Xirui He

Eucommia ulmoides Oliv.: Ethnopharmacology, phytochemistry and pharmacology of an important traditional Chinese medicine

ETHNOPHARMACOLOGICAL RELEVANCE Eucommia ulmoides Oliv. (Family Eucommiaceae), also known as Dù-zhòng (Chinese: ), Tuchong (in Japanese), is the sole species of the genus Eucommia. The leaf, stem, and bark as well as staminate flower of Eucommia ulmoides have been traditionally used to cure many diseases in China, Japan, Korea, among others. The aim of this review is to comprehensively outline the botanical description, ethnopharmacology, phytochemistry, biological activities, and toxicology of Eucommia ulmoides and to discuss possible trends for further study of Eucommia ulmoides. MATERIALS AND METHODS Information on Eucommia ulmoides was gathered via the internet (using Pub Med, Elsevier, Baidu Scholar, Google Scholar, Medline Plus, ACS, CNKI, and Web of Science) and from books in local libraries. RESULTS One-hundred twelve compounds of Eucommia ulmoides, including the main active constituents, lignans and iridoids, have been isolated and identified. In vitro and in vivo studies indicated that monomer compounds and extracts from Eucommia ulmoides possess wide-ranging pharmacological actions, especially in treating hypertension, hyperlipemia, diabetes, obesity, sexual dysfunction, osteoporosis, Alzheimers disease, aging, lupus-like syndrome, and immunoregulation. CONCLUSIONS Eucommia ulmoides has been used as a source of traditional medicine and as a beneficial health food. Phytochemical and pharmacological studies of Eucommia ulmoides have received much interest, and extracts and active compounds continue to be isolated and proven to exert various effects. Further toxicity and clinical studies are warranted to establish more detailed data on crude extracts and pure compounds, enabling more convenient preparations for patients. Therefore, this review on the ethnopharmacology, phytochemistry, biological activities, and toxicity of Eucommia ulmoides will provide helpful data for further studies as well as the commercial exploitation of this traditional medicine.

Structures, biological activities, and industrial applications of the polysaccharides from Hericium erinaceus (Lion’s Mane) mushroom: A review

Hericium erinaceus (Bull.) Pers., also known as Yamabushitake, Houtou and Lions Mane, is capable of fortifying the spleen and nourishing the stomach, tranquilizing the mind, and fighting cancer. Over the past decade, it has been demonstrated that H. erinaceus polysaccharides possess various promising bioactivities, including antitumor and immunomodulation, anti-gastric ulcer, neuroprotection and neuroregeneration, anti-oxidation and hepatoprotection, anti-hyperlipidemia, anti-hyperglycemia, anti-fatigue and anti-aging. The purpose of the present review is to provide systematically reorganized information on extraction and purification, structure characteristics, biological activities, and industrial applications of H. erinaceus polysaccharides to support their therapeutic potentials and sanitarian functions.

