Objective: To isolate bioactive compounds from the endophytic fungus Fusarium sporotrichioides isolated from Rauwolfia yunnanensis, and investigate their pharmacological activities.Methods: The chemical constituents w...Objective: To isolate bioactive compounds from the endophytic fungus Fusarium sporotrichioides isolated from Rauwolfia yunnanensis, and investigate their pharmacological activities.Methods: The chemical constituents were isolated and purified by combining with ODS column chromatography, silica gel column chromatography and by performing semipreparative HPLC. Their structures were established on the basis of 1D NMR(1H-NMR and13C-NMR) and 2D NMR(1H–1H COSY,HSQC, HMBC and NOESY), as well as HRESIMS and comparison with literature data. In addition, the absolute configuration of compound 1 was determined by calculated ECD data.Results: One previously undescribed tetracyclic triterpenoid derivative, named as integracide L(1), 12aacetoxy-4,4-dimethyl-24-methylene-5a-cholesta-8,14-diene-2a,3β,11β-triol(2), 12a-acetoxy-4,4-dime thyl-24-methylene-5a-cholesta-8-momoene-2a,3β,11β-triol(3), 12a-acetoxy-4,4-dimethyl-24-methy lene-5a-cholesta-8,14-diene-3β,11β-triol(4), and 12a-acetoxy-4,4-dimethyl-24-methylene-5acholesta-8-momoene-3β,11β-triol(5) were isolated from F. sporotrichioide. Moreover, compound 1 was rare tetracyclic triterpenoid with single methyl replacement at C-4 position.Conclusion: Compound 1 was a new tetracyclic triterpenoid isolated from the endophytic fungus F.sporotrichioides. In addition, compound 2 could inhibit the growth of three different human cancer cells significantly. Compounds 3 and 5 were found to possess better cytotoxic activities on Hep G-2 cells than the other compounds, with IC50values of(2.8 ± 0.1) and(6.3 ± 0.3) μmol/L respectively.展开更多
Bottle gourd (Lagenaria siceraria), colloquially known as “lauki” or “doodhi” in India, is an edible plant in the Cucurbitaceae family. Consumption of raw bottle gourd juice is common practice in India. However, l...Bottle gourd (Lagenaria siceraria), colloquially known as “lauki” or “doodhi” in India, is an edible plant in the Cucurbitaceae family. Consumption of raw bottle gourd juice is common practice in India. However, little known is the fact that ingestion of raw bottle gourd juice that is extremely bitter tasting is associated with cucurbitacin toxicity. Cucurbitacin is a pheromone produced by the plant as a defense mechanism against insects and herbivores. It is responsible for imparting the bitter taste, and the associated toxicity. The exact mechanism of cucurbitacin toxicity is not well understood, however it is suspected to result in gastric erosions and increased capillary permeability, resulting in rapid onset of vomiting, diarrhea, gastrointestinal bleeding, hypotension and shock. As serum and urine concentration measurements of cucurbitacin are not readily available, bottle gourd toxicity remains a clinical diagnosis based largely on the temporal association of ingestion of unusually bitter tasting vegetable or its juice with rapid onset of symptoms. Physician awareness is therefore of paramount importance in the diagnosis of this unusual entity. We present the case of a 78-year-old woman, with no comorbid conditions, who presented to the Emergency Department (ED) with three episodes of vomiting and multiple episodes of watery loose stools soon after ingestion of extremely bitter tasting, fresh bottle gourd juice. A prompt diagnosis of cucurbitacin toxicity was made in the ED and fluid resuscitation was commenced expeditiously. However, it was noted that most physicians were unfamiliar with this entity, and therefore skeptical of the diagnosis. Our rationale in presenting this clinical case report is three-fold: 1) To create physician awareness regarding this unique clinical entity, especially among emergency physicians, as they are the first point of contact for a critically ill patient. 2) To highlight the rapid onset and progression of symptoms in cucurbitacin toxicity. 3) To emphasize aggressive fluid resuscitation and symptomatic management as the mainstay of clinical treatment.展开更多
基金funded by Outstanding Youth Foundation of Heilongjiang province(NO.YQ2021H009).
文摘Objective: To isolate bioactive compounds from the endophytic fungus Fusarium sporotrichioides isolated from Rauwolfia yunnanensis, and investigate their pharmacological activities.Methods: The chemical constituents were isolated and purified by combining with ODS column chromatography, silica gel column chromatography and by performing semipreparative HPLC. Their structures were established on the basis of 1D NMR(1H-NMR and13C-NMR) and 2D NMR(1H–1H COSY,HSQC, HMBC and NOESY), as well as HRESIMS and comparison with literature data. In addition, the absolute configuration of compound 1 was determined by calculated ECD data.Results: One previously undescribed tetracyclic triterpenoid derivative, named as integracide L(1), 12aacetoxy-4,4-dimethyl-24-methylene-5a-cholesta-8,14-diene-2a,3β,11β-triol(2), 12a-acetoxy-4,4-dime thyl-24-methylene-5a-cholesta-8-momoene-2a,3β,11β-triol(3), 12a-acetoxy-4,4-dimethyl-24-methy lene-5a-cholesta-8,14-diene-3β,11β-triol(4), and 12a-acetoxy-4,4-dimethyl-24-methylene-5acholesta-8-momoene-3β,11β-triol(5) were isolated from F. sporotrichioide. Moreover, compound 1 was rare tetracyclic triterpenoid with single methyl replacement at C-4 position.Conclusion: Compound 1 was a new tetracyclic triterpenoid isolated from the endophytic fungus F.sporotrichioides. In addition, compound 2 could inhibit the growth of three different human cancer cells significantly. Compounds 3 and 5 were found to possess better cytotoxic activities on Hep G-2 cells than the other compounds, with IC50values of(2.8 ± 0.1) and(6.3 ± 0.3) μmol/L respectively.
文摘Bottle gourd (Lagenaria siceraria), colloquially known as “lauki” or “doodhi” in India, is an edible plant in the Cucurbitaceae family. Consumption of raw bottle gourd juice is common practice in India. However, little known is the fact that ingestion of raw bottle gourd juice that is extremely bitter tasting is associated with cucurbitacin toxicity. Cucurbitacin is a pheromone produced by the plant as a defense mechanism against insects and herbivores. It is responsible for imparting the bitter taste, and the associated toxicity. The exact mechanism of cucurbitacin toxicity is not well understood, however it is suspected to result in gastric erosions and increased capillary permeability, resulting in rapid onset of vomiting, diarrhea, gastrointestinal bleeding, hypotension and shock. As serum and urine concentration measurements of cucurbitacin are not readily available, bottle gourd toxicity remains a clinical diagnosis based largely on the temporal association of ingestion of unusually bitter tasting vegetable or its juice with rapid onset of symptoms. Physician awareness is therefore of paramount importance in the diagnosis of this unusual entity. We present the case of a 78-year-old woman, with no comorbid conditions, who presented to the Emergency Department (ED) with three episodes of vomiting and multiple episodes of watery loose stools soon after ingestion of extremely bitter tasting, fresh bottle gourd juice. A prompt diagnosis of cucurbitacin toxicity was made in the ED and fluid resuscitation was commenced expeditiously. However, it was noted that most physicians were unfamiliar with this entity, and therefore skeptical of the diagnosis. Our rationale in presenting this clinical case report is three-fold: 1) To create physician awareness regarding this unique clinical entity, especially among emergency physicians, as they are the first point of contact for a critically ill patient. 2) To highlight the rapid onset and progression of symptoms in cucurbitacin toxicity. 3) To emphasize aggressive fluid resuscitation and symptomatic management as the mainstay of clinical treatment.