[Essence of acupoints and meridians based on the studies of myofascial trigger points].

Based on the modern anatomy and physiology, the referred pain of myofascial trigger points of each muscle is integrated; compared with the twelve meridians as well as conception vessel and governor vessel, the similarity of their position and running course is observed. With the current research progress of myofascial trigger points and fasciology, based on the running course of referred pain of trigger points, combined with fascia mechanics, nerve and vascular, the location of acupoints and meridians, as well as the relationship between acupoints and meridians, are discussed.

Discovery of Novel Substituted N-(4-Amino-2-chlorophenyl)-5-chloro-2-hydroxybenzamide Analogues as Potent Human Adenovirus Inhibitors.

An effective therapy for human adenovirus (HAdV) infections in immunocompromised patients and healthy individuals with community-acquired pneumonia remains an unmet medical need. We herein reported a series of novel substituted N-(4-amino-2-chlorophenyl)-5-chloro-2-hydroxybenzamide analogues as potent HAdV inhibitors. Compounds 6, 15, 29, 40, 43, 46, 47, and 54 exhibited increased selectivity indexes (SI > 100) compared to the lead compound niclosamide, while maintaining sub-micromolar to low micromolar potency against HAdV. The preliminary mechanistic studies indicated that compounds 6 and 43 possibly target the HAdV DNA replication process, while compounds 46 and 47 suppress later steps of HAdV life cycle. Notably, among these derivatives, compound 15 showed improved anti-HAdV activity (IC50 = 0.27 µM), significantly decreased cytotoxicity (CC50 = 156.8 µM), and low in vivo toxicity (maximum tolerated dose = 150 mg/kg in hamster) as compared with niclosamide, supporting its further in vivo efficacy studies for the treatment of HAdV infections.

Design, Synthesis, and Biological Evaluation of Substituted 4,6-Dihydrospiro[[1,2,3]triazolo[4,5-b]pyridine-7,3'-indoline]-2',5(3H)-dione Analogues as Potent NS4B Inhibitors for the Treatment of Dengue Virus Infection.

A series of substituted 4,6-dihydrospiro[[1,2,3]triazolo[4,5-b]pyridine-7,3'-indoline]-2',5(3H)-dione analogues were synthesized and evaluated as potent dengue virus inhibitors. Throughout a structure-activity relationship exploration on the amide of the indolone moiety, a wide range of substitutions were found to be well tolerated for chemical optimization at this position. Among these compounds, 15 (JMX0254) displayed the most potent and broad inhibitory activities, effective against DENV-1 to -3 with EC50 values of 0.78, 0.16, and 0.035 µM, respectively, while compounds 16, 21, 27-29, 47, and 70 exhibited relatively moderate to high activities with low micromolar to nanomolar potency against all four serotypes. The biotinylated compound 73 enriched NS4B protein from cell lysates in pull-down studies, and the findings together with the mutation investigations further validated dengue NS4B protein as the target of this class of compounds. More importantly, compound 15 exhibited good in vivo pharmacokinetic properties and efficacy in the A129 mouse model, indicating its therapeutic potential against the dengue virus infection as a drug candidate for further preclinical development.

Therapeutic Potential of Oridonin and Its Analogs: From Anticancer and Antiinflammation to Neuroprotection.

Oridonin, a diterpenoid natural product commonly used in East Asian herbal medicine, is garnering increased attention in the biomedical community due to its extensive biological activities that include antitumor, anti-inflammatory, antimicrobial, hepatic fibrosis prevention, and neurological effects. Over the past decade, significant progress has been made in structure activity relationship and mechanism of action studies of oridonin for the treatment of cancer and other diseases. This review provides a brief summary on oridonin and its analogs in cancer drug discovery and antiinflammation and highlights its emerging therapeutic potential in neuroprotection applications.

[Post-stroke unilateral spatial neglect treated with acupuncture and rehabilitation: a randomized controlled trial].

OBJECTIVE: To observe the impacts on post-stroke unilateral spatial neglect treated with acupuncture for "regaining consciousness, benefiting marrow and opening orifices" and rehabilitation. METHODS: Forty patients of post-stroke unilateral spatial neglect were randomized into an observation group and a control group, 20 cases in each one. In the observation group, acupuncture was applied to the acupoints for "regaining consciousness, benefiting marrow and opening orifices", named Baihui (GV 20), Sishencong (EX-HN 1), Benshen (GB 13), Shenting (GV 24), and the bilateral yuan-primary points and luo-connecting points of the heart meridian, pericardium meridian and kidney meridian, as well as the acupoints along the affected meridians. Additionally, the rehabilitation was provided. In the control group, acupuncture at the acupoints along the affected meridians and rehabilitation were adopted. The treatment was given once a day, 5 times a week. After 8 weeks of treatment the evaluation was made. the indexes of unilateral spatial neglect such as line bisection test, the score of the mini-mental state examination (MMSE), the score of simple Fugl-Meyer motor function assessment and the modified Barthel indexes were adopted for the assessment of the severity of unilateral spatial neglect, cognitive function, motor function, and the activities of daily living. RESULTS: After treatment, the indexes of unilateral spatial neglect (line bisection test, line cancellation test, clock-drawing test and copying drawing test), MMSE score, the simple Fugl-Meyer motor function assessment and modified Barthel indexes were all improved as compared with those before treatment in the two groups (all P<0.01). The improvements in the observation group were more obvious than those in the control group (P<0.05, P<0.01). CONCLUSION: The combination of acupuncture treatment for "regaining consciousness, benefiting marrow and opening orifices" and rehabilitation much more effectively alleviates the severity of post-stroke unilateral spatial neglect and improves the motor function and the activities of daily living in the patients.