Bletilla striata: Medicinal uses, phytochemistry and pharmacological activities

ETHNOPHARMACOLOGICAL RELEVANCE Bletilla striata (Thunb.) Reichb. f. (Orchidaceae), also known as Hyacinth Orchid and Baiji (Simplified Chinese: ), not only has been widely used for the treatment of hematemesis, hemoptysis, and traumatic bleeding due to the efficacy of arresting bleeding with astringent action, but also has been applied topically to overcome ulcers, sores, swellings, and chapped skin due to the efficacy of dispersing swelling and promoting tissue regeneration. Additional medical applications include the treatment of tuberculosis, malignant ulcers, hemorrhoids, anthrax, eye diseases, and silicosis. AIM OF THIS REVIEW This review aims to provide up-to-date information on the botanical characterization, medicinal uses, chemical constituents, pharmacological activities, and toxicity of B. striata. In addition, this paper also focuses on the possible exploitation of this plant for the treatment of different diseases, and uncovers opportunities for future research. MATERIALS AND METHODS The relevant information on B. striata was gathered from worldwide accepted scientific databases via an electronic search (Google Scholar, Web of Science, ScienceDirect, ACS Publications, PubMed, Wiley Online Library, SciFinder, CNKI). Information was also obtained from The Plant List, Chinese pharmacopoeia, Chinese herbal classics books, PhD and MSc dissertations, etc. RESULTS A comprehensive analysis of the literature obtained through the above-mentioned sources confirmed that the ethnomedical usages of B. striata have been recorded in Mongolia, Korea, Japan, and China. Phytochemical investigations revealed that the major chemical constituents of B. striata are polysaccharides, bibenzyls, phenanthrenes, triterpenoids and its saponins, steroids and its saponins, which also have been proven to be the main bioactive substances capable of exhibiting numerous pharmacological activities including wound healing, antiulcer, hemostasis, cytotoxicity, antimicrobial, anti-inflammation, anti-oxidation, immunomodulation, anti-fibrosis, antiaging, anti-allergy, and anti-itch. CONCLUSIONS Preliminary investigations on pharmacological properties of B. striata have shown that B. striata is an outstanding astringent hemostatic medicinal, B. striata polysaccharides (BSP) as the major bioactive components not only capable of promoting wound healing, but also show good performance as a kind of promising natural biomaterial. More importantly, BSP are also reported to be excellent embolic material. However, further investigations need to be carried out to fully clarify its efficacy of dispersing swelling and promoting tissue regeneration. Moreover, this plant also needs a lot more investigations to clarify the pathways of absorption, distribution, metabolism and excretion, and to evaluate its long-term in vivo chronic toxicity before proceeding to the development of pharmaceutical formulation.

Phytochemistry and Pharmacology of the Genus Pedicularis Used in Traditional Chinese Medicine

In the present review, the literature data on the chemical constituents and biological investigations of the genus Pedicularis are summarized. Some species of Pedicularis have been widely applied in traditional Chinese medicine. A wide range of chemical components including iridoid glycosides, phenylpropanoid glycosides (PhGs), lignans glycosides, flavonoids, alkaloids and other compounds have been isolated and identified from the genus Pedicularis. In vitro and in vivo studies indicated some monomer compounds and extracts from the genus Pedicularis have been found to possess antitumor, hepatoprotective, anti-oxidative, antihaemolysis, antibacterial activity, fatigue relief of skeletal muscle, nootropic effect and other activities.

The genus Achyranthes: A review on traditional uses, phytochemistry, and pharmacological activities

ETHNOPHARMACOLOGICAL RELEVANCE Achyranthes L. (Amaranthaceae), also known as Chaff Flower and Niuxi/, mainly includes two famous medicinal species namely A. bidentata and A. aspera. A. bidentata has been widely used as blood-activating and stasis-resolving medicine for the treatment of various diseases including amenorrhea, dysmenorrhea, lumbago, gonalgia, paraplegia, edema, stranguria, headache, dizziness, odontalgia, oral ulcer, hematemesis, and epistaxis. A. aspera has been widely used to treat various diseases, including gynecological disorder, asthma, ophthalmia, odontalgia, haemorrhoids, and abdominal tumor, and has been applied to difficult labour, wound healing, insect and snake bites. AIM OF THIS REVIEW This review aims to provide systematically reorganized information on distributions, botanical characteristics, ethnopharmacology, chemical constituents, qualitative and quantitative analysis, pharmacological activities, and toxicity of Achyranthes species to support their therapeutic potential. MATERIALS AND METHODS The relevant information on Achyranthes species was gathered from worldwide accepted scientific databases via electronic search (Google Scholar, Web of Science, ScienceDirect, ACS Publications, PubMed, Wiley Online Library, SciFinder, CNKI). Information was also obtained from International Plant Names Index, Chinese Pharmacopoeia, Chinese herbal classic books, PhD and MSc dissertations, etc. RESULTS A comprehensive analysis of literatures obtained through the above- mentioned sources confirms that the ethnomedicinal uses of Achyranthes species are mainly recorded in China, India, Korea, Pakistan, Ethiopia, Kenya, Sri Lanka, Bangladesh, Philippines, etc. Phytochemical investigations revealed that the major bioactive substances of Achyranthes plants are polysaccharides, polypeptides, triterpenoid saponins, and ketosteroids. Achyranthes plants have been shown to not only act on immune system, nervous system, bone metabolism, and reproduction, but also possess a wide range of biological activities, including blood-activating, anti-tumor, anti-inflammation, anti-arthritis, anti-oxidation, anti-aging, wound healing, etc. Toxicity studies indicated that A. bidentata and A. aspera seem non-toxic at the common therapeutic doses. CONCLUSIONS A. bidentata and A. aspera are very promising to be fully utilized in the development of nutraceutical and pharmaceutical products. There are, however, needs for further in-depth studies to confirm some ethnomedicinal uses of Achyranthes plants and to elucidate the scientific connotation of the widely documented property of conducting drug downward of A. bidentata. In addition, other widespread Achyranthes species like A. japonica and A. rubrofusca ought to be studied. Likewise, systematic comparative studies of the chemical constituents of medicinal Achyranthes plants resources with the same local name are also needed. Furthermore, not only should the investigations on the structure-activity relationship of the main bioactive compounds triterpenoid saponins and ketosteroids be carried out, but the pathways of absorption, distribution, metabolism, and excretion ought to be clarified. Last but not least, there is also a need to evaluate the long-term chronic toxicity and acute toxicity in vivo of the main bioactive compounds.

