Plasma pharmacokinetics and lung distribution of tetrahydropalmatine after topical application of cold asthma recipe extract: Feishu (BL 13) versus Non-Feishu acupoint

Ethnopharmacological relevance

Acupoint application of cold asthma recipe (CAR) was a traditional Chinese medicine (TCM) method, widely used as an alternative medicine for clinical prevention of the common winter diseases of asthma and bronchitis. Tetrahydropalmatine (THP) was a main active ingredient of CAR extract. The aim of this study is to compare plasma pharmacokinetics and lung distribution of THP between Feishu (FS) acupoint (BL 13) and Non-Feishu (NFS) acupoint application of CAR extract by ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS).

Materials and methods

The extract of CAR was topically administrated in FS and NFS acupoint of rats for plasma pharmacokinetics, and topically administrated in FS and NFS acupoint of mice for lung distribution. The plasma and lung homogenates were pretreated by protein precipitation with acetonitrile. Chromatographic separation was performed on an ACQUITY UPLC BEH C18 column with a mobile phase consisted of 0.1% formic acid in acetonitrile and 0.1% formic acid in water. The detection was accomplished by multiple-reaction monitoring (MRM) scanning in the positive electrospray ionization (ESI⁺) mode. All pharmacokinetic parameters were estimated by non-compartmental analysis.

Results

A sensitive, accurate and precise UPLC-MS/MS method was successfully established for determination of THP in 100 μL plasma and lung homogenate. The lower limit of quantification (LLOQ) of THP was 0.05 ng/mL and 0.072 ng/mL, respectively. The pharmacokinetic results manifested that THP was absorbed and eliminated slowly in plasma. Additionally, it was found that there was significantly higher amount of THP absorbed into blood and lung after FS acupoint application compared to NFS acupoint application.

Conclusions

Both of the rat plasma pharmacokinetics and mice lung distribution of THP could support that FS acupoint application of CAR extract has greater advantages of absorption into the blood circulation and distribution in target tissue over NFS acupoint application. The results might be helpful in providing a rational explanation for why the TCM chose the acupoint application and elucidating the underlying mechanism of this treatment.     

The genus Anemarrhena Bunge: A review on ethnopharmacology,phytochemistry and pharmacology

Ethnopharmacological relevance

Anemarrhena asphodeloides Bunge. (Asparagaceae) yields Anemarrhenae Rhizoma, which has a long history to be used as a traditional medicine to treat various ailments, like cold-induced febrile disease with arthralgia, hematochezia, tidal fever and night sweats by Yin deficiency, bone-steaming, cough, and hemoptysis. It is also used as an ingredient of healthy food, wine, tea, biological toothpaste. Its importance is demonstrated by large scale to treat kinds of diseases in eastern Asian countries. The aim of this review is to provide up-to-date information about phytochemistry, pharmacology, and toxicology of Anemarrhena asphodeloides based on scientific literatures. It will build up a new foundation for further study on mechanism and development of better therapeutic agent and healthy product from Anemarrhena asphodeloides.

Material and methods

All the available information on Anemarrhena asphodeloides was collected via electronic search (using PubMed, SciFinder Scholar, CNKI, TPL (www.theplantlist.org), Google Scholar, Baidu Scholar, and Web of Science).

Results

Comprehensive analysis of the literatures searched through sources available above confirmed that the ethnomedical uses of Anemarrhena asphodeloides had been recorded in China, Japan, and Korea for thousands of years. The phytochemical investigation revealed the presence of steroidal saponins, flavonoids, phenylpropanoids, alkaloids, steroids, organic acids, anthraquinones, and others. Crude extracts and pure compounds from Anemarrhena asphodeloides exhibited significant pharmacological effects on the nervous system and the blood system. They also showed valuable bioactivities, such as antitumor, anti-oxidation, anti-microbial, anti-virus, anti-inflammation, anti-osteoporosis, anti-skin aging and damage as well as other activities.

Conclusions

In light of long traditional use and modern phytochemical and pharmacological studies summarized, Anemarrhena asphodeloides has demonstrated a strong potential for therapeutic and health-maintaining purposes. Both the extracts and chemical components isolated from the plant showed a wide range of biological activities. Thus more pharmacological mechanisms on main active compounds (TBII, TAIII, mangiferin and other ingredients) are necessary to be explored. In addition, as a good source of the traditional medicine, clinical studies of main therapeutic aspects (e.g. diabetes, Alzheimer?s disease, Parkinson?s disease, etc.), toxicity and adverse effect of Anemarrhena asphodeloides will also undoubtedly be the focus of future investigation.     

Topical analgesic,anti-inflammatory and antioxidant properties of Oxybaphus nyctagineus: Phytochemical characterization of active fractions

Ethnopharmacological relevance

Oxybaphus nyctagineus (Michx.) Sweet has traditionally been used by several Native American tribes predominantly as a topical anti-inflammatory and analgesic agent.

Aim of the study

To evaluate the antioxidant, analgesic and anti-inflammatory activity of the extracts prepared from the aerial parts of Oxybaphus nyctagineus and to characterize the major chemical constituents of the bioactive extracts.

Materials and methods

Crude polar and apolar extracts (PCE and ACE) of the herb of Oxybaphus nyctagineus were prepared and tested in the models of the CFA-induced hyperalgesia in rat knee and carrageenan-induced paw edema in rat. To identify the active compounds, subfractions were prepared by column chromatography and subjected in vitro assays, such as antioxidant assays (DPPH, peroxynitrite (ONOO⁻) scavenging), and the LPS-induced IL-1β release test in human monocytes. Preparative HPLC was employed for the isolation of active substances, while phytochemical analysis was performed by mean of LC–MS/MS and NMR.

