1.Antiplasmodial, cytotoxic activities and characterization of a new naturally occurring quinone methide pentacyclic triterpenoid derivative isolated from Salacia leptoclada Tul. (Celastraceae) originated from Madagascar
Ruphin Pierre Fatiany ; Baholy Robijaona ; Emmanuel Randrianarivo ; Amelie Raharisololalao ; Martin Marie-Therese ; Koto-te-Nyiwa Ngbolua
Asian Pacific Journal of Tropical Biomedicine 2013;(10):780-784
Objective:To validate scientifically the traditional use of Salacia leptoclada Tul. (Celastraceae) (S. leptoclada) and to isolate and elucidate the structure of the biologically active compound.
Methods:Bioassay-guided fractionation of the acetonic extract of the stem barks of S. leptoclada was carried out by a combination of chromatography technique and biological experiments in viro using Plasmodium falciparum and P388 leukemia cell lines as models. The structure of the biologically active pure compound was elucidated by 1D and 2D NMR spectroscopy and mass spectrometry.
Results:Biological screening of S. leptoclada extracts resulted in the isolation of a pentacyclic triterpenic quinone methide. The pure compound exhibited both in vitro a cytotoxic effect on murine P388 leukemia cells with IC50 value of (0.041±0.020) μg/mL and an antiplasmodial activity against the chloroquine-resistant strain FC29 of Plasmodium falciparum with an IC50 value of (0.052±0.030) μg/mL. Despite this interesting anti-malarial property of the lead compound, the therapeutic index was weak (0.788). In the best of our knowledge, the quinone methide pentacyclic triterpenoid derivative compound is reported for the first time in S. leptoclada.
Conclusions:The results suggest that furthers studies involving antineoplastic activity is needed for the development of this lead compound as anticancer drug.
2.Assessment of antidiabetic activity and acute toxicity of leaf extracts from Physalis peruviana L. in guinea-pig
Kasali Mushagalusa Flicien ; Kadima Ntokamunda Justin ; Mpiana Tshimankinda Pius ; Ngbolua Koto-te-Nyiwa ; Tshibangu Sha-Tshibey Damien
Asian Pacific Journal of Tropical Biomedicine 2013;(11):841-846
Objective: To verify the antidiabetic activity of leaf extracts from Physalis peruviana L. popularly used in the Eastern part of the Democratic Republic of the Congo and to point out the possible toxicity.Method:pigs at the dose range of 100 mg/kg to 3.2 g/kg of body weight. The hypoglycemic activity was evaluated by glucose tolerance test, loading animals with glucose 4 g/kg and measuring blood glucose concentrations at various times. The effect was compared to the control and glibenclamide as antidiabetic reference drug. Acute toxicity was evaluated by recording mortality rate, changes on blood biomarkers and damage caused to vital organs.Results:At a dose of 100 mg/kg, the aqueous extract induced a significant reduction of peak Aqueous decoctions prepared from dried leaves powder were administrated to guinea concentration at 30 min after glucose loading as compared with control or reference (P<0.05). At doses greater than 400 mg, some alterations on blood, kidney and liver markers were observed. Upper 800 mg/kg, mortality was observed with LD50 estimated at about 1280 mg/kg. At the autopsy, vital organs were in haemorrhage and swelling state.Conclusion:The crude aqueous extracts from the leaves of Physalis peruviana L. present hypoglycemic activity in animal model, but at high doses the plant may cause severe intoxication.
3. Chemo-type of essential oil of Ocimum basilicum L. from DR Congo and relative in vitro antioxidant potential to the polarity of crude extracts
Dorothée Dinangayi TSHILANDA ; Damase Nguwo Vele ONYAMBOKO ; Christian Muamba Tshilolo TSHIONGO ; Damien Sha-Tshibey TSHIBANGU ; Philippe Vuka TSALU ; Pius Tshimankinda MPIANA ; Philippe Bila BABADY ; Koto-te-Nyiwa NGBOLUA
Asian Pacific Journal of Tropical Biomedicine 2016;6(12):1022-1028
Objective To carry out a phyto-chemical characterization of essential oil from Ocimum basilicum L. (O. basilicum) harvested in DR Congo and to assess the antioxidant potential of crude extracts with respect to the polarity for comparison reason. Methods The phyto-chemical characterization of essential oil produced by hydro-distillation was performed by coupled gas chromatography-mass spectrometer analysis and the antioxidant potential evaluation by in vitro 2,2-diphenyl-1-picrylhydrazyl free radical scavenging activity method. Results A previously weighed amount of fresh leaves of O. basilicum produced 0.65% of essential oil that led to the identification of a set of 84.44% out of 99.98% as major compounds (> 1.5%). The chemo-type of this essential oil was linalool-methyl chavicol. Chemical components of oil were characterized by oxygenated aromatic hydrocarbons (46.00%) and oxygenated monoterpenes (26.75%). With respect to the amount of components, methyl chavicol also known as estragole (35.72%) constituted the very large quantity afterward linalool (21.25%) and then epi-α-cadinol (8.02%), α-bergamotene (6.56%), eugenol (4.60%), 1,8-cineole (4.04%), germacrene D (2.06%), thymol (1.64%), and (E)-citral (1.55%), respectively. Essential oil exhibited antioxidant potential and IC
4.Isolation and structural elucidation of cytotoxic compounds from the root bark of Diospyros quercina (Baill.) endemic to Madagascar.