Structures, bioactivities and future prospective of polysaccharides from Morus alba (white mulberry): A review

Morus alba L. (family Moreaceae), also known as white mulberry, is distinguished as a source of highly promising traditional medicines (including Mori Folium, Mori Fructus, Mori Ramulus and Mori Cortex) and also functional foods. Over the past two decades, the vast majority of the studies with regard to the isolation and bioactivities of M. alba polysaccharides have mainly focused on its leaves and fruits, which are both medicinal and edible. The tender M. alba leaf is edible and can be used to make tea, the mature M. alba fruit is sweet and juicy. M. alba fruits and leaves contain rich bioactive polysaccharides, which are shown to possess various promising bioactivities, mainly including antidiabetic, immunomodulation, anti-inflammation, antioxidation, anti-obesity, hepatoprotection and renoprotection. The main purpose of this review is to provide systematically reorganized information on structural characteristics and bioactivities of M. alba polysaccharides to support their further therapeutic potentials and sanitarian functions.

Traditional Uses, Chemical Constituents and Biological Activities of Plants from the Genus Sanguisorba L.

Plants from the genus Sanguisorba have been treated as medicinal ingredients for over 2000 years. This paper reviews advances in the botanical, phytochemical and pharmacological studies of the genus. To date, more than 120 chemical constituents have been isolated and identified from these plants, especially from S. officinalis and S. minor. Among these compounds, triterpenoids, phenols and flavonoids are the primary biologically active constituents. Triterpenoids can be used as quality control markers to determine the quality of medicinal materials and their preparations. In vivo and in vitro studies have shown that plants from the genus Sanguisorba exhibit a wide range of pharmacological properties, including hemostatic, antibacterial, antitumor, neuroprotective and hypoglycemic activities. In Chinese medical practice, many drugs (e.g., tablets and powders) that contain S. officinalis roots have been used to treat leukopenia, hemorrhaging and burns. However, there is still a multitude of Sanguisorba species that have garnered little or no attention. Indeed, there are few reports concerning the clinical use and toxic effects of these plants. Further attention should be focused on the study of these species in order to gather information on their respective toxicology data, any relevant quality-control measures, and the clinical value of the crude extracts, active compounds, and bioactive metabolites from Genus Sanguisorba.

Design, Synthesis and Evaluation of Novel 2-Hydroxypyrrolobenzodiazepine-5,11-dione Analogues as Potent Angiotensin Converting Enzyme (ACE) Inhibitors