[Influence of electroacupuncture on spinal TNF-alpha and IL-6 contents in spinal cord ischemia-reperfusion injury rabbits].

OBJECTIVE: To observe the effect of electroacupuncture (EA) of "Zusanli" (ST 36)-"Quchi" (LI 11) on behavior changes and spinal inflammatory reactions in spinal ischemia-reperfusion injury (SI/RI) rabbits, so as to assess its protective effect on SI/RI. METHODS: Thirty New Zealand rabbits were randomly divided into sham-operation (sham), SI/RI model (model) and EA groups. SI/RI model was established by occlusion of the abdominal aorta for 45 min. EA (2 Hz, 1 mA) was applied to bilateral "Zusanli" (ST 36)-"Quchi" (LI 11) for 30 min after modeling, 4 times (0 h, 12 h, 24 h and 36 h after modeling) altogether. The animals' motor function score of the hindlimb was assessed according to Tarlov's method. The contents of tumor necrosis factor-alpha (TNF-alpha) and Interleukin-6 (IL-6) of the lumbar spinal cord tissue were assayed by ELISA 48 h after modeling. RESULTS: Compared with the sham group, the animals' motor scores at 24 h and 48 h after modeling were decreased, and spinal TNF-alpha and IL-6 contents were increased significantly (all P < 0.05) in the model group. In comparison with the model group, the animals' motor scores at both 24 h and 48 h were up-regulated considerably in the EA group (P < 0.05), suggesting an improvement of the neuronal function after EA intervention. The spinal TNF-alpha and IL-6 contents were obviously lower in the EA group than in the model group (P < 0.05). CONCLUSION: Electroacupuncture has a protective effect on the spinal cord ischemia- reperfusion injury of rabbits probably by reducing the local inflammatory reactions.

[Herbalism, botany and components analysis study on original plants of frankincense].

In order to clarify original plants of traditional Chinese medicine (TCM) frankincense, a GC method for determination essential oils and a HPLC method for determination boswellic acids were carried out together with analysis of herbalism, botany, components and pharmacology papers of frankincense. It was concluded that original plants of TCM frankincense include at least Boswellia sacra, B. papyrifera and B. serrata.

[Effect of acupuncture on the speech and acoustics level in patients with dysarthria].

OBJECTIVE: To observe the effect of acupuncture combined with speech therapy for dysarthria after stroke or cerebral trauma. METHODS: Sixty-one cases were randomly divided into two groups. The observation group (30 cases) was treated with speech therapy and acupuncture at Lianquan (CV 23), Jinjin (EX-HN 12), Yuye (EX-HN 13), Fengchi (GB 20), Yifeng (TE 17) and Wangu (GB 12) as major acupoints, while the control group (31 cases) was treated with speech therapy only. The changes of speech and acoustics indices were evaluated after 9 weeks treatment. RESULTS: The word articulation and correct rate of text of patients in two groups were both obviously improved after treatment (both P < 0.01). The total effective rate of 96.7% (29/30) in observation group was superior to that of 67.7% (21/31) in control group (P < 0.01). The maximum phonation time (MPT) of patients tested by aeromechanics analyzer were obviously prolonged in observation group (12 cases) and control group (11 cases) (both P < 0.01), and the improvement in observation group was more obvious (P < 0.01). CONCLUSION: Acupuncture combined with speech therapy can improve the effect on language and acoustics level for dysarthria.

[Study on chemical constituents in seeds of Helicia nilagirica (II)].

OBJECTIVE: To study the chemical constituents in seeds of Helicia nilagirica. METHOD: The ethanol extract was seperated by petroleum ether, dichloromethane, n-butanol in sequence, then isolated by silica gel column chromatography. The structures were identified and elucidated by physicochemical properties and spectral analysis. RESULT: Five compounds were isolated from the dichloromethane and n-butanol extracts, identified as p-hydroxybenzaldehyde (1), p-hydroxybenzoic acid (2), gallic acid (3), helicide (4), 4-formylpymyl-O-beta-D-glucopyranoside (5). CONCLUSION: All the compounds except IV were isolated from the plant for the first time. The compounds I, II and III were isolated from the genus Helicia for the first time.

[Studies on the chemical constituents of the stems of Alyxia sinensis (I)].

OBJECTIVE: To demonstrate the chemical constituents of Alyxia sinensis. METHOD: Phytochmical experiment was carried out, using column chromatograph technologies. RESULT: Five compounds have been isolated from the petroleum ether soluble part of the stems of A. sinensis. Their structures have been elucidated respectively as heptatriacontane(1), octatriacontane(2), 20-noatriacontannone(3), 20-nonatriacontanone(4), 20-tetraacontanoe(5), physcion(6), emodin(7), chrysophanol(8), coumarin(9), stigmasterol acetate(10), beta-sitosterol acetate(11), lupeol(12), betulin(13), stigmasterol(14), beta-sitosterol(15), ursolic acid(16), oleanolic acid(17). CONCLUSION: All these compounds are firstly been isolated from A. sinensis. And compound 5-9, 10, 11 are also been separated from Alyxiae genus for the first time.