea. Several secondary metabolites have been identified, importantly the cytotoxic santalbic acid from the seeds. Bioactivity studies on this plant demonstrated its medicinal potential mainly as an analgesic, anthelmintic, anti-arthritic, antidepressant, antihyperglycaemic, anti-inflammatory, antioxidant, antimalarial and antimicrobial agent. Oral acute toxicity of the leaf extracts in rats appears to be negligible. Conclusion: Published literature available to date on O. subscorpioidea Oliv. provides some preliminary scientific basis for the ethnomedicinal uses of this plant. However, some ethnomedicinal uses have not been scientifically validated yet, and similarly, only a limited amount of information is available on properly isolated and identified phytochemicals from this plant that link to its bioactivities.
... This plant has been investigated several times for its antimicrobial, antioxidant, anti-inflammatory, and cytotoxic activities (Tsakem et al. 2021). However, there are few reports on its phytochemical exploration (Ahmad et al. 2021). In the course of our search for bioactive compounds from medicinal plants growing in Cameroon (Nzowa et al. 2013;Tchegnitegni et al. 2015;Teponno et al. 2016; Kianf e et al. 2020), we have investigated the chemical constituents of O. subscorpioidea stem barks. ...
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A previously unreported gallocatechin glycoside, (2R,3S) 40 -O- methyl-gallocatechin-3-O-a-ʟ -rhamnopyranoside (1) and an unse- parable mixture of two previously undescribed dihydromyricetin glycosides, (2 R,3R) 40 -O-methyl-dihydromyricetin-3-O-a-ʟ -rhamno- pyranoside (2a) and (2 R,3S) 40 -O-methyl-dihydromyricetin-3-O-a-ʟ -rhamnopyranoside (2 b) along with three known compounds were isolated from the n-butanol soluble fraction of the stem bark of Olax subscorpioidea Oliv. Their structures were elucidated by detailed spectroscopic analyses, including 1 H NMR, 13C NMR, 1 H-1 H COSY, HSQC, HMBC, NOESY, HR-ESI-MS and chemical meth- ods. The crude ethanol extract, the fractions, and some of the iso- lated compounds were screened for their antioxidant and antibacterial activities. They showed significant antioxidant activ- ities with EC50 ranging from 6.29 to 18.19 mg/mL in 2,2-diphenyl- 1-picrylhydrazyl (DPPH) method and EC50 ranging from 85.77 to 86.39 mmol FeSO4/g in ferric reducing antioxidant power (FRAP) methods compared with 2.29 mg/mL and 3.52 mmol FeSO4/g for the positive control (ʟ -ascorbic acid). Nevertheless, no inhibition was observed against the tested bacterial strains at a MIC less than 256 lg/mL.
... Flavonoids, glycosides, and lignans [50] Treatment of fungi-related skin disorders [51]. ...
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The abundance of plants with medicinal values has been of great impact on the skincare industry in Nigeria. However, proper documentation of plants with skincare values has not been made. Hence, this study was aimed at surveying the traditional medicinal values of some commonly used plants for the management of skin conditions by herbal practitioners in Ilorin metropolis. Ethnobotanical and demographic information of willing respondents were obtained on the most commonly used medicinal plants via semi-structured questionnaires and oral interviews. The names of the plants were further confirmed in the world flora online (www.worldfloraonline.org). A total of 57 plants species representing 30 families, were reported by 62 respondents including males (40%) and females (60%) designated as herbs sellers (32%), traditional medicine practitioners (16%), farmers (8%), housewives (11 %) and Herb sellers/traditonal medicine practitioners (33%). Their knowledge sources include inheritance (40%), training (24 %), and a combination of inheritance and training (36%). Euphorbiaceae was the most cited (11 %) plant family, the leaves were the most cited (48%) plant part used, crush to extract juice was the most widely used (51%) method of preparation, and topical application on the affected spot was the most reported (43%) method of administration. The plants mentioned in this survey were reported to have applications against psoriasis, eczema, boils, acne, measles, dandruff, rashes, and wounds. General skin conditions represented the most commonly mentioned (14%) skin condition while mastitis was the least mentioned (1%) condition. Also, the highest (0.923) informant consensus factor (ICF) was mentioned for insect bites while the least (0.263) ICF was mentioned for general skin conditions. This study documented some of the medicinal plants that have been used to treat various skin-related conditions most of which have been mentioned in available scientific pieces of literature.
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Medicinal plants are rich sources of bioactive compounds with diverse pharmacological properties, including antimicrobial activities. This study aimed to assess the antibiofilm potential of methanol and ethanol extracts from nine selected medicinal plants, as well as their synergistic effects with doxycycline against Bacillus strains. Standard procedures were employed to determine the phytochemical composition, total phenolic, and flavonoid contents of the extracts. The antibacterial activity was evaluated using the broth microdilution method, while biofilm formation was assessed via the microtiter plate method. Antibiofilm activity was determined using the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium-bromide (MTT) assay. Combination studies were conducted using the checkerboard microdilution method. All extracts contained phenols, flavonoids, steroids, triterpenes, and anthraquinones. The methanolic extract of Psidium guajava exhibited the highest total phenolic and flavonoid contents (90.48 ± 0.55 mg GAE/g), while the ethanolic extract of Olax subscorpioidea showed the highest flavonoid content (6.48 ± 0.33 mg QE/g). Ethanol extracts of Eucalyptus globulus and Psidium guajava and methanolic extract of Syzygium jambos demonstrated significant antibacterial activity against Bacillus anthracis 34F2 Sterne strains, with a MIC value of 64 μg/mL. Biofilm formation in Bacillus strains was notably enhanced in the presence of glucose. The methanolic extract of O. subscorpioides exhibited the highest biofilm imbibition (85%), while Picralima nitida methanolic extract showed the most effective biofilm eradication (79%). The combination of Solanum torvum ethanol extract with doxycycline displayed synergistic effects against biofilm formation inhibition and eradication in all tested Bacillus strains. Taken together, Solanum torvum ethanol extract shows promise for developing new combination antibacterial therapies.