Results

The topically administered PCE and ACE of Oxybaphus nyctagineus demonstrated a significant analgesic and anti-inflammatory effect in the inflammation animal models. The subfraction A4 of ACE and the subfraction P5 of PCE considerably inhibited the LPS-induced IL-1β release in human monocytes, while the strongest activity was localized in the subfraction P5 in the antioxidant assays. The HPLC–MS/MS and NMR analysis revealed that 6-methoxyflavonol diglycosides, namely patuletin-3-O-robinobioside (1), 6-methoxykaempferol-3-O-robinobioside (2), spinacetin-3-O-robinobioside (3), and hydroxy-polyenoic fatty acids, namely corchorifatty acid B (4), 9-hydroxy-10E,12Z,15Z-octadecatrienoic acid (9-HOT acid) (5), and 9-hydroxy-10E,12Z-octadecadienoic acid (9-HOD acid) (6) were present in PCE, and in ACE as major compounds.

Conclusion

The results of this study established a pharmacological evidence for the traditional use of Oxybaphus nyctagineus as an anti-inflammatory agent used topically, and provided data on its phytochemical composition for the first time.     

Antinociceptive and anti-inflammatory activities of extract and two isolated flavonoids of Carthamus tinctorius L

Ethnopharmacological relevance

Safflower (Carthamus tinctorius L.) has been long used both in the traditional system and folk medicine as an analgesic anti-inflammatory agent in China. The aim of the study was to evaluate the antinociceptive and anti-inflammatory activities of hydroalcoholic extract (HE) and two isolated kaempferol glycosides of Carthamus tinctorius L. to provide experimental evidence for its traditional use.

Materials and methods

Antinociceptive effects of HE, kaempferol 3-O-rutinoside (K-3-R) and kaempferol 3-O-glucoside (K-3-G) were assessed in mice using the acetic acid-induced writhing test, formalin test and cinnamaldehyde test. The anti-inflammatory effects of HE, K-3-R and K-3-G were determined in two animal models: carrageenan-induced paw edema and xylene-induced ear edema.

Results

The HPLC analysis showed the presence of K-3-R and K-3-G in Carthamus tinctorius L. HE (500 and 1000 mg/kg) as well as K-3-R and K-3-G (150, 300 and 600 mg/kg) produced significant inhibition on nociception induced by acetic acid and formalin. Oral treatment of HE, K-3-R and K-3-G at all doses significantly reduced both the nociceptive response and cinnamaldehyde-induced paw edema, effect that was superior to aspirin. In anti-inflammatory tests, HE and K-3-G significantly inhibited the paw edema during the both phases of carrageenan-induced inflammation while K-3-G suppressed the late phase inflammation only. HE (400 and 800 mg/kg) and K-3-G (200, 400, 800 mg/kg) produced significant dose-dependent inhibition of xylene-induced ear edema development. K-3-R only suppressed ear edema formation at a high dose (800 mg/kg).

Conclusions

These results demonstrate that Carthamus tinctorius L. extract possess remarkable antinociceptive and anti-inflammatory activities which may be due to K-3-R and K-3-G at least in part, supporting the folkloric usage of the plant to treat various inflammatory and pain diseases.     

Botany,traditional uses,phytochemistry and pharmacology of Waltheria indica L. (syn. Waltheria americana): A review

Ethnopharmacological relevance

Waltheria indica L. (syn. Waltheria americana) is commonly used in traditional medicine in Africa, South America and Hawaii, mainly against pain, inflammation, conditions of inflammation, diarrhea, dysentery, conjunctivitis, wounds, abscess, epilepsy, convulsions, anemia, erectile dysfunctions, bladder ailments and asthma. Aim of the review to provide an up-to-date overview of the botany, phytochemistry, traditional uses, pharmacological activities and toxicity data of Waltheria indica. Additionally, studies providing an evidence for local and traditional uses of Waltheria indica are discussed. Further phytochemical and pharmacological potential of this species are suggested for future investigations.

Materials and methods

The information was collected from scientific journals, books, theses and reports via academic libraries and electronic search. These sources include Pubmed, Web of Science, Portal de Portales-Latindex, Science Research.com and Google scholar. These studies about the medical botanical, traditional uses, chemical, pharmacological and toxicological data on Waltheria indica were published in English, Portuguese, Spanish, German and French.

Results

Crude extracts and isolated compounds from Waltheria indica were investigated and showed analgesic, anti-inflammatory, antibacterial, antifungal, antimalarial, anti-anemic, anti-oxidant, sedative and anticonvulsant activities. The phytochemical investigations showed the presence of cyclopeptid alkaloids, flavonoids (e.g., (–)-epicatechin, quercetin, kaempferol, kaempferol-3-O-β-d-(6″-E-p-coumaryl)-glucopyranoside), tannins, sterols, terpenes, saponins, anthraquinones. Studies of acute toxicity in animal indicated that Waltheria indica can be toxic.

Conclusion

Waltheria indica possess therapeutic potential in the treatment of inflammation, malaria, infectious diseases (e.g., lungs infection due to Klebsiella pneumoniae, diarrhea due to Candida albicans or Escherichia coli) and prevention of oxidative stress. Further studies are necessary to explore pure compounds responsible for the pharmacological effects and the mechanisms of action. Further investigations are also needed to provide an evidence base for traditional uses of this species against pain, anemia, convulsions and epilepsy. In addition, there is a pressing need to investigate the other traditional uses such as dysentery, syphilis, erectile dysfunctions and asthma.