Fatiany Pierre RUPHIN ; Robijaona BAHOLY ; Randrianarivo EMMANUEL ; Raharisololalao AMELIE ; Marie-Therese MARTIN ; Ngbolua KOTO-TE-NYIWA
Asian Pacific Journal of Tropical Biomedicine 2014;4(3):169-175
OBJECTIVETo isolate and characterize the cytotoxic compounds from Diospyros quercina (Baill.) G.E. Schatz & Lowry (Ebenaceae).
METHODSAn ethno-botanical survey was conducted in the south of Madagascar from July to August 2010. Bio-guided fractionation assay was carried out on the root bark of Diospyros quercina, using cytotoxicity bioassay on murine P388 leukemia cell lines as model. The structures of the cytotoxic compounds were elucidated by 1D and 2D NMR spectroscopy and mass spectrometry.
RESULTSBiological experiments resulted in the isolation of three bioactive pure compounds (named TR-21, TR-22, and TR-23) which exhibited very good in vitro cytotoxic activities with the IC50 values of (0.017 5±0.0060) µg/mL, (0.089±0.005) µg/mL and (1.027±0.070) µg/mL respectively. Thus, they support the claims of traditional healers and suggest the possible correlation between the chemical composition of this plant and its wide use in Malagasy folk medicine to treat cancer.
CONCLUSIONSThe ability of isolated compounds in this study to inhibit cell growth may represent a rational explanation for the use of Diospyros quercina root bark in treating cancer by Malagasy traditional healers. Further studies are, therefore, necessary to evaluate the in vivo anti-neoplastic activity of these cytotoxic compounds as effective anticancer drugs.
5. Antisickling activity of butyl stearate isolated from Ocimum basilicum (Lamiaceae)
Dorothée Dinangayi TSHILANDA ; Pius Tshimankinda MPIANA ; Damase Nguwo Vele ONYAMBOKO ; Blaise Mavinga MBALA ; Koto-te-Nyiwa NGBOLUA ; Damien Sha Tshibey TSHIBANGU ; Matthieu Kokengo BOKOLO ; Kalulu Muzele TABA ; Teddy Kabeya KASONGA
Asian Pacific Journal of Tropical Biomedicine 2014;4(5):393-398
Objective: To perform phytochemical analyses on the leaves of Ocimum basilicum L. (0. basilicum), to elucidate the structure of isolate and then perform the antisickling activity on the crude extract and on the isolate. Methods: The Emmel test performed on the acidified methanolic extract of this plant was used to evaluate the antisickling activity. The structure characterization of the active compound was performed using chromatographic techniques for the separation and the spectroscopic ones for structure elucidation (1H-NMR, 13C-NMR, COSY, HMBC). Results: The chemical screening on the crude extract revealed the presence of polyphenols (flavonoids, anthocyanins, leucoanthocyanins, tannins, quinones) alkaloids, saponins, triterpenoids and steroids. The obtained extract after evaporation yielded 34.50 g (11.5%) out of 300 g of powdered leaves of O. basilicum. The acidified methanolic extract and butyl stearate showed an interesting antisickling activity. Conclusions: The acidified methanolic extract and butyl stearate from 0. basilicum displayed a good antisickling activity. To the best of our knowledge, this is the first time to report the antisickling activity of this compound in this plant. The synthesized compound presented the same spectroscopic characteristics than the natural one and the antisickling activities of its derivatives are understudying.
6.Antisickling activity of butyl stearate isolated from Ocimum basilicum (Lamiaceae).
Dorothée Dinangayi TSHILANDA ; Pius Tshimankinda MPIANA ; Damase Nguwo Vele ONYAMBOKO ; Blaise Mavinga MBALA ; Koto-Te-Nyiwa NGBOLUA ; Damien Sha Tshibey TSHIBANGU ; Matthieu Kokengo BOKOLO ; Kalulu Muzele TABA ; Teddy Kabeya KASONGA
Asian Pacific Journal of Tropical Biomedicine 2014;4(5):393-398
OBJECTIVETo perform phytochemical analyses on the leaves of Ocimum basilicum L. (O. basilicum), to elucidate the structure of isolate and then perform the antisickling activity on the crude extract and on the isolate.
METHODSThe Emmel test performed on the acidified methanolic extract of this plant was used to evaluate the antisickling activity. The structure characterization of the active compound was performed using chromatographic techniques for the separation and the spectroscopic ones for structure elucidation (1H-NMR, 13C-NMR, COSY, HMBC).
RESULTSThe chemical screening on the crude extract revealed the presence of polyphenols (flavonoids, anthocyanins, leucoanthocyanins, tannins, quinones) alkaloids, saponins, triterpenoids and steroids. The obtained extract after evaporation yielded 34.50 g (11.5%) out of 300 g of powdered leaves of O. basilicum. The acidified methanolic extract and butyl stearate showed an interesting antisickling activity.
CONCLUSIONSThe acidified methanolic extract and butyl stearate from O. basilicum displayed a good antisickling activity. To the best of our knowledge, this is the first time to report the antisickling activity of this compound in this plant. The synthesized compound presented the same spectroscopic characteristics than the natural one and the antisickling activities of its derivatives are understudying.