RESUMEN
Three new cycloartane triterpenoids, commikuanoids A-C (1-3), together with four known compounds 4-7, were isolated from the resin of Commiphora kua. Their structures were confirmed by advanced NMR techniques such as 1D (1H and 13C) and 2D (HMBC, HSQC, COSY, NOESY and NOE) and high-resolution mass spectrometry (HRMS). Five compounds (1-5) were screened for in vitro carbonic anhydrase II (CA II) inhibitory activity. All the tested compounds demonstrated significant activity against CA II with IC50 values ranging from 4.9-19.6 µM. Moreover, the binding pattern of each compound in the binding site of CA-II was predicted through in silico molecular docking approach. It was observed that compounds 2, 4, and 5 binds with the Zn ion present in the active site of CA II, while compounds 1 and 3 mediated hydrogen bonding with Thr199 of CA-II, and all the compounds showed good binding score (> - 5 kcal/mol).
Asunto(s)
Anhidrasa Carbónica II/antagonistas & inhibidores , Commiphora/química , Simulación del Acoplamiento Molecular/métodos , Resinas de Plantas/química , Triterpenos/aislamiento & purificación , Anhidrasa Carbónica II/metabolismo , Concentración 50 Inhibidora , Espectroscopía de Resonancia Magnética/métodos , Espectrometría de Masa por Ionización de Electrospray , Triterpenos/química , Triterpenos/farmacologíaRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Drug induced liver damage remains a prevalent concern in healthcare and may reduce the effectiveness of therapy by compromising therapeutic regimens. Many Commiphora species are known for their medicinal properties, and some of them are used traditionally for hepatoprotective effect. In the course of our drugs discovery from natural sources, phytosterols (lophenol (Lop) and lathosterol (Lat)), isolated from Commiphora kua were studied to evaluate their hepatoprotective effects in acetaminophen (APAP) induced hepatotoxicity in mice. AIMS AND OBJECTIVE: To evaluate the hepatoprotective effects of phytosterols isolated from C. kua using in vivo experimental model. MATERIALS AND METHODS: Mice of either sex were divided into 7 groups: Vehicle, silymarin (SLY), acetaminophen (APAP), Lop 25, Lop 50, Lat 25, Lat 50 (nâ¯=â¯5). Vehicle group received only vehicle (0.1% DMSO solution) for 7 days, APAP group received single dose of acetaminophen on day 7 and SLY group received silymarin for 7 days. Lop 25 and Lop 50 received low and high doses of Lop (25⯵g/kg BW and 50⯵g/kg BW), respectively, for 7 days, while Lat 25 and Lat 50 received low and high doses of Lat (25⯵g/kg BW and 50⯵g/kg BW) for 7 days. On day 7, all animals except Vehicle group kept fasted for 18â¯h and received APAP i. p. 400â¯mg/kg BW. After 20â¯h of APAP administration, the animals anesthetized with light chloroform and scarified by cervical decapitation. The blood serum and liver tissue samples were collected for biochemical and histopathological analysis. Liver function tests (LFTs) including lactate deydrogenase (LDH), alkaline phosphatase (ALP), alanine transaminase (ALT), aspartate transaminase (AST) and direct bilirubin) were used as biochemical parameters. While catalase (CAT), superoxide dismutase (SOD) and reduced glutathione (GSH) were taken as anti-oxidant enzymes. RESULTS: Significant increase in levels of ALT, AST, ALP, LDH and direct bilirubin, and significant decrease in concentration of anti-oxidant enzymes (SOD, CAT and GSH) was observed in APAP-treated group. Similarly, histological slides showed obvious signs of damage to liver cells, reflecting acetaminophen induced hepatotoxicity. Treatment of test animals with phytosterols resulted in significant recovery of LFTs profile and concentration of anti-oxidant enzymes. Similarly, significant improvement of liver tissues was noted in histological analysis. CONCLUSIONS: Both phytosterols possessed hepatoprotective potential and should be further evaluated for acute toxicity studies and pharmacokinetics/pharmacodynamics profile.
Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico , Colesterol/uso terapéutico , Commiphora , Extractos Vegetales/uso terapéutico , Sustancias Protectoras/uso terapéutico , Acetaminofén , Animales , Catalasa/metabolismo , Enfermedad Hepática Inducida por Sustancias y Drogas/metabolismo , Enfermedad Hepática Inducida por Sustancias y Drogas/patología , Colestenos/farmacología , Colestenos/uso terapéutico , Colesterol/farmacología , Femenino , Glutatión/metabolismo , Hígado/efectos de los fármacos , Hígado/metabolismo , Hígado/patología , Masculino , Ratones , Extractos Vegetales/farmacología , Sustancias Protectoras/farmacología , Resinas de Plantas/química , Superóxido Dismutasa/metabolismoRESUMEN
BACKGROUND AND AIMS: Southern Arabia is a global biodiversity hotspot with a high proportion of endemic desert-adapted plants. Here we examine evidence for a Pleistocene climate refugium in the southern Central Desert of Oman, and its role in driving biogeographical patterns of endemism. METHODS: Distribution data for seven narrow-range endemic plants were collected systematically across 195 quadrats, together with incidental and historic records. Important environmental variables relevant to arid coastal areas, including night-time fog and cloud cover, were developed for the study area. Environmental niche models using presence/absence data were built and tuned for each species, and spatial overlap was examined. KEY RESULTS: A region of the Jiddat Al Arkad reported independent high model suitability for all species. Examination of environmental data across southern Oman indicates that the Jiddat Al Arkad displays a regionally unique climate with higher intra-annual stability, due in part to the influence of the southern monsoon. Despite this, the relative importance of environmental variables was highly differentiated among species, suggesting that characteristic variables such as coastal fog are not major cross-species predictors at this scale. CONCLUSIONS: The co-occurrence of a high number of endemic study species within a narrow monsoon-influenced region is indicative of a refugium with low climate change velocity. Combined with climate analysis, our findings provide strong evidence for a southern Arabian Pleistocene refugium in Oman's Central Desert. We suggest that this refugium has acted as an isolated temperate and mesic island in the desert, resulting in the evolution of these narrow-range endemic flora. Based on the composition of species, this system may represent the northernmost remnant of a continuous belt of mesic vegetation formerly ranging from Africa to Asia, with close links to the flora of East Africa. This has significant implications for future conservation of endemic plants in an arid biodiversity hotspot.
Asunto(s)
Filogenia , Plantas , África , África Oriental , Arabia , Asia , Islas , Clima TropicalRESUMEN
Major botanical and scientific references currently identify two species of frankincense, Boswellia carterii and Boswellia sacra, as being synonymous. We evaluated the Somalian (B. carterii) and Omani/Yemeni (B. sacra) species by chemical analyses to determine if there were any minor or major differences between the two species of frankincense. Components identified with their average percent for B. sacra are α-thujene (0.6%), α-pinene (68.2%), camphene (2.1%), sabinene (2.9%), ß-pinene (2.0%), myrcene (0.7%), limonene+ß-phellandrene (6.2%). Components identified with their average percent for B. carterii are α-thujene (7.9%), α-pinene (37.3%), camphene (0.8%), sabinene (4.9%), ß-pinene (1.8%), myrcene (7.3%), limonene+ß-phellandrene (14.4%). Initially, GC-MS analysis did not reveal major statistical differences. However, optical rotation values, B. Sacra (+30.1°) and B. carterii (-13.3°), demonstrated a greater significant difference. Enantiomeric ratio (+)/(-) values of α-pinene for B. sacra and B. carterii are 8.24 and 0.68, respectively, were also calculated aiding our conclusion that B. sacra and B. carterii are not synonymous but rather two distinct and individual frankincense species.