Under the guidance of combination of traditional Chinese medicine chemistry (CTCMC), this study describes the preparation of a phenolic acid/dipeptide/borneol hybrid consisting of phenolic acid and a bornyl moiety connected to the dipeptide N-terminal and C-terminal respectively. It also evaluates their angiotensin converting enzyme (ACE) inhibitory and synergistic antihypertensive activities. Briefly, a series of novel phenolic acid/dipeptide/borneol hybrids were prepared and investigated for their ability to inhibit ACE. The influence of the phenolic acid and bornyl moiety on subsite selectivity is also demonstrated. Among all the new compounds, two compounds—7a and 7g—reveal good inhibition potency in in vitro ACE-inhibitory tests. Interestingly, favorable binding results in molecular docking studies also supported the in vitro results. Additionally, the bioassay showed that oral administration of the two compounds displayed high and long-lasting antihypertensive activity both in acute antihypertensive tests and in therapeutic antihypertensive tests by non-invasive blood pressure measurements in spontaneously hypertensive rats.Under the guidance of combination of traditional Chinese medicine chemistry (CTCMC), this study describes the preparation of a phenolic acid/dipeptide/borneol hybrid consisting of phenolic acid and a bornyl moiety connected to the dipeptide N-terminal and C-terminal respectively. It also evaluates their angiotensin converting enzyme (ACE) inhibitory and synergistic antihypertensive activities. Briefly, a series of novel 2-hydroxypyrrolobenzodiazepine-5,11-dione analogues were prepared and investigated for their ability to inhibit ACE. The influence of the phenolic acid and bornyl moiety on subsite selectivity is also demonstrated. Among all the new compounds, two compounds-7a and 7g-reveal good inhibition potency in in vitro ACE-inhibitory tests. Interestingly, favorable binding results in molecular docking studies also supported the in vitro results. Additionally, the bioassay showed that oral administration of the two compounds displayed high and long-lasting antihypertensive activity both in acute antihypertensive tests and in therapeutic antihypertensive tests by non-invasive blood pressure measurements in spontaneously hypertensive rats.

Anticonvulsant Activities of α-Asaronol ((E)-3′-hydroxyasarone), an Active Constituent Derived from α-Asarone

BACKGROUND Epilepsy is one of chronic neurological disorders that affects 0.5-1.0% of the worlds population during their lifetime. There is a still significant need to develop novel anticonvulsant drugs that possess superior efficacy, broad spectrum of activities and good safety profile. METHODS α-Asaronol and two current antiseizure drugs (α-asarone and carbamazepine (CBZ)) were assessed by in vivo anticonvulsant screening with the three most employed standard animal seizure models, including maximal electroshock seizure (MES), subcutaneous injection-pentylenetetrazole (PTZ)-induced seizures and 3-mercaptopropionic acid (3-MP)-induced seizures in mice. Considering drug safety evaluation, acute neurotoxicity was assessed with minimal motor impairment screening determined in the rotarod test, and acute toxicity was also detected in mice. RESULTS In our results, α-asaronol displayed a broad spectrum of anticonvulsant activity (ACA) and showed better protective indexes (PI = 11.11 in MES, PI = 8.68 in PTZ) and lower acute toxicity (LD50 = 2940 mg/kg) than its metabolic parent compound (α-asarone). Additionally, α-asaronol displayed a prominent anticonvulsant profile with ED50 values of 62.02 mg/kg in the MES and 79.45 mg/kg in the sc-PTZ screen as compared with stiripentol of ED50 of 240 mg/kg and 115 mg/kg in the relevant test, respectively. CONCLUSION The results of the present study revealed α-asaronol can be developed as a novel molecular in the search for safer and efficient anticonvulsants having neuroprotective effects as well as low toxicity. Meanwhile, the results also suggested that α-asaronol has great potential to develop into another new aromatic allylic alcohols type anticonvulsant drug for add-on therapy of Dravets syndrome.

Recent advances in polysaccharides from Ophiopogon japonicus and Liriope spicata var. prolifera

O. japonicus and L. spicata var. prolifera are distinguished as sources of highly promising yin-tonifying medicinals, namely Ophiopogonis Radix and Liriopes Radix. Liriopes Radix is generally medicinally used as a substitute for Ophiopogonis Radix in various prescriptions due to their extremely similar nature. Ophiopogonis Radix and Liriopes Radix are both very rich in bioactive polysaccharides, especially β‑fructans. Over the past twelve years, except for work on physical entrapment and chemical modification of obtained β‑fructans, the vast majority of studies are carried out to investigate the bioactivities of O. japonicus polysaccharides (OJP) and L. spicata var. prolifera polysaccharides (LSP), mainly including anti-diabetes, immunomodulation, anti-inflammation, antioxidation, anti-obesity, cardiovascular protection, etc. In addition, OJP and LSP are considered to have the potential to regulate intestinal flora. The main purpose of this review is to provide systematically reorganized information on structural characteristics and bioactivities of OJP and LSP to support their further therapeutic potentials and sanitarian functions.