Preparation, In Vitro and In Vivo Evaluation of Nanoemulsion In Situ Gel for Transnasal Delivery of Traditional Chinese Medicine Volatile Oil from Ligusticum sinense Oliv.cv. Chaxiong.

Ischemic stroke is a difficult-to-treat brain disease that may be attributed to a limited therapeutic time window and lack of effective clinical drugs. Nasal-brain administration is characterized by low systemic toxicity and is a direct and non-invasive brain targeting route. Preliminary studies have shown that the volatile oil of Chaxiong (VOC) has an obvious anti-ischemic stroke effect. In this work, we designed a nanoemulsion thermosensitive in situ gel (VOC-NE-ISG) loaded with volatile oil of Chaxiong for ischemia via intranasal delivery to rat brain treatment of cerebral ischemic stroke. The developed VOC-NE-ISG formulation has a suitable particle size of 21.02 ± 0.25 nm and a zeta potential of -20.4 ± 1.47 mV, with good gelling ability and prolonged release of the five components of VOC. The results of in vivo pharmacokinetic studies and brain targeting studies showed that intranasal administration of VOC-NE-ISG could significantly improve the bioavailability and had excellent brain-targeting efficacy of nasal-to-brain delivery. In addition, the results of pharmacodynamics experiments showed that both VOC-NE and VOC-NE-ISG could reduce the neurological deficit score of model rats, reducing the size of cerebral infarction, with a significant effect on improving ischemic stroke. Overall, VOC-NE-ISG may be a promising intranasal nanomedicine for the effective treatment of ischemic stroke.

Novel phthalide dimers from the aerial parts of Ligusticum sinense Oliv cv. Chaxiong.

Five new phthalide dimers, chaxiongnolides C-G (1-5), the two enantiomers of riligustilide (6a and 6b) and tokinolide B (7) were isolated from the aerial parts of Ligusticum sinense Oliv cv. Chaxiong. The structures of 1-5 were elucidated through extensive spectroscopic analysis, and the relative configurations of compounds 2 and 3 were further confirmed by an X-ray diffraction experiment. The absolute configurations of 1-3 were assigned by comparing calculated and experimental ECD spectra. The ECD exciton chirality method was used to confirm the absolute configurations of compounds 4, 5, 6a and 6b. Compounds 1-3 are the first dimeric phthalides to be reported that are comprising a sedanolide unit. The compounds were evaluated in vitro for their cytotoxic activity against select human cell lines.

New dimeric phthalides from Ligusticum sinense Oliv cv. Chaxiong.

A new dimeric phthalide, chaxiongnolide A (1), and a new natural product, chaxiongnolide B (2), together with a known compound Z-ligustilide (3), were isolated from the rhizome of Ligusticum sinense Oliv cv. Chaxiong. Their structures were elucidated by various spectroscopic methods and confirmed by X-ray crystallographic analysis.

Bioactive phthalides from Ligusticum sinense Oliv cv. Chaxiong.

Five new phthalides (1-4, 6), two new natural products (5, 7) and five known phthalides (8-12) were isolated from the aerial parts of Ligusticum sinense Oliv cv. Chaxiong. Their structures were elucidated by HR-ESI-MS, UV, IR, 1D and 2D NMR (HSQC, HMBC, (1)H-(1)H COSY, NOESY) methods. The absolute configurations were established by the circular dichroism (CD) spectrum and the modified Mosher's method. Compounds 1-8 were tested against SK-N-SH cell depriving oxygen and glucose and showed different degrees of increasing the cell survival, among which compounds 1, 4 and 8 (10 µM) showed higher cell survival than Ginsenoside Rg1.

Chemical constituents from aerial parts of Ligusticum sinense cv. chaxiong / 中草药

Objective: To study the chemical constituents from the aerial parts of Ligusticum sinense cv. chaxiong. Methods: The chemical constituents were separated and purified by silica gel, ODS column chromatography, and preparative HPLC. Their structures were determined by various of spectroscopic analyses. Results: Fourteen compounds were isolated from the petrol ester and CH2Cl2 fractions of 95% ethanol extract of the aerial parts of L. sinense cv. chaxiong, and their structures were identified as 5-hydroxy-3- butylphthalide (1), 3-hydroxy-octa-1, 5-dien-7-one (2), umbelliferone (3), pumbinernoid A (4), crocinervolide (5), (3R, 6R, 7E)-3- hydroxy-4, 7-megastignadien-9-one (6), senkyunolide G (7), scopoletin (8), (2Z)-3-(3, 4-dihydroxyphenyl)-2-propenal (9), (3S, 5R, 6S, 7E, 9R)-5, 6-epoxy-3, 9-dihydroxy-7-megastigmene (10), vomifoliol (11), dihydroactinidiolide (12), 7-hydroxy-3-butylphthalide (13), and senkyunolide A (14). Conclusion: Compounds 1-13 are isolated from this plant for the first time, compounds 1, 2, 4-6, and 9-13 are found from the plants of genus Ligusticum L. for the first time, and compound 1 is a new natural product.

Comparison with differentiation of Ligusticum chuanxiong from its easily confusable Ligusticum sinense chaxiong / 中草药

Object　To provide a scientific basis for the identification and rational clinical use of the two herbal drugs. Methods　Experiments were carried out by comparing their properties, microscopic characteristics, UV spectra, TLC and GC chromatograms. Results　There are remarkable differences between the two crude drugs in these respects, and a convenient and effective method for their differentiation and identification has been established. Conclusion　Ligusticum sinense Hort. and Ligusticum sinense Oliv. cv. chaxiong Mass should not be used one instead of the other.

Comparison with differentiation of Ligusticum chuanxiong from its easily confusable Ligusticum sinense chaxiong / 中草药

Object To provide a scientific basis for the identification and rational clinical use of the two herbal drugs Methods Experiments were carried out by comparing their properties, microscopic characteristics, UV spectra, TLC and GC chromatograms Results There are remarkable differences between the two crude drugs in these respects, and a convenient and effective method for their differentiation and identification has been established Conclusion Ligusticum sinense Hort and Ligusticum sinense Oliv cv chaxiong Mass should not be used one instead